KCNA5

Summary

Gene Symbol: KCNA5
Description: potassium voltage-gated channel subfamily A member 5
Alias: ATFB7, HCK1, HK2, HPCN1, KV1.5, PCN1, potassium voltage-gated channel subfamily A member 5, cardiac potassium channel, insulinoma and islet potassium channel, potassium channel 1, potassium channel, voltage gated shaker related subfamily A, member 5, potassium voltage-gated channel, shaker-related subfamily, member 5, voltage-gated potassium channel HK2, voltage-gated potassium channel protein Kv1.5, voltage-gated potassium channel subunit Kv1.5
Species: human

Top Publications

  1. ncbi Expression of voltage-gated potassium channels Kv1.3 and Kv1.5 in human gliomas
    Katja Preussat
    Institute of Pathology Neuropathology, Friedrich Schiller University Jena, Bachstrasse 18, D 07740 Jena, Germany
    Neurosci Lett 346:33-6. 2003
  2. pmc Structural determinants of Kvbeta1.3-induced channel inactivation: a hairpin modulated by PIP2
    Niels Decher
    Nora Eccles Harrison Cardiovascular Research and Training Institute, University of Utah, Salt Lake City, UT, USA
    EMBO J 27:3164-74. 2008
  3. pmc A mechanism for combinatorial regulation of electrical activity: Potassium channel subunits capable of functioning as Src homology 3-dependent adaptors
    M N Nitabach
    Department of Biology, New York University, New York, NY 10003, USA
    Proc Natl Acad Sci U S A 98:705-10. 2001
  4. ncbi Voltage-dependent potassium channels Kv1.3 and Kv1.5 in human cancer
    J Bielanska
    Molecular Physiology Laboratory, Departament de Bioquimica i Biologia Molecular, Facultat de Biologia, Universitat de Barcelona, E 08028 Barcelona, Spain
    Curr Cancer Drug Targets 9:904-14. 2009
  5. pmc Protein kinase C (PKC) activity regulates functional effects of Kvβ1.3 subunit on KV1.5 channels: identification of a cardiac Kv1.5 channelosome
    Miren David
    Instituto de Investigaciones Biomedicas, Madrid Consejo Superior de Investigaciones Científicas Universidad Autónoma de Madrid, c Arturo Duperier 4, 28029 Madrid, Spain
    J Biol Chem 287:21416-28. 2012
  6. ncbi Molecular basis of transient outward potassium current downregulation in human heart failure: a decrease in Kv4.3 mRNA correlates with a reduction in current density
    S Kaab
    Department of Medicine, Johns Hopkins University, Baltimore, Maryland, USA
    Circulation 98:1383-93. 1998
  7. ncbi Potassium channels Kv1.3 and Kv1.5 are expressed on blood-derived dendritic cells in the central nervous system
    Katherine M Mullen
    Department of Neurology, Johns Hopkins University, Baltimore, MD 21287, USA
    Ann Neurol 60:118-27. 2006
  8. ncbi Amino-terminal determinants of U-type inactivation of voltage-gated K+ channels
    Harley T Kurata
    Department of Physiology, University of British Columbia, Vancouver, British Columbia V6T 1Z3, Canada
    J Biol Chem 277:29045-53. 2002
  9. pmc Coupling of voltage sensing to channel opening reflects intrasubunit interactions in kv channels
    Alain J Labro
    Laboratory for Molecular Biophysics, Physiology and Pharmacology, Department of Biomedical Sciences, University of Antwerp, Antwerp 2610, Belgium
    J Gen Physiol 125:71-80. 2005
  10. ncbi Function of Kv1.5 channels and genetic variations of KCNA5 in patients with idiopathic pulmonary arterial hypertension
    Carmelle V Remillard
    Department of Medicine, University of California San Diego, 9500 Gilman Dr, MC 0725, La Jolla, CA 92093 0725, USA
    Am J Physiol Cell Physiol 292:C1837-53. 2007

Research Grants

  1. SRINIVAS TIPPARAJU; Fiscal Year: 2015
  2. ACTIVATION OF PROSTATE SPECIFIC ANTIGEN PRECURSOR
    Thomas Takayama; Fiscal Year: 2000
  3. Geoffrey W Abbott; Fiscal Year: 2015
  4. KALLIKREIN GENE EXPRESSION IN HUMAN PROSTATE CELLS
    Charles Young; Fiscal Year: 2002
  5. Biacore T100 SPR system for studying and characterizing biomolecular interaction
    Ewa Folta Stogniew; Fiscal Year: 2009
  6. Stephen L Archer; Fiscal Year: 2015
  7. Victoria L Seewaldt; Fiscal Year: 2015
  8. Andrew J Vickers; Fiscal Year: 2015
  9. Modulation of Kir Channel Function by Phosphorylation
    Diomedes E Logothetis; Fiscal Year: 2012
  10. Potassium channels in myotonic dystrophy type 1
    Christine Beeton; Fiscal Year: 2012

Detail Information

Publications434 found, 100 shown here

  1. ncbi Expression of voltage-gated potassium channels Kv1.3 and Kv1.5 in human gliomas
    Katja Preussat
    Institute of Pathology Neuropathology, Friedrich Schiller University Jena, Bachstrasse 18, D 07740 Jena, Germany
    Neurosci Lett 346:33-6. 2003
    ..This result corresponds to previous data on the expression of voltage-gated sodium channels in gliomas, which likewise showed a low or absent expression of channel subtypes in high-grade tumors...
  2. pmc Structural determinants of Kvbeta1.3-induced channel inactivation: a hairpin modulated by PIP2
    Niels Decher
    Nora Eccles Harrison Cardiovascular Research and Training Institute, University of Utah, Salt Lake City, UT, USA
    EMBO J 27:3164-74. 2008
    ..Taken together, our findings indicate that inactivation of Kv1.5 is mediated by an equilibrium binding of the N terminus of Kvbeta1.3 between phosphoinositides (PIPs) and the inner pore region of the channel...
  3. pmc A mechanism for combinatorial regulation of electrical activity: Potassium channel subunits capable of functioning as Src homology 3-dependent adaptors
    M N Nitabach
    Department of Biology, New York University, New York, NY 10003, USA
    Proc Natl Acad Sci U S A 98:705-10. 2001
    ..This is a mechanism for information transfer between subunits in heteromultimeric ion channels that is likely to underlie the generation of combinatorial signaling diversity in the control of cellular electrical excitability...
  4. ncbi Voltage-dependent potassium channels Kv1.3 and Kv1.5 in human cancer
    J Bielanska
    Molecular Physiology Laboratory, Departament de Bioquimica i Biologia Molecular, Facultat de Biologia, Universitat de Barcelona, E 08028 Barcelona, Spain
    Curr Cancer Drug Targets 9:904-14. 2009
    ..The concept of Kv channels as therapeutic targets or prognostic biomarkers attracts increasing interest and warrants further investigation...
  5. pmc Protein kinase C (PKC) activity regulates functional effects of Kvβ1.3 subunit on KV1.5 channels: identification of a cardiac Kv1.5 channelosome
    Miren David
    Instituto de Investigaciones Biomedicas, Madrid Consejo Superior de Investigaciones Científicas Universidad Autónoma de Madrid, c Arturo Duperier 4, 28029 Madrid, Spain
    J Biol Chem 287:21416-28. 2012
    ..5, K(v)β1.3, the receptor for activated C kinase (RACK1), PKCβI, PKCβII, and PKCθ in HEK293 cells. A very similar K(v)1.5 channelosome was found in rat ventricular tissue but not in atrial tissue...
  6. ncbi Molecular basis of transient outward potassium current downregulation in human heart failure: a decrease in Kv4.3 mRNA correlates with a reduction in current density
    S Kaab
    Department of Medicine, Johns Hopkins University, Baltimore, Maryland, USA
    Circulation 98:1383-93. 1998
    ..The mechanism for the reduction of Ito in heart failure is unknown. The K+ channel alpha-subunit Kv4.3, a homolog of the Drosophila Shal family, is most likely to encode all or part of the native cardiac Ito in humans...
  7. ncbi Potassium channels Kv1.3 and Kv1.5 are expressed on blood-derived dendritic cells in the central nervous system
    Katherine M Mullen
    Department of Neurology, Johns Hopkins University, Baltimore, MD 21287, USA
    Ann Neurol 60:118-27. 2006
    ..We examined K(+) channels on dendritic cells (DCs), which infiltrate the brain in MS and may impact disease course...
  8. ncbi Amino-terminal determinants of U-type inactivation of voltage-gated K+ channels
    Harley T Kurata
    Department of Physiology, University of British Columbia, Vancouver, British Columbia V6T 1Z3, Canada
    J Biol Chem 277:29045-53. 2002
    ..1. These data suggest that intersubunit T1 domain interactions influence U-type inactivation in Kv1 channels, and suggest a generalized influence of the T1 domain on U-type inactivation between Kv channel subfamilies...
  9. pmc Coupling of voltage sensing to channel opening reflects intrasubunit interactions in kv channels
    Alain J Labro
    Laboratory for Molecular Biophysics, Physiology and Pharmacology, Department of Biomedical Sciences, University of Antwerp, Antwerp 2610, Belgium
    J Gen Physiol 125:71-80. 2005
    ..With each mutation in a separate subunit of a tandem, this compensation did not occur. This suggests that for Kv channels, the coupling between voltage sensing and gating reflects primarily an intrasubunit interaction...
  10. ncbi Function of Kv1.5 channels and genetic variations of KCNA5 in patients with idiopathic pulmonary arterial hypertension
    Carmelle V Remillard
    Department of Medicine, University of California San Diego, 9500 Gilman Dr, MC 0725, La Jolla, CA 92093 0725, USA
    Am J Physiol Cell Physiol 292:C1837-53. 2007
    ..Here, we report that overexpression of the Kv1.5 channel gene (KCNA5) in human PASMC and other cell lines produced a 15-pS single channel current and a large whole cell current that ..
  11. ncbi Mitochondrial metabolism, redox signaling, and fusion: a mitochondria-ROS-HIF-1alpha-Kv1.5 O2-sensing pathway at the intersection of pulmonary hypertension and cancer
    Stephen L Archer
    University of Chicago, Section of Cardiology, IL 60637, USA
    Am J Physiol Heart Circ Physiol 294:H570-8. 2008
    ..Mitochondrial abnormalities that disturb the ROS-HIF-1alpha-Kv1.5 O(2)-sensing pathway contribute to the pathogenesis of PAH and cancer and constitute promising therapeutic targets...
  12. pmc Kv1.5 association modifies Kv1.3 traffic and membrane localization
    Rubén Vicente
    Molecular Physiology Laboratory, Departament de Bioquimica i Biologia Molecular, Institut de Biomedicina, Universitat de Barcelona, Barcelona, Spain
    J Biol Chem 283:8756-64. 2008
    ..3 and Kv1.5 targeting to rafts. Our results implicate the traffic and localization of Kv1.3/Kv1.5 heteromers in the complex regulation of immune system cells...
  13. doi The anchoring protein SAP97 retains Kv1.5 channels in the plasma membrane of cardiac myocytes
    Joëlle Abi-Char
    INSERM UMR 621, Faculté de Médecine Pierre Marie Curie, 91 Boulevard de l Hopital, 75013 Paris, France
    Am J Physiol Heart Circ Physiol 294:H1851-61. 2008
    ..In conclusion, SAP97 regulates the K(+) current in cardiac myocytes by retaining and immobilizing Kv1.5 subunits in the plasma membrane. This new regulatory mechanism may contribute to the targeting of Kv channels in cardiac myocytes...
  14. doi Four and a half LIM protein 1: a partner for KCNA5 in human atrium
    Zhenjiang Yang
    Department of Medicine, Vanderbilt University School of Medicine, Nashville, TN 37232 6602, USA
    Cardiovasc Res 78:449-57. 2008
    ..In human heart, the Shaker-related voltage-gated K(+) channel KCNA5 alpha-subunit forms the major basis of an atrial-specific, ultra-rapid delayed rectifier K(+) current, I(Kur)...
  15. doi Novel KCNA5 loss-of-function mutations responsible for atrial fibrillation
    Yiqing Yang
    Department of Cardiology, Tongji Hospital, Tongji University School of Medicine, Shanghai, China
    J Hum Genet 54:277-83. 2009
    ..However, the molecular defects in most patients with AF remain to be identified. Here, we report on three novel KCNA5 mutations that were identified in 4 of 120 unrelated AF families...
  16. pmc Tetramerization domain mutations in KCNA5 affect channel kinetics and cause abnormal trafficking patterns
    Elyssa D Burg
    Dept of Medicine, Univ of California, San Diego, 9500 Gilman Dr, MC 0725, La Jolla, CA 92093 0725, USA
    Am J Physiol Cell Physiol 298:C496-509. 2010
    ..We recently reported two nonsynonymous mutations (G182R and E211D) in the KCNA5 gene of patients with idiopathic pulmonary arterial hypertension, which localize to the T1 domain of KCNA5...
  17. doi Association of a KCNA5 gene polymorphism with systemic sclerosis-associated pulmonary arterial hypertension in the European Caucasian population
    J Wipff
    Universite Paris Descartes, INSERM U781, Hopital Necker, and Hôpital Cochin, Paris, France
    Arthritis Rheum 62:3093-100. 2010
    ..genes have also been advocated, including potassium voltage-gated channel, shaker-related subfamily, member 5 (KCNA5)...
  18. pmc Novel KCNA5 mutation implicates tyrosine kinase signaling in human atrial fibrillation
    Tao Yang
    Department of Medicine, Vanderbilt University School of Medicine, Nashville, Tennessee 37323 6602, USA
    Heart Rhythm 7:1246-52. 2010
    Emerging evidence has strongly implicated hereditary determinants for atrial fibrillation (AF). Loss-of-function mutations in KCNA5 encoding the ultrarapid delayed rectifier potassium current I(Kur) have been identified in AF families.
  19. doi Genetic variation in KCNA5: impact on the atrial-specific potassium current IKur in patients with lone atrial fibrillation
    Ingrid E Christophersen
    Danish National Research Foundation Centre for Cardiac Arrhythmia and Department of Biomedical Sciences, Faculty of Health and Medical Sciences, University of Copenhagen, Blegdamsvej 3, Copenhagen N, Denmark
    Eur Heart J 34:1517-25. 2013
    Genetic factors may be important in the development of atrial fibrillation (AF) in the young. KCNA5 encodes the potassium channel α-subunit KV1.5, which underlies the voltage-gated atrial-specific potassium current IKur...
  20. ncbi Molecular cloning and characterization of two voltage-gated K+ channel cDNAs from human ventricle
    M M Tamkun
    Department of Molecular Physiology and Biophysics, Vanderbilt University School of Medicine, Nashville, Tennessee 37205
    FASEB J 5:331-7. 1991
    ..These two cDNAs, designated HK1 and HK2, encode proteins of 653 and 605 amino acids, respectively...
  21. ncbi Gating of shaker-type channels requires the flexibility of S6 caused by prolines
    Alain J Labro
    Laboratory for Molecular Biophysics, Physiology and Pharmacology, Department of Biomedical Sciences, University of Antwerp, Universiteitsplein 1, 2610 Antwerp, Belgium
    J Biol Chem 278:50724-31. 2003
    ..These results indicate that the destabilization or bending of the S6 alpha-helix caused by the PXP motif apparently creates a flexible "hinge" that allows movement of the lower S6 segment during channel gating and opening...
  22. ncbi Molecular basis for Kv1.5 channel block: conservation of drug binding sites among voltage-gated K+ channels
    Niels Decher
    University of Utah, Department of Physiology, Eccles Institute of Human Genetics, Salt Lake City, Utah 84112, USA
    J Biol Chem 279:394-400. 2004
    ..Based on the homology models, the positions of the five amino acids identified to interact with S0100176 face toward the central cavity and overlap with putative binding sites for other blockers and voltage-gated potassium channels...
  23. ncbi Overexpression of human KCNA5 increases IK V and enhances apoptosis
    Elena E Brevnova
    Division of Pulmonary and Critical Care Medicine, Dept of Medicine, Medical Teaching Facility, University of California San Diego, 0725, 9500 Gilman Drive, La Jolla, CA 92093 0725, USA
    Am J Physiol Cell Physiol 287:C715-22. 2004
    ..The objective of this study was to test the hypothesis that overexpression of KCNA5, which encodes a delayed-rectifier voltage-gated K+ (Kv) channel, increases K+ currents and enhances apoptosis...
  24. pmc Antiarrhythmic drug-induced internalization of the atrial-specific k+ channel kv1.5
    Sarah M Schumacher
    Department of Pharmacology, 1301 MSRBIII, 1150 W Medical Center Dr, Ann Arbor, MI 48109 0632, USA
    Circ Res 104:1390-8. 2009
    ....
  25. pmc Stereoselective block of a human cardiac potassium channel (Kv1.5) by bupivacaine enantiomers
    C Valenzuela
    Institute of Pharmacology and Toxicology, CSIC, School of Medicine, Universidad Complutense, Madrid, Spain
    Biophys J 69:418-27. 1995
    ..We studied the effects of the enantiomers of bupivacaine on a cloned human cardiac potassium channel (hKv1.5)...
  26. ncbi High affinity of ergopeptides for cytochromes P450 3A. Importance of their peptide moiety for P450 recognition and hydroxylation of bromocriptine
    M A Peyronneau
    Laboratoire de Chimie et Biochimie Pharmacologiques et Toxicologiques Unité de Recherche Associée au CNRS URA 400, Universite Rene Descartes, France
    Eur J Biochem 223:947-56. 1994
    ..Very similar results were observed with two allelic forms of human liver P450 3A4, P450 NF25 and P450 hPCN1, produced in yeast. In both cases all the ergopeptides studied showed high affinities for the P450s (Ks 0.6-2...
  27. doi Effect of noble gases on oxygen and glucose deprived injury in human tubular kidney cells
    Maleeha Rizvi
    Anaesthetics, Pain Medicine and Intensive Care, Department of Surgery and Cancer, Imperial College London, London, UK
    Exp Biol Med (Maywood) 235:886-91. 2010
    ..the protective effects of the other noble gases, helium, neon, argon, krypton and xenon, on human tubular kidney HK2 cells in vitro...
  28. pmc Mechanism of block of a human cardiac potassium channel by terfenadine racemate and enantiomers
    T Yang
    Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, Tennessee 37232, USA
    Br J Pharmacol 115:267-74. 1995
    ..the mechanism of action of the racemate, both enantiomers and a major metabolite on a cloned human cardiac potassium channel, hKv1.5...
  29. ncbi Measurement of prostate-specific antigen and human glandular kallikrein 2 in different body fluids
    J Lovgren
    Department of Laboratory Medicine, Lund University, University Hospital, Malmo, Sweden
    J Androl 20:348-55. 1999
    ..Investigations have shown that human glandular kallikrein 2 (hK2), a related prostate-secreted protease, can activate the zymogen form of PSA, suggesting that the two enzymes might ..
  30. ncbi Expression of voltage-gated K+ channels in human atrium
    Federica Bertaso
    Cell Signalling Group, Department of Renal Medicine, Guy s, King s and St Thomas School of Medicine, King s College London, Bessemer Road, London, SE5 7PJ, United Kingdom
    Basic Res Cardiol 97:424-33. 2002
    ..2 and Kv2.1 is consistent with the major contribution of Kv1.5 to this current. The physiological significance of the expression of KvLQT1 and Kv1.4 mRNA in the human atrium warrants further investigation...
  31. ncbi The effects of quinidine and its chiral isolates on erg-1sm potassium current and correlation with gastrointestinal augmentation
    Ivana Cvetanovic
    Department of Pharmacology and Medicine, Rush University Medical Center, Chicago, Illinois, USA
    Am J Ther 14:269-76. 2007
    ..Because quinidine inhibits cardiac potassium channel and as a result augments gastrointestinal contractility, it was thought that quinidine may affect erg1-..
  32. ncbi Expression of prostate-specific antigen (PSA) and human glandular kallikrein 2 (hK2) in ileum and other extraprostatic tissues
    A Yvonne Olsson
    Department of Laboratory Medicine, Lund University, University Hospital UMAS, S 205 02 Malmo, Sweden
    Int J Cancer 113:290-7. 2005
    ..comprehensive study of the tissue distribution of PSA and the closely related protein human glandular kallikrein 2 (hK2)...
  33. ncbi Atrial-selective antiarrhythmic actions of novel Ikur vs. Ikr, Iks, and IKAch class Ic drugs and beta blockers in pigs
    Karsten Knobloch
    DG Cardiovascular Diseases, Aventis Pharma, Frankfurt am Main, Germany
    Med Sci Monit 10:BR221-8. 2004
    ....
  34. pmc Slow gating charge immobilization in the human potassium channel Kv1.5 and its prevention by 4-aminopyridine
    D Fedida
    Department of Physiology, Queen s University, Kingston, Ontario, Canada
    J Physiol 494:377-87. 1996
    ..Some actions of 4-AP appear independent of its properties as a blocker of open K+ channels, and are not mimicked by internal TEA...
  35. ncbi Properties of a time-dependent potassium current in pig atrium: evidence for a role of kv1.5 in repolarization
    Joachim R Ehrlich
    Division of Cardiology, J W Goethe University, Theodor Stern Kai 7, 60590 Frankfurt, Germany
    J Pharmacol Exp Ther 319:898-906. 2006
    ..5 expression, and shows a pharmacological profile typical of K(v)1.5-dependent currents...
  36. pmc Human axons contain at least five types of voltage-dependent potassium channel
    G Reid
    Sobell Department of Neurophysiology, Institute of Neurology, Queen Square, London WC1N 3BG, UK
    J Physiol 518:681-96. 1999
    ..At least five channel types exist, and their characteristics overlap to a considerable extent...
  37. doi High-throughput analysis of drug binding interactions for the human cardiac channel, Kv1.5
    Jerzy Karczewski
    Department of Pain Research, Merck Research Laboratories, West Point, PA 19486, USA
    Biochem Pharmacol 77:177-85. 2009
    ....
  38. doi Shared requirement for dynein function and intact microtubule cytoskeleton for normal surface expression of cardiac potassium channels
    Matthew E Loewen
    Dept of Anesthesiology, Pharmacology and Therapeutics, University of British Columbia, 2350 Health Sciences Mall, Vancouver, BC, Canada V6T 1Z3
    Am J Physiol Heart Circ Physiol 296:H71-83. 2009
    ..channels at the cardiomyocyte surface must eventually be internalized and degraded, and changes in cardiac potassium channel expression are known to occur during myocardial disease...
  39. ncbi Cytochrome P-450 hPCN3, a novel cytochrome P-450 IIIA gene product that is differentially expressed in adult human liver. cDNA and deduced amino acid sequence and distinct specificities of cDNA-expressed hPCN1 and hPCN3 for the metabolism of steroid hormo
    T Aoyama
    Laboratory of Molecular Carcinogenesis, National Cancer Institute, Bethesda, Maryland 20892
    J Biol Chem 264:10388-95. 1989
    Immunoblotting analysis of human liver microsome preparations revealed that human cytochrome P-450 PCN1 (hPCN1, Mr approximately 52,000) was expressed in each of 40 individual specimens examined...
  40. ncbi Identification of the transcriptional regulatory sequences of human kallikrein 2 and their use in the construction of calydon virus 764, an attenuated replication competent adenovirus for prostate cancer therapy
    D C Yu
    Calydon, Inc, Sunnyvale, California 94089, USA
    Cancer Res 59:1498-504. 1999
    Human glandular kallikrein (hK2) and prostate-specific antigen (PSA) are related members of the human kallikrein gene family...
  41. ncbi Similar rates of exponential decrease in serum concentrations of free prostate-specific antigen (PSA), PSA complexed to alpha-1-antichymotrypsin, and human glandular kallikrein 2 (hK2) in prostate cancer patients treated with GnRH-analogues
    T Bjork
    Department of Urology, Malmö and Lund University Hospitals, Lund University, Malmo, Sweden
    Prostate 47:14-20. 2001
    ..In addition, serum concentrations of hK2, the activator of proPSA, were measured.
  42. pmc Kv1.5 is a major component underlying the A-type potassium current in retinal arteriolar smooth muscle
    Mary K McGahon
    Centre of Vision Sciences, The Queen s University of Belfast, Institute of Clinical Sciences, The Royal Victoria Hospital, Grosvenor Road, Belfast BT12 6BA UK
    Am J Physiol Heart Circ Physiol 292:H1001-8. 2007
    ..The findings of this study suggest that K(v)1.5, most likely co-assembled with K(v)beta1 subunits, comprises a major component underlying the A-type K(+) current in retinal arteriolar smooth muscle cells...
  43. ncbi Serpin-derived peptide substrates for investigating the substrate specificity of human tissue kallikreins hK1 and hK2
    L Bourgeois
    Laboratory of Enzymology and Protein Chemistry, CNRS EP 117, University Francois Rabelais, 37032 Tours, France
    J Biol Chem 272:29590-5. 1997
    The third human tissue kallikrein to be identified, hK2, could be an alternate or complementary marker to kallikrein hK3 (prostate-specific antigen) for prostate diseases...
  44. ncbi Enzymatic action of human glandular kallikrein 2 (hK2). Substrate specificity and regulation by Zn2+ and extracellular protease inhibitors
    J Lovgren
    Department of Laboratory Medicine, Lund University, Malmo, Sweden
    Eur J Biochem 262:781-9. 1999
    Human glandular kallikrein 2 (hK2) is a serine protease expressed by the prostate gland with 80% identity in primary structure to prostate-specific antigen (PSA)...
  45. pmc Structural investigation of the alpha-1-antichymotrypsin: prostate-specific antigen complex by comparative model building
    B O Villoutreix
    Technical Research Centre of Finland, Espoo, Finland
    Protein Sci 5:836-51. 1996
    ..the human kallikrein family of enzymes, a second prostate-derived member of which is human glandular kallikrein-1 (hK2). Active PSA and hK2 are both 237-residue kallikrein-like proteases, based on sequence homology...
  46. doi Dichloroacetate shifts the metabolism from glycolysis to glucose oxidation and exhibits synergistic growth inhibition with cisplatin in HeLa cells
    Jing Xie
    Department of Pharmacology and Biostatistics, Institute of Medical Sciences, Shanghai Jiao Tong University School of Medicine, Shanghai 200025, PR China
    Int J Oncol 38:409-17. 2011
    ....
  47. ncbi KVLQT1 C-terminal missense mutation causes a forme fruste long-QT syndrome
    C Donger
    INSERM U153, Groupe Hospitalier Pitie Salpetriere, Institut de Myologie, Paris, France
    Circulation 96:2778-81. 1997
    KVLQT1, the gene encoding the alpha-subunit of a cardiac potassium channel, is the most common cause of the dominant form of long-QT syndrome (LQT1-type), the Romano-Ward syndrome (RWS)...
  48. ncbi Kallikrein 4 (hK4) and prostate-specific antigen (PSA) are associated with the loss of E-cadherin and an epithelial-mesenchymal transition (EMT)-like effect in prostate cancer cells
    T L Veveris-Lowe
    School of Life Sciences and Science Research Centre, Queensland University of Technology, Brisbane, Australia
    Endocr Relat Cancer 12:631-43. 2005
    ..protein in prostate cancer tissues, compared with benign glands, is greater than that of PSA and kallikrein 2 (KLK2/hK2), suggesting that hK4 may play an important functional role in prostate cancer progression in addition to its ..
  49. ncbi Cardiac glycosides as novel inhibitors of human ether-a-go-go-related gene channel trafficking
    Lu Wang
    Rammelkamp Center for Education and Research, Case Western Reserve University, Cleveland, OH 44109, USA
    J Pharmacol Exp Ther 320:525-34. 2007
    Direct block of the cardiac potassium channel human ether-a-go-go-related gene (hERG) by a large, structurally diverse group of therapeutic compounds causes drug-induced QT prolongation and torsades de pointes arrhythmias...
  50. doi Stabilizing effects of eicosapentaenoic acid on Kv1.5 channel protein expressed in mammalian cells
    Shunya Koshida
    Division of Regenerative Medicine and Therapeutics, Department of Genetic Medicine and Regenerative Therapeutics, Institute of Regenerative Medicine and Biofunction, Tottori University Graduate School of Medical Science, Nishimachi 86, Yonago 683, Japan
    Eur J Pharmacol 604:93-102. 2009
    ..These results indicate that chronic treatment with EPA at lower concentrations stabilizes Kv1.5 channel protein in the endoplasmic reticulum and Golgi apparatus thereby enhancing the Kv1.5 channel current on the cell membrane...
  51. ncbi Human tissue kallikrein 5 is a member of a proteolytic cascade pathway involved in seminal clot liquefaction and potentially in prostate cancer progression
    Iacovos P Michael
    Department of Pathology and Laboratory Medicine, Mount Sinai Hospital, Toronto, Ontario M5G 1X5, Canada
    J Biol Chem 281:12743-50. 2006
    ..the activation site of each kallikrein and recombinant pro-hKs, we demonstrated that hK5 is able to activate pro-hK2 and pro-hK3. We then showed that, following their activation, hK5 can internally cleave and deactivate hK2 and hK3...
  52. ncbi Mutant recombinant serpins as highly specific inhibitors of human kallikrein 14
    Loyse M Felber
    Urology Research Unit, Department of Urology, CHUV, Epalinges, Switzerland
    FEBS J 273:2505-14. 2006
    ..the construction of alpha1-antichymotrypsin (ACT) variants with high specificity towards human kallikrein 2 (hK2) [Cloutier SM, Kündig C, Felber LM, Fattah OM, Chagas JR, Gygi CM, Jichlinski P, Leisinger HJ & Deperthes D (..
  53. pmc SUMO modification regulates inactivation of the voltage-gated potassium channel Kv1.5
    Mark D Benson
    Department of Pharmacology, University of Michigan Medical School, Ann Arbor, MI 48109 0632, USA
    Proc Natl Acad Sci U S A 104:1805-10. 2007
    ..Reversible control of voltage-sensitive channels through SUMOylation constitutes a unique and likely widespread mechanism for adaptive tuning of the electrical excitability of cells...
  54. doi Modulation of the voltage-gated potassium channel Kv1.5 by the SGK1 protein kinase involves inhibition of channel ubiquitination
    Christoph Boehmer
    Department of Physiology I, University of Tubingen, Tubingen, Germany
    Cell Physiol Biochem 22:591-600. 2008
    ..5 stabilization in the plasma membrane. Our results suggest that the kinase might participate in the regulation of insulin secretion in part by controlling Kv1.5 surface abundance...
  55. pmc Aging and muscle fiber type alter K+ channel contributions to the myogenic response in skeletal muscle arterioles
    Lori S Kang
    Department of Physiology and Pharmacology, West Virginia University School of Medicine, Morgantown, WV, USA
    J Appl Physiol (1985) 107:389-98. 2009
    ....
  56. doi Effects of lobeline, a nicotinic receptor ligand, on the cloned Kv1.5
    Imju Jeong
    Department of Physiology, Medical Research Center, College of Medicine, The Catholic University of Korea, 505 Banpo Dong, Socho gu, Seoul, 137 701, South Korea
    Pflugers Arch 460:851-62. 2010
    ..7, 28.2, and 0.34 μM, respectively. These results indicate that lobeline produces a concentration-, time-, voltage-, and use-dependent inhibition of Kv1.5, which can be interpreted as an open-channel block mechanism...
  57. ncbi Sinus node function and ventricular repolarization during exercise stress test in long QT syndrome patients with KvLQT1 and HERG potassium channel defects
    H Swan
    Department of Medicine, Helsinki University Central Hospital, Finland
    J Am Coll Cardiol 34:823-9. 1999
    ..This study was performed to evaluate the QT interval and heart rate responses to exercise and recovery in gene and mutation type-specific subgroups of long QT syndrome (LQTS) patients...
  58. pmc Risk assessment for biochemical recurrence prior to radical prostatectomy: significant enhancement contributed by human glandular kallikrein 2 (hK2) and free prostate specific antigen (PSA) in men with moderate PSA-elevation in serum
    Thomas Steuber
    Department of Urology, Memorial Sloan Kettering Cancer Center, New York, NY, USA
    Int J Cancer 118:1234-40. 2006
    ..We investigated whether human glandular kallikrein 2 (hK2) and free prostate-specific antigen (fPSA) measured in pretreatment serum enhance prediction...
  59. ncbi Human Kallikrein 2 (hK2) and prostate-specific antigen (PSA): two closely related, but distinct, kallikreins in the prostate
    H G Rittenhouse
    Research and Development Department, Hybritech Incorporated, Beckman Coulter, Inc, San Diego, California, USA
    Crit Rev Clin Lab Sci 35:275-368. 1998
    Recent studies on human kallikrein 2 (hK2) have revealed striking similarities and significant differences with the closely related kallikrein PSA...
  60. ncbi Highly sensitive automated chemiluminometric assay for measuring free human glandular kallikrein-2
    G G Klee
    Departments of Laboratory Medicine and Pathology, Epidemiology, and Urology Research, Mayo Clinic and Mayo Foundation, 200 First Street SW, Rochester, MN 55905, USA
    Clin Chem 45:800-6. 1999
    Human glandular kallikrein (hK2) is a serine protease that has 79% amino acid identity with prostate-specific antigen (PSA). Both free hK2 and hK2 complexed to alpha1-antichymotrypsin (ACT) are present in the blood in low concentrations...
  61. ncbi Angiotensin IV stimulates plasminogen activator inhibitor-1 expression in proximal tubular epithelial cells
    L Gesualdo
    Dipartimento dell Emergenza e dei Trapianti di Organi, Sezione di Nefrologia, Policlinico, Bari, Italy
    Kidney Int 56:461-70. 1999
    ..PAI-1 induction by Ang II in endothelial cells seems to be mediated by Ang IV via a receptor that is different from Ang II type 1 and 2 receptors (AT1 and AT2)...
  62. ncbi Cloning, expression analysis and chromosome mapping of human casein kinase 1 gamma1 (CSNK1G1): identification of two types of cDNA encoding the kinase protein associated with heterologous carboxy-terminal sequences
    J Kusuda
    Division of Genetic Resources, National Institute of Infectious Diseases, Tokyo, Japan
    Cytogenet Cell Genet 90:298-302. 2000
    ..We have isolated two types of cDNA for human casein kinase 1 gamma1 (hCK1 gamma1)...
  63. ncbi Insulin-like growth factor binding proteins (IGFBPs) as potential physiological substrates for human kallikreins hK2 and hK3
    S Rehault
    Laboratoire d Enzymologie et Chimie des Protéines, INSERM Université François Rabelais, Tours, France
    Eur J Biochem 268:2960-8. 2001
    ..To elucidate the putative biological role of prostatic kallikreins hK2 and hK3 (prostate-specific antigen) in tumour progression, we analyzed the degradation of IGFBP-2, -3, -4 and -5 by ..
  64. ncbi Development of a dual monoclonal antibody immunoassay for total human kallikrein 2
    J A Finlay
    Research Department, Hybritech Inc, a subsidiary of Beckman Coulter, Inc, San Diego, CA 92121, USA
    Clin Chem 47:1218-24. 2001
    Human kallikrein 2 (hK2) shares 80% sequence identity with prostate-specific antigen (PSA)...
  65. ncbi Prognostic value of combined "triple"-reverse transcription-PCR analysis for prostate-specific antigen, human kallikrein 2, and prostate-specific membrane antigen mRNA in peripheral blood and lymph nodes of prostate cancer patients
    Ralf Kurek
    Department of Anatomy and Cell Biology, Philipps University, Marburg, Germany
    Clin Cancer Res 10:5808-14. 2004
    ....
  66. ncbi Activation of the zymogen form of prostate-specific antigen by human glandular kallikrein 2
    J Lovgren
    Department of Clinical Chemistry, Lund University Hospital, Malmo, S 205 02, Sweden
    Biochem Biophys Res Commun 238:549-55. 1997
    Prostate-specific antigen (PSA) and human glandular kallikrein 2 (hK2) are glandular kallikreins secreted by the prostate gland...
  67. ncbi Human glandular kallikrein, hK2, shows arginine-restricted specificity and forms complexes with plasma protease inhibitors
    S D Mikolajczyk
    Hybritech Incorporated, San Diego, CA 92196 9006, USA
    Prostate 34:44-50. 1998
    Human glandular kallikrein (hK2) is a new potential marker for prostate cancer. It is a serine protease expressed in human prostate epithelial cells which has 78% sequence identity with prostate-specific antigen (PSA)...
  68. pmc Single point mutations located outside the inter-monomer domains abolish trimerization of Schizosaccharomyces pombe PCNA
    K Piard
    UPR9044, IFC1 CNRS, 7 rue Guy Moquet, 94801 Villejuif, France
    Nucleic Acids Res 26:2598-605. 1998
    ..for lethal mutations by testing for lack of complementation of a Schizosaccharomyces pombe strain disrupted for the pcn1 + gene. We thus identified eight lethal mutants out of the 50 cDNAs tested...
  69. ncbi The 1997 Stevenson Award Lecture. Cardiac K+ channel gating: cloned delayed rectifier mechanisms and drug modulation
    D Fedida
    Department of Physiology, Queen s University, Kingston, ON, Canada
    Can J Physiol Pharmacol 76:77-89. 1998
    ..In this way we can uncover the detailed mechanisms of action of K+ channel blockers such as tetraethylammonium ions and 4-aminopyridine, and antiarrhythmic agents such as nifedipine and quinidine...
  70. ncbi alpha2-macroglobulin and C1-inactivator are plasma inhibitors of human glandular kallikrein
    M J Heeb
    Departments of Molecular and Experimental Medicine and of Vascular Biology, The Scripps Research Institute, La Jolla, CA
    Blood Cells Mol Dis 24:412-9. 1998
    Human glandular kallikrein (hK2) is a possible new marker for prostate cancer that is homologous to prostate specific antigen...
  71. ncbi Detection of extraprostatic prostate cells utilizing reverse transcription-polymerase chain reaction
    S L Su
    Northwest Biotherapeutics, Inc, Seattle, Washington 98125, USA
    Semin Surg Oncol 18:17-28. 2000
    ..are prostate-specific antigen (PSA), prostate-specific membrane antigen (PSMA), and human glandular kallikrein-2 (hK2). False positives among negative controls are low...
  72. ncbi Targeted replacement of KV1.5 in the mouse leads to loss of the 4-aminopyridine-sensitive component of I(K,slow) and resistance to drug-induced qt prolongation
    B London
    Cardiovascular Institute, University of Pittsburgh, Pittsburgh, PA, USA
    Circ Res 88:940-6. 2001
    ..1 may explain the phenotypic differences between SWAP mice and the previously described transgenic mice expressing a truncated dominant-negative Kv1.1 construct...
  73. ncbi Characterization of androgen receptor and nuclear receptor co-regulator expression in human breast cancer cell lines exhibiting differential regulation of kallikreins 2 and 3
    Angeliki Magklara
    Department of Pathology and Laboratory Medicine, Mount Sinai Hospital, Toronto, Ontario, Canada
    Int J Cancer 100:507-14. 2002
    ..regulation of 2 known androgen-regulated kallikreins, KLK3 (encoding PSA) and KLK2 (encoding human kallikrein 2 or hK2) in BT-474, T-47D, ZR75-1, MCF-7, MFM-223 and BT-20 human breast cancer cells and found that they were ..
  74. ncbi Identification, synthesis, and activity of novel blockers of the voltage-gated potassium channel Kv1.5
    Stefan Peukert
    Aventis Pharma Deutschland GmbH, Medicinal Chemistry and DG Cardiovascular, D 65926 Frankfurt Main, Germany
    J Med Chem 46:486-98. 2003
    ..3 and no significant effect on the HERG channel and sodium currents. In addition, compounds 17c and 17m have already shown antiarrhythmic effects in a pig model...
  75. ncbi Circadian variation of cardiac K+ channel gene expression
    Takeshi Yamashita
    The Cardiovascular Institute, Roppongi 7 3 10, Minato ku, Tokyo 106 0032, Japan
    Circulation 107:1917-22. 2003
    ....
  76. ncbi The discovery of Kv1.5 blockers as a case study for the application of virtual screening approaches
    Bernard Pirard
    Aventis Pharma Deutschland GmbH, a Company of the Sanofi Aventis Group, Computational Chemistry, Medicinal Chemistry, Industrie Park Höchst, Building G878, D 65926 Frankfurt am Main, Germany
    J Chem Inf Model 45:477-85. 2005
    ..The analysis of the results supports the conventional wisdom of using as many virtual screening techniques as possible in order to maximize the chance of finding as many chemotypes as possible...
  77. ncbi Activity- and mTOR-dependent suppression of Kv1.1 channel mRNA translation in dendrites
    Kimberly F Raab-Graham
    Howard Hughes Medical Institute, Departments of Physiology and Biochemistry, University of California, San Francisco, CA 94158, USA
    Science 314:144-8. 2006
    ..1 synthesis in dendrites upon inhibition of mTOR or the N-methyl-d-aspartate (NMDA) glutamate receptor. Thus, synaptic excitation may cause local suppression of dendritic Kv1 channels by reducing their local synthesis...
  78. ncbi Electrophysiological properties of human adipose tissue-derived stem cells
    Xiaowen Bai
    Department of Molecular Pathology, University of Texas, MD Anderson Cancer Center, Houston, Texas 77054, USA
    Am J Physiol Cell Physiol 293:C1539-50. 2007
    ..TTX) are present in undifferentiated hASCs and their potential physiological function in these cells as a basic understanding for future in vitro experiments and in vivo clinical investigations...
  79. pmc Voltage clamp fluorimetry reveals a novel outer pore instability in a mammalian voltage-gated potassium channel
    Moninder Vaid
    Department of Anesthesiology, Pharmacology, and Therapeutics, University of British Columbia, Vancouver, BC V6T 1Z3, Canada
    J Gen Physiol 132:209-22. 2008
    ....
  80. doi URG11 mediates hypoxia-induced epithelial-to-mesenchymal transition by modulation of E-cadherin and beta-catenin
    Rui Du
    Department of Nephrology, Xijing Hospital, Fourth Military Medical University, Xi an, PR China
    Biochem Biophys Res Commun 391:135-41. 2010
    ..Overexpression of URG11 in a human proximal tubule cell line (HK2) promoted a mesenchymal phenotype accompanied by reduced expression of the epithelial marker E-cadherin and ..
  81. doi Aconitine blocks HERG and Kv1.5 potassium channels
    Yifu Li
    Ion Channelopathy Research Center, Institute of Cardiology, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430022, PR China
    J Ethnopharmacol 131:187-95. 2010
    ..Aconitine (ACO), a diterpenoid alkaloid from aconitum, mainly contributes to cardio-toxic effects of aconitum and has also been commonly known to induce arrhythmias in animal models. However, its pro-arrhythmic mechanisms are not clear...
  82. pmc Molecular determinants of pentamidine-induced hERG trafficking inhibition
    Adrienne T Dennis
    Rammelkamp Center for Education and Research, MetroHealth Campus, Cleveland, OH 44109, USA
    Mol Pharmacol 81:198-209. 2012
    ..At the same time, pentamidine reduces surface expression of the cardiac potassium channel I(Kr)/human ether à-go-go-related gene (hERG)...
  83. pmc Fasting induces the expression of PGC-1α and ERR isoforms in the outer stripe of the outer medulla (OSOM) of the mouse kidney
    Christina T Teng
    Biomolecular Screening Branch, National Institute of Environmental Health Sciences, National Institutes of Health, Research Triangle Park, North Carolina, United States of America
    PLoS ONE 6:e26961. 2011
    ..We found that PGC-1α, ERRα and ERRγ was highly expressed in human kidney HK2 cells and that PGC-1α induced dynamic protein interactions on the ERRα chromatin...
  84. doi Activation of voltage gated K⁺ channel Kv1.5 by β-catenin
    Carlos Munoz
    Department of Physiology, University of Tubingen, Gmelinstr 5, D 72076 Tubingen, Germany
    Biochem Biophys Res Commun 417:692-6. 2012
    ..5 requires the same protein domains that are required for association of β-catenin with cadherin. The experiments disclose a completely novel function of β-catenin, i.e. the regulation of Kv1.5 channel activity...
  85. ncbi [Effects of puerarin on proliferation, apoptosis and Kv1.5 gene expression of pulmonary artery smooth muscle cells induced by hypoxia]
    Chan Chen
    Cadres Ward, The First Affiliated Hospital of Wenzhou Medical College, Wenzhou, Zhejiang Province 325000, China
    Zhonghua Lao Dong Wei Sheng Zhi Ye Bing Za Zhi 29:731-4. 2011
    ..To study the effects of puerarin on proliferation, apoptosis and Kv1.5 gene expression of rat pulmonary artery smooth muscle cells (PASMCs) induced by hypoxia...
  86. doi Absence of Rgs5 prolongs cardiac repolarization and predisposes to ventricular tachyarrhythmia in mice
    Mu Qin
    Department of Cardiology, Renmin Hospital of Wuhan University, Wuhan 430060, China
    J Mol Cell Cardiol 53:880-90. 2012
    ..The results strongly indicate that Rgs5(-/-) induced prolonged repolarization and ventricular tachyarrhythmia, which were closely related to the remodeling of voltage-dependent K(+) currents...
  87. pmc Effects of SGLT2 inhibition in human kidney proximal tubular cells--renoprotection in diabetic nephropathy?
    Usha Panchapakesan
    Department of Medicine, The University of Sydney, Renal Research Group, Kolling Institute of Medical Research, Royal North Shore Hospital, St Leonards, New South Wales, Australia
    PLoS ONE 8:e54442. 2013
    ..We used an in vitro model of human PTCs. HK2 cells (human kidney PTC line) were exposed to control 5 mM, high glucose (HG) 30 mM or the profibrotic cytokine ..
  88. doi Calcium-activated potassium channel SK1 is widely expressed in the peripheral nervous system and sensory organs of adult zebrafish
    R Cabo
    Departamento de Morfologia y Biologia Celular, Grupo SINPOS, Universidad de Oviedo, Spain
    Neurosci Lett 555:62-7. 2013
    ..Here we focus on small-conductance calcium-activated potassium channel 1 (SK1) which plays an important role in all excitable cells acting as feedback regulators in after-..
  89. pmc Inhibitory role of the KEAP1-NRF2 pathway in TGFβ1-stimulated renal epithelial transition to fibroblastic cells: a modulatory effect on SMAD signaling
    In Geun Ryoo
    College of Pharmacy, The Catholic University of Korea, Bucheon, Gyeonggi Do, Republic of Korea
    PLoS ONE 9:e93265. 2014
    ..of the cellular antioxidant system, in TGFβ1-stimulated EMT gene changes using human renal tubular epithelial HK2. Treatment with TGFβ1 enhanced the levels of reactive oxygen species (ROS) and TGFβ1-stimulated EMT gene changes, ..
  90. pmc Implication of Bcl-2-associated athanogene 3 in fibroblast growth factor-2-mediated epithelial-mesenchymal transition in renal epithelial cells
    Feng Du
    Department of Nephrology, Shengjing Hospital, China Medical University, Shenyang 110004, China
    Exp Biol Med (Maywood) 240:566-75. 2015
    ..The current study found that FGF-2 induced EMT, simultaneously increased BAG3 expression in human kidney 2 (HK2) cells...
  91. pmc Genetic Disruption of Protein Kinase STK25 Ameliorates Metabolic Defects in a Diet-Induced Type 2 Diabetes Model
    Manoj Amrutkar
    Lundberg Laboratory for Diabetes Research, Department of Molecular and Clinical Medicine, University of Gothenburg, Gothenburg, Sweden
    Diabetes 64:2791-804. 2015
    ..controlling the muscle oxidative capacity (Cpt1, Acox1, Cs, Cycs, Ucp3) and glucose metabolism (Glut1, Glut4, Hk2) was increased...
  92. doi Quinolone-indolone conjugate induces apoptosis by inhibiting the EGFR-STAT3-HK2 pathway in human cancer cells
    Ying Hua Liu
    Biopharmaceutical Department, Institute of Traditional Chinese Medicine, College of Pharmacy, Henan University, Kaifeng, Henan 475004, P R China
    Mol Med Rep 12:2749-56. 2015
    ..of EGFR, and the downstream signal transducer and activator of transcription 3 (STAT3)-mediated hexokinase II (HK2) signaling pathways...
  93. pmc p63 supports aerobic respiration through hexokinase II
    Guiditta Viticchiè
    Department of Experimental Medicine and Surgery, University of Tor Vergata, 00133 Rome, Italy
    Proc Natl Acad Sci U S A 112:11577-82. 2015
    ..The glycolytic enzyme hexokinase 2 (HK2) represents the first step of glucose utilization in cells...
  94. doi The association of (18)F-FDG PET and glucose metabolism biomarkers GLUT1 and HK2 in p16 positive and negative head and neck squamous cell carcinomas
    Andrew M Baschnagel
    Department of Human Oncology, University of Wisconsin, Madison, USA
    Radiother Oncol 117:118-24. 2015
    To investigate the relationship between FDG-PET maximum standard uptake value (SUVmax), p16, EGFR, GLUT1 and HK2 expression in head and neck squamous cell carcinomas (HNSCC).
  95. doi Stabilization of Kv1.5 channel protein by the inotropic agent olprinone
    Ryo Endo
    Department of Anesthesiology, Tottori University Faculty of Medicine, 86 NIshi cho, Yonago 683 8503, Japan
    Eur J Pharmacol 765:488-94. 2015
    ..5 proteins at the ER through an action as a chemical chaperone, and thereby increases the density of Kv1.5 channels on the cell membrane. The enhancement of Kv1.5 currents could underlie less arrhythmogenicity of olprinone...
  96. doi Design and demonstration of a pumpless 14 compartment microphysiological system
    Paula G Miller
    Department of Biomedical Engineering, Cornell University, 113 Weill Hall, Ithaca, 14853, New York
    Biotechnol Bioeng 113:2213-27. 2016
    ..organs (barrier lines-A549 [lung] and Caco2 [GI]) (nonbarrier lines-HepG2 C3A [liver], Meg01 [bone marrow], and HK2 [kidney])...
  97. pmc Regulation of HK2 expression through alterations in CpG methylation of the HK2 promoter during progression of hepatocellular carcinoma
    Hyun Gyu Lee
    Department of Microbiology and Immunology, Institute for Immunology and Immunological Diseases, Yonsei University College of Medicine, Seoul, Republic of Korea
    Oncotarget 7:41798-41810. 2016
    Hexokinase 2 (HK2) is a rate-determining enzyme in aerobic glycolysis, a process upregulated in tumor cells...
  98. pmc Integrative genomics reveals hypoxia inducible genes that are associated with a poor prognosis in neuroblastoma patients
    Mark A Applebaum
    Departments of Pediatrics, University of Chicago, Chicago, Illinois, 60637, United States of America
    Oncotarget 7:76816-76826. 2016
    ..those from neuroblastoma patients and neuroblastoma derived cell lines, we identified nine genes (SLCO4A1, ENO1, HK2, PGK1, MTFP1, HILPDA, VKORC1, TPI1, and HIST1H1C) that are up-regulated in hypoxia and whose expression levels are ..
  99. ncbi Effect of lanthanum on voltage-dependent gating of a cloned mammalian neuronal potassium channel
    J Tytgat
    Laboratory of Toxicology, University of Leuven, Belgium
    Brain Res 749:232-7. 1997
    ..Our results provide evidence for a direct interaction with the potassium channel protein, shedding new light on the mechanism of action of this lanthanide...
  100. ncbi Physical mapping of potassium channel gene clusters on mouse chromosomes three and six
    V A Street
    Department of Otolaryngology Head and Neck Surgery, University of Washington School of Medicine, Seattle 98195, USA
    Genomics 44:110-7. 1997
    ..the physical spacing as 5'-Kcna3-(60 kb)-Kcna2-(90 kb)-Kcna8-3' on Chr 3, and as 5'-Kcna6-(80 kb)-Kcna1-(110 kb)-Kcna5-3' on Chr 6, with all genes oriented in a head-to-tail manner within their respective clusters...
  101. ncbi Expression of hexokinase 1 and hexokinase 2 in mammary tissue of nonlactating and lactating rats: evaluation by RT-PCR
    G L Kaselonis
    Department of Pediatrics, UCLA School of Medicine, Los Angeles, California, 90095, USA
    Mol Genet Metab 68:371-4. 1999
    ..HK), we tested the hypothesis that the expression of the isozymes, hexokinase type 1 (HK1) and hexokinase type 2 (HK2), would be different in rat mammary tissue during pregnancy and lactation...

Research Grants78

  1. SRINIVAS TIPPARAJU; Fiscal Year: 2015
    ..These findings could provide insights into the development of new therapeutic interventions for the treatment and management of myocardial ischemic injury. ..
  2. ACTIVATION OF PROSTATE SPECIFIC ANTIGEN PRECURSOR
    Thomas Takayama; Fiscal Year: 2000
    ..We therefore, propose to study the potential pathogenic mechanisms of PSA, hK2 (another prostate specific serine protease) and other serine proteases recently isolated from the prostate...
  3. Geoffrey W Abbott; Fiscal Year: 2015
    ....
  4. KALLIKREIN GENE EXPRESSION IN HUMAN PROSTATE CELLS
    Charles Young; Fiscal Year: 2002
    ..Prostate-specific antigen (PSA) and human glandular kallikrein (hK2) are the prostate-specific kallikreins, which are not only of clinical significance as prostate cancer markers, but ..
  5. Biacore T100 SPR system for studying and characterizing biomolecular interaction
    Ewa Folta Stogniew; Fiscal Year: 2009
    ....
  6. Stephen L Archer; Fiscal Year: 2015
    ..Since HOSK may have arisen independent of the canonical K+ channel family, exploring its structure-function relationship will extend our fundamental knowledge K+ channels. ..
  7. Victoria L Seewaldt; Fiscal Year: 2015
    ..PHS 398/2590 (Rev. 09/04, Reissued 4/2006) Page Continuation Format Page ..
  8. Andrew J Vickers; Fiscal Year: 2015
    ..we have shown that a statistical model based on measuring isoforms of PSA, and kallikrein-related peptidase 2 (hK2), is a highly accurate predictor of prostate biopsy outcome in men with elevated PSA...
  9. Modulation of Kir Channel Function by Phosphorylation
    Diomedes E Logothetis; Fiscal Year: 2012
    ..This project aims to identify amino acid residues of cardiac potassium channel proteins that are phosphorylated...
  10. Potassium channels in myotonic dystrophy type 1
    Christine Beeton; Fiscal Year: 2012
    ..Such new therapeutic targets would have tremendous benefits for public health. ..
  11. SERINE PROTEASES IN PROSTATE CANCER METASTASIS
    Peter Nelson; Fiscal Year: 2002
    ..Two of these, prostate specific antigen (PSA) and human glandular kallikrein 2 (hK2) exhibit an expression profile essentially restricted to the human prostate...
  12. K+ channel protein complexes in auditory biology
    WILLIAM KOBERTZ; Fiscal Year: 2009
    ..The results from these aims will provide a molecular and cellular framework, which will aid in the understanding of JLNS and other KCNQ1-KCNE-linked diseases. ..
  13. NOVEL MARKERS FOR PROSTATE CANCER
    Charles Young; Fiscal Year: 2005
    ..Highly specific and sensitive immunoassays for serum human kallikrein 2 (hK2) have been developed for prostate cancer detection...
  14. Small Molecule Kv1.3 Blockers as New Therapeutics for Multiple Sclerosis
    Heike Wulff; Fiscal Year: 2007
    ..Lay: In multiple sclerosis the immune system attacks proteins in the brain of afflicted patients. The aim of this study is to identify and test new drugs that can suppress the white blood cells that are invading the brain. ..
  15. MOLECULAR DETERMINANTS OF POTASSIUM CHANNEL DRUG BLOCK
    Dirk Snyders; Fiscal Year: 2003
    ....
  16. REGULATORY MECHANISMS OF CARDIAC REPOLARIZATION
    Michael Tamkun; Fiscal Year: 2005
    ..Given the role that both Kv channels and connexins play in cardiac and vascular smooth muscle, the proposed research will significantly advance our understanding of electrical excitability in the cardiovascular system. ..
  17. Targeting of Voltage-gated K+ Channels to Lipid Rafts
    Michael Tamkun; Fiscal Year: 2004
    ..1-containing lipid rafts from brain. This proposed research examines a new area in Kv channel research that will have important implications in multiple tissue systems. ..
  18. NEW APPLICATIONS OF THE PROSTATE CANCER MARKER PSA
    Paul Lange; Fiscal Year: 2002
    ..g. psm, hk2)...
  19. Cardiac KCNE2 (MIRP1) Regulation by Estrogen and Cardiac Stress
    Mansoureh Eghbali; Fiscal Year: 2012
    ..The goal of this project is to gain insight in how estrogen may induce cardioprotection by regulating the activity of a gene that is exquisitely modulated by estrogen and that modifies cardiac excitability. ..
  20. Trafficking and Regulation of Cardiovascular K+ Channels
    JEFFREY MARTENS; Fiscal Year: 2013
    ....
  21. ERR-gamma-dependent mammary tumorigenesis in response to BPA and a high-fat diet
    Rebecca B Riggins; Fiscal Year: 2010
    ..of early INS resistance, and hepatic expression of ERR? and two of its putative target genes (hexokinase 2, HK2;pyruvate dehydrogenase kinase 4, PDK4) are increased by BPA exposure in these animals...
  22. Brian F Clem; Fiscal Year: 2016
    ..shift was mediated by changes in the expression of multiple glycolytic enzymes including increased Glut-1, HK2, PK-M2 levels and decreased HK1, ALT1, and PCB...
  23. William M Chilian; Fiscal Year: 2016
    ..This integrated approach-from electrophysiology to in vivo flow regulation should enable answers regarding basic coronary physiology and flow regulation, as well as potential therapies for diabetic cardiomyopathy. ..
  24. XIAOFENG FRANK YANG; Fiscal Year: 2016
    ..ii) To determine the role of Hk2 in Rrp2 activation during tick transmission and mammalian infection...
  25. Nissim Hay; Fiscal Year: 2016
    DESCRIPTION (provided by applicant): We found that in human prostate carcinoma and in lung carcinoma hexokinase 2 (HK2) expression is markedly elevated, while in normal prostate and lung cells its expression is hardly detectable...
  26. Russell O Pieper; Fiscal Year: 2016
    ..the HK1 and PKM1 isoforms and preferentially use glucose for ATP generation while gliomas, in contrast, express HK2 and PKM2 and use glucose to synthesize macromolecules needed for proliferation...
  27. Regulation of Kv Channels by Anorexigens
    Bruce Pitt; Fiscal Year: 2007
    ..1 proteins, inhibition of Kv1.5 gene transcription and blockade of Kv currents at plasma membrane. ..
  28. A Novel High Throughput Assay for Ion Channel Modulators
    Barbara Wible; Fiscal Year: 2006
    ..The cardiac potassium channel hERG is the most common target of undesired drug interactions; block of hERG can predispose individuals ..
  29. REGULATION OF CARDIAC POTASSIUM CHANNEL GENE EXPRESSION
    Koichi Takimoto; Fiscal Year: 2002
    ..x gene expression independently of hypertrophy. Hence, this proposal is to test these possibilities using hypertension animal models and neonatal myocyte cultures. ..
  30. A Novel High Throughput Assay for Ion Channel Modulators
    Barbara Wible; Fiscal Year: 2004
    ..The cardiac potassium channel hERG is an example of frequent unwanted drug interactions; block of hERG can predispose individuals to ..
  31. MODULATION OF K+ CHANNEL FUNCTION BY PERMEANTIONS
    Stephen Korn; Fiscal Year: 2004
    ..Furthermore, these experiments will lead to a better understanding of how intracellular channel blockers interact with external pH and K+ to produce physiological and pathological consequences in both brain and heart. ..
  32. ITO IN DOGS WITH INHERITED VENTRICULAR ARRHYTHMIAS
    Bruce Kornreich; Fiscal Year: 2005
    ..abstract_text> ..
  33. A High Throughput Assay for Cancer Drug Cardiotoxicity
    Barbara Wible; Fiscal Year: 2005
    ..The cardiac potassium channel hERG is a frequent target of unwanted drug interactions, often leading to acquired long QT syndrome in ..
  34. Postmortem PSA: role in epidemiology of prostate cancer
    Gabriel Haas; Fiscal Year: 2002
    ..a study to evaluate the ability of PSA and its related forms such as free PSA (fPSA), complexed PSA (cPSA), hK2, etc. to detect microscopic, occult malignancies...
  35. CARDIAC POTASSIUM CHANNEL SUBUNITS AND SUDDEN DEATH
    Martin Tristani Firouzi; Fiscal Year: 2002
    ..Environment: The University of Utah is a preeminent research institution in the field of cardiac ion channel research and the molecular genetics of LQT. ..
  36. SNPs in Idopathic Pulmonary Artierial Hypertension
    JASON YUAN; Fiscal Year: 2006
    ..proposed to test the hypothesis that a) specific single nucleotide polymorphysisms (SNPs) in other genes, such as KCNA5 (K+ channel), ANGPT1 (angiopoietin-1), TRPC6 (Ca2+ channel), HTR2B (5-HT receptor) and SLC6A4 (5-HT transporter), ..
  37. Detection of occult prostate cancers in elderly men
    Gabriel Haas; Fiscal Year: 2004
    ..In Aim 2, we will determine the serum levels of tumor markers (total, free and complexed PSA, hK2, and the ratios of free/total PSA and complexed/free PSA) which correspond to the occult tumors detected in the ..
  38. Molecular Recognition of Potassium Channels
    Dirk Trauner; Fiscal Year: 2006
    ..x channels is proposed. Pharmacologically relevant Kv1.x channels such as Kv1.3 or Kv1.5 will receive special attention. The ability of the synthetic ligands to bind to different functional states of a given channel will be evaluated. ..
  39. VOLTAGE DEPENDENT K+ CHANNELS IN HEAT--KV15 ALPHA SUBUNI
    Joseph Hill; Fiscal Year: 2003
    ..5. The methods to be used are biochemical and immunological (Western blots, immunoprecipitation) and electrophysiological (patch clamping, ambulatory electrocardiography). ..
  40. MODULATION OF VOLTAGE DEPENDENT POTASSIUM CHANNELS
    IRWIN LEVITAN; Fiscal Year: 2000
    ....
  41. A Parallel High-Throughput Pharmacogenetic Profiling Assay for Clinical Use
    Gao Chen; Fiscal Year: 2009
    ..fluorescence detector to decode and detect fluorescence one by one;(3) developed multiplex PCR for P450 (CYP2A7), KCNA5 and ITPase, and bead hybridization;and (4) evaluated the SNP genotyping assay using multiplex PCR amplified ..
  42. HYPERTENSION: CONTRIBUTION OF ARTERIAL WALL CHANGES
    Robert Cox; Fiscal Year: 2007
    ..These studies will define a novel therapeutic target for antihypertensive drug development based upon the mechanism(s) of Ca2+-Kv channel modulation. ..
  43. Methodology of Phase I and II trials of anticancer CAM
    Andrew Vickers; Fiscal Year: 2004
    ....
  44. A New Biomarker for Ovarian Cancer Detection
    Eleftherios Diamandis; Fiscal Year: 2003
    ..In this grant proposal, we describe further studies, which will examine in greater detail, the ability of a test for the amount of this protein in blood to correctly diagnose the presence of ovarian cancer. ..
  45. KALLIKREINS AS DIAGNOSTIC MARKERS OF OVARIAN CARCINOMA
    Eleftherios Diamandis; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  46. Human Kallikrein 4 (hK4): A New Prostatic Biomarker?
    Eleftherios Diamandis; Fiscal Year: 2003
    ..If successful, our research will contribute to the development of new prostatic biomarkers and possibly, to better diagnosis which may lead to better clinical outcomes and reduced healthcare costs. ..
  47. Long-term prediction of prostate cancer death from kallikreins measured in blood
    Hans Lilja; Fiscal Year: 2008
    ..by applicant): We will determine whether kallikrein forms (prostate-specific antigen [PSA] and kallikrein 2 [hK2]) measured in men aged 44 - 50 predict subsequent metastases or death from prostate cancer...
  48. Role of Molecular Chaperones in hERG Processing
    Eckhard Ficker; Fiscal Year: 2008
    ..abstract_text> ..
  49. CARDIAC GROWTH REGULATION
    Kaie Ojamaa; Fiscal Year: 2002
    ..End of Abstract) ..
  50. Thyroid Hormone Receptor Function in Cardiac Hypertrophy
    Kaie Ojamaa; Fiscal Year: 2006
    ..abstract_text> ..
  51. Genetic Aspects of Vestibular Dysfunction
    Stephen Roth; Fiscal Year: 2004
    ..The proposed project will generate important pilot data related to the genetics of vestibular dysfunction, thus fitting within the R21 grant mechanism. ..
  52. Breast Cancer Prediction Using Nipple Aspirate Fluid
    Edward Sauter; Fiscal Year: 2007
    ..unreadable] [unreadable]..
  53. MOLECULAR AND CHEMICAL DESCRIPTION OF CFTR FUNCTION
    Peter Pedersen; Fiscal Year: 2003
    ..The proposed studies are fundamental to understanding structure/function relationships within CFTR, to understanding the underlying basis of most cases of CF, and to developing new strategies to treat the disease. ..
  54. Pathogenesis of HIVAN: the role of Nef
    JOHN HE; Fiscal Year: 2007
    ..These studies should elucidate essential mechanism responsible for the development of HIV-associated nephropathy and how Nef plays a role in this pathologic process. ..
  55. Genetic Epidemiology of Aging Skeletal Muscle
    Stephen Roth; Fiscal Year: 2007
    ..abstract_text> ..
  56. FORMS OF PROSTATE SPECIFIC ANTIGEN AND HK2 IN CANCER
    MARY HEEB; Fiscal Year: 2003
    We seek to extend promising studies showing that prostate specific antigen (PSA) and glandular kallikrein (hK2) occur in several forms in blood of prostate cancer (CaP) patients and that measurement of the proportion of PSA in the form ..
  57. THROMBOGENIC FACTORS AND RECURRENT CORONARY EVENTS
    Arthur Moss; Fiscal Year: 2003
    ..abstract_text> ..
  58. Defective trafficking Mechanisms in a Cardiac K+ Channel
    Sabina Kupershmidt; Fiscal Year: 2006
    ..Three of the five genetic loci known to cause the inherited form of the disease code for cardiac potassium channel subunits...
  59. Novel Anticoagulant Mechanisms
    MARY HEEB; Fiscal Year: 2006
    ..We will find whether a ZPI polymorphism we identified affects function. ..
  60. THERAPUTIC TRIAL IN PATIENTS WITH LQTS 3 GENE MUTATION
    Arthur Moss; Fiscal Year: 2002
    ..The significance of this work relates to the future use of molecular therapeutics to treat ion-channel disorders associated with congenital and acquired cardiac repolarization disorders. ..
  61. Genetic Architecture of Aging Skeletal Muscle
    Stephen Roth; Fiscal Year: 2005
    ..abstract_text> ..
  62. Cancer-Related Glycolytic Gene:Regulation and Targeting
    Peter Pedersen; Fiscal Year: 2008
    ..abstract_text> ..
  63. Protein Profiling in Nipple Aspirate Fluid
    Edward Sauter; Fiscal Year: 2007
    ..abstract_text> ..
  64. The Effect of Black Cohosh Extract on the Human Breast
    Edward Sauter; Fiscal Year: 2004
    ..The findings should allow us to design a high quality R01 submission involving a larger, randomized study of longer duration which should provide some answers on the potential role of BCE in breast cancer. ..
  65. Altered Breast Methylation after Low/Hi Dose Isoflavones
    Edward Sauter; Fiscal Year: 2005
    ..abstract_text> ..
  66. New drugs for treatment of atrial fibrillation
    Antonio Lacerda; Fiscal Year: 2004
    ..ChanTest believes that this drug will offer great relief to the many people who are debilitated by atrial fibrillation. ..
  67. Cytoskeletal Basis of Ventricular Arrhythmias
    Matteo Vatta; Fiscal Year: 2005
    ..Identifying cytoskeletal mecahnisms involved in malignant arrhythmias, could lead to the design of novel drugs and the employment of therapeutic means, resulting in a better patients management. ..
  68. ION CHANNELS IN DEMYELINATING DISEASES
    Betty Soliven; Fiscal Year: 2003
    ..In addition, there may be ways to promote remyelination using the K+ channels of OP cells/OLGs as drug targets. ..
  69. Fibroblast Activation Protein-alpha Activated Anti-Stromal Prodrug Therpay for Ca
    Samuel R Denmeade; Fiscal Year: 2010
    ..e. "stroma") within cancers rather than the cancer cells themselves can be effective therapy. The FAP- activated prodrug, therefore, could represent a new targeted therapy for a variety of human cancers. ..
  70. DEVELOPMENT OF VESTIBULAR NUCLEI NEURONS
    KENNA PEUSNER; Fiscal Year: 2005
    ..abstract_text> ..
  71. CONTROL OF ENZYMATIC PHOSPHATE TRANSFER IN MITOCHONDRIA
    Peter Pedersen; Fiscal Year: 2009
    ..These studies also have direct relevance to using nanotechnology in medicine as the ATP synthasome is comprised of 2 reversible nanomotors. ..
  72. Identification of compounds that protect HERG from block by proarrhythmic agents
    Sabina Kupershmidt; Fiscal Year: 2008
    ..The most common cause of this unpredictable effect is the unintended block of a cardiac potassium channel, called HERG that is essential for maintaining the balanced electrical activity and rhythmic contraction ..
  73. LONG QT SYNDROME--GENETIC STUDIES
    Arthur Moss; Fiscal Year: 2002
    ....
  74. Novel therapeutic targets in inflammatory neuropathies
    Betty Soliven; Fiscal Year: 2006
    ..abstract_text> ..
  75. Mutant ZASP in Cytoskeletal Remodeling and Arrhythmia
    Matteo Vatta; Fiscal Year: 2006
    ..In addition, little is known about the role of Cypher/ZASP mutations in skeletal muscle, and we have suggested that Cypher/ZASP could be a candidate for orphan forms of muscular dystrophies. ..