Genomes and Genes
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
Publications406 found, 100 shown here
- Expression of voltage-gated potassium channels Kv1.3 and Kv1.5 in human gliomasKatja 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...
- Structural determinants of Kvbeta1.3-induced channel inactivation: a hairpin modulated by PIP2Niels 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...
- A mechanism for combinatorial regulation of electrical activity: Potassium channel subunits capable of functioning as Src homology 3-dependent adaptorsM 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...
- Voltage-dependent potassium channels Kv1.3 and Kv1.5 in human cancerJ 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...
- Protein kinase C (PKC) activity regulates functional effects of Kvβ1.3 subunit on KV1.5 channels: identification of a cardiac Kv1.5 channelosomeMiren 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...
- Molecular basis of transient outward potassium current downregulation in human heart failure: a decrease in Kv4.3 mRNA correlates with a reduction in current densityS 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...
- Potassium channels Kv1.3 and Kv1.5 are expressed on blood-derived dendritic cells in the central nervous systemKatherine 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...
- Amino-terminal determinants of U-type inactivation of voltage-gated K+ channelsHarley 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...
- Coupling of voltage sensing to channel opening reflects intrasubunit interactions in kv channelsAlain 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...
- Function of Kv1.5 channels and genetic variations of KCNA5 in patients with idiopathic pulmonary arterial hypertensionCarmelle 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 ..
- Mitochondrial metabolism, redox signaling, and fusion: a mitochondria-ROS-HIF-1alpha-Kv1.5 O2-sensing pathway at the intersection of pulmonary hypertension and cancerStephen 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...
- Kv1.5 association modifies Kv1.3 traffic and membrane localizationRubén 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...
- The anchoring protein SAP97 retains Kv1.5 channels in the plasma membrane of cardiac myocytesJoëlle 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...
- Four and a half LIM protein 1: a partner for KCNA5 in human atriumZhenjiang 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)...
- Novel KCNA5 loss-of-function mutations responsible for atrial fibrillationYiqing 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...
- Tetramerization domain mutations in KCNA5 affect channel kinetics and cause abnormal trafficking patternsElyssa 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...
- Association of a KCNA5 gene polymorphism with systemic sclerosis-associated pulmonary arterial hypertension in the European Caucasian populationJ 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)...
- Novel KCNA5 mutation implicates tyrosine kinase signaling in human atrial fibrillationTao Yang
Department of Medicine, Vanderbilt University School of Medicine, Nashville, Tennessee 37323 6602, USA
Heart Rhythm 7:1246-52. 2010Emerging 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.
- Genetic variation in KCNA5: impact on the atrial-specific potassium current IKur in patients with lone atrial fibrillationIngrid 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. 2013Genetic 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...
- Molecular cloning and characterization of two voltage-gated K+ channel cDNAs from human ventricleM 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...
- Gating of shaker-type channels requires the flexibility of S6 caused by prolinesAlain 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...
- Molecular basis for Kv1.5 channel block: conservation of drug binding sites among voltage-gated K+ channelsNiels 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...
- Overexpression of human KCNA5 increases IK V and enhances apoptosisElena 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...
- Antiarrhythmic drug-induced internalization of the atrial-specific k+ channel kv1.5Sarah M Schumacher
Department of Pharmacology, 1301 MSRBIII, 1150 W Medical Center Dr, Ann Arbor, MI 48109 0632, USA
Circ Res 104:1390-8. 2009....
- Stereoselective block of a human cardiac potassium channel (Kv1.5) by bupivacaine enantiomersC 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)...
- High affinity of ergopeptides for cytochromes P450 3A. Importance of their peptide moiety for P450 recognition and hydroxylation of bromocriptineM 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...
- Effect of noble gases on oxygen and glucose deprived injury in human tubular kidney cellsMaleeha 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...
- Mechanism of block of a human cardiac potassium channel by terfenadine racemate and enantiomersT 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...
- Measurement of prostate-specific antigen and human glandular kallikrein 2 in different body fluidsJ 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 ..
- Expression of voltage-gated K+ channels in human atriumFederica 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...
- The effects of quinidine and its chiral isolates on erg-1sm potassium current and correlation with gastrointestinal augmentationIvana 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-..
- Expression of prostate-specific antigen (PSA) and human glandular kallikrein 2 (hK2) in ileum and other extraprostatic tissuesA 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)...
- Atrial-selective antiarrhythmic actions of novel Ikur vs. Ikr, Iks, and IKAch class Ic drugs and beta blockers in pigsKarsten Knobloch
DG Cardiovascular Diseases, Aventis Pharma, Frankfurt am Main, Germany
Med Sci Monit 10:BR221-8. 2004....
- Slow gating charge immobilization in the human potassium channel Kv1.5 and its prevention by 4-aminopyridineD 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...
- Properties of a time-dependent potassium current in pig atrium: evidence for a role of kv1.5 in repolarizationJoachim 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...
- Human axons contain at least five types of voltage-dependent potassium channelG 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...
- High-throughput analysis of drug binding interactions for the human cardiac channel, Kv1.5Jerzy Karczewski
Department of Pain Research, Merck Research Laboratories, West Point, PA 19486, USA
Biochem Pharmacol 77:177-85. 2009....
- Shared requirement for dynein function and intact microtubule cytoskeleton for normal surface expression of cardiac potassium channelsMatthew 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...
- 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 hormoT Aoyama
Laboratory of Molecular Carcinogenesis, National Cancer Institute, Bethesda, Maryland 20892
J Biol Chem 264:10388-95. 1989Immunoblotting 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...
- 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 therapyD C Yu
Calydon, Inc, Sunnyvale, California 94089, USA
Cancer Res 59:1498-504. 1999Human glandular kallikrein (hK2) and prostate-specific antigen (PSA) are related members of the human kallikrein gene family...
- 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-analoguesT 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.
- Kv1.5 is a major component underlying the A-type potassium current in retinal arteriolar smooth muscleMary 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...
- Serpin-derived peptide substrates for investigating the substrate specificity of human tissue kallikreins hK1 and hK2L Bourgeois
Laboratory of Enzymology and Protein Chemistry, CNRS EP 117, University Francois Rabelais, 37032 Tours, France
J Biol Chem 272:29590-5. 1997The third human tissue kallikrein to be identified, hK2, could be an alternate or complementary marker to kallikrein hK3 (prostate-specific antigen) for prostate diseases...
- alpha2-macroglobulin and C1-inactivator are plasma inhibitors of human glandular kallikreinM 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. 1998Human glandular kallikrein (hK2) is a possible new marker for prostate cancer that is homologous to prostate specific antigen...
- Enzymatic action of human glandular kallikrein 2 (hK2). Substrate specificity and regulation by Zn2+ and extracellular protease inhibitorsJ Lovgren
Department of Laboratory Medicine, Lund University, Malmo, Sweden
Eur J Biochem 262:781-9. 1999Human glandular kallikrein 2 (hK2) is a serine protease expressed by the prostate gland with 80% identity in primary structure to prostate-specific antigen (PSA)...
- Structural investigation of the alpha-1-antichymotrypsin: prostate-specific antigen complex by comparative model buildingB 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...
- Dichloroacetate shifts the metabolism from glycolysis to glucose oxidation and exhibits synergistic growth inhibition with cisplatin in HeLa cellsJing 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....
- KVLQT1 C-terminal missense mutation causes a forme fruste long-QT syndromeC Donger
INSERM U153, Groupe Hospitalier Pitie Salpetriere, Institut de Myologie, Paris, France
Circulation 96:2778-81. 1997KVLQT1, 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)...
- 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 cellsT 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 ..
- Cardiac glycosides as novel inhibitors of human ether-a-go-go-related gene channel traffickingLu Wang
Rammelkamp Center for Education and Research, Case Western Reserve University, Cleveland, OH 44109, USA
J Pharmacol Exp Ther 320:525-34. 2007Direct 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...
- Stabilizing effects of eicosapentaenoic acid on Kv1.5 channel protein expressed in mammalian cellsShunya 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...
- Human tissue kallikrein 5 is a member of a proteolytic cascade pathway involved in seminal clot liquefaction and potentially in prostate cancer progressionIacovos 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...
- Mutant recombinant serpins as highly specific inhibitors of human kallikrein 14Loyse 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 (..
- SUMO modification regulates inactivation of the voltage-gated potassium channel Kv1.5Mark 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...
- 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 prolongationB 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...
- Identification, synthesis, and activity of novel blockers of the voltage-gated potassium channel Kv1.5Stefan 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...
- Voltage clamp fluorimetry reveals a novel outer pore instability in a mammalian voltage-gated potassium channelMoninder Vaid
Department of Anesthesiology, Pharmacology, and Therapeutics, University of British Columbia, Vancouver, BC V6T 1Z3, Canada
J Gen Physiol 132:209-22. 2008....
- Modulation of the voltage-gated potassium channel Kv1.5 by the SGK1 protein kinase involves inhibition of channel ubiquitinationChristoph 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...
- Aging and muscle fiber type alter K+ channel contributions to the myogenic response in skeletal muscle arteriolesLori S Kang
Department of Physiology and Pharmacology, West Virginia University School of Medicine, Morgantown, WV, USA
J Appl Physiol (1985) 107:389-98. 2009....
- Effects of lobeline, a nicotinic receptor ligand, on the cloned Kv1.5Imju 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...
- Sinus node function and ventricular repolarization during exercise stress test in long QT syndrome patients with KvLQT1 and HERG potassium channel defectsH 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...
- 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 serumThomas 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...
- Human Kallikrein 2 (hK2) and prostate-specific antigen (PSA): two closely related, but distinct, kallikreins in the prostateH G Rittenhouse
Research and Development Department, Hybritech Incorporated, Beckman Coulter, Inc, San Diego, California, USA
Crit Rev Clin Lab Sci 35:275-368. 1998Recent studies on human kallikrein 2 (hK2) have revealed striking similarities and significant differences with the closely related kallikrein PSA...
- Highly sensitive automated chemiluminometric assay for measuring free human glandular kallikrein-2G 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. 1999Human 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...
- Angiotensin IV stimulates plasminogen activator inhibitor-1 expression in proximal tubular epithelial cellsL 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)...
- 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 sequencesJ 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)...
- Insulin-like growth factor binding proteins (IGFBPs) as potential physiological substrates for human kallikreins hK2 and hK3S 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 ..
- Development of a dual monoclonal antibody immunoassay for total human kallikrein 2J A Finlay
Research Department, Hybritech Inc, a subsidiary of Beckman Coulter, Inc, San Diego, CA 92121, USA
Clin Chem 47:1218-24. 2001Human kallikrein 2 (hK2) shares 80% sequence identity with prostate-specific antigen (PSA)...
- Characterization of androgen receptor and nuclear receptor co-regulator expression in human breast cancer cell lines exhibiting differential regulation of kallikreins 2 and 3Angeliki 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 ..
- 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 patientsRalf Kurek
Department of Anatomy and Cell Biology, Philipps University, Marburg, Germany
Clin Cancer Res 10:5808-14. 2004....
- Effect of lanthanum on voltage-dependent gating of a cloned mammalian neuronal potassium channelJ 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...
- Physical mapping of potassium channel gene clusters on mouse chromosomes three and sixV 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...
- Expression of hexokinase 1 and hexokinase 2 in mammary tissue of nonlactating and lactating rats: evaluation by RT-PCRG 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...
- Unusual alternative splicing within the human kallikrein genes KLK2 and KLK3 gives rise to novel prostate-specific proteinsAnat David
Compugen Ltd, 72 Pinchas Rosen St, Tel Aviv 69512, Israel
J Biol Chem 277:18084-90. 2002..The novel proteins encoded by these transcripts, named PSA-linked molecule (PSA-LM) and hK2-linked molecule (K-LM), share only the signal peptide with the original protein product of the respective gene...
- The sigma receptor as a ligand-regulated auxiliary potassium channel subunitEbru Aydar
Department of Physiology, School of Medicine, University of Wisconsin Madison, 1300 University Avenue, Madison, WI 53706, USA
Neuron 34:399-410. 2002..The ligand-independent effects on channels suggest that sigma receptors serve as auxiliary subunits to voltage-gated K+ channels with distinct functional interactions, depending on the presence or absence of ligand...
- Quantitative analysis of human kallikrein gene 14 expression in breast tumours indicates association with poor prognosisG M Yousef
Department of Pathology and Laboratory Medicine, Mount Sinai Hospital, Toronto, Ontario, Canada
Br J Cancer 87:1287-93. 2002..This family harbours several genes aberrantly expressed in various cancers as well as established (PSA/hK3, hK2) and potential (hK6, hK10) cancer markers...
- Developmental change in expression and subcellular localization of two shaker-related potassium channel proteins (Kv1.1 and Kv1.2) in the chick tangential vestibular nucleusAnastas Popratiloff
Department of Anatomy and Cell Biology, George Washington University Medical Center, Washington, DC 20037, USA
J Comp Neurol 461:466-82. 2003..Accordingly, both of these protein subunits could be involved in regulating excitability of the principal cells...
- Rapid elimination by glomerular filtration of free prostate specific antigen and human kallikrein 2 after renal transplantationLaila Bruun
Department of Nephrology and Transplantation, Lund University, University Hospital, Malmo, Sweden
J Urol 171:1432-5. 2004..have been sparse data reported on the rates and pathways of elimination of PSA complexes and human kallikrein 2 (hK2)...
- Effect of mitochondrial KATP channel on voltage-gated K+ channel in 24 hour-hypoxic human pulmonary artery smooth muscle cellsTao Wang
Department of Respiratory Medicine, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China
Chin Med J (Engl) 118:12-9. 2005..This study investigated the changes of cell membrane potential and Kv channel in cultured human pulmonary artery smooth muscle cell (hPASMC) exposed to 24 hour-hypoxia, and explored the role of MitoKATP and DeltaPsim in this condition...
- The effects of putative K+ channel blockers on volume regulation of murine spermatozoaJ P Barfield
Institute of Reproductive Medicine of the University, D 48129 Munster, Germany
Biol Reprod 72:1275-81. 2005..4 (also known as KCNA1), Kv1.5 (KCNA5), Kv4.1 (KCND1), Kv4.2 (KCND2), Kv4.3 (KCND3), mink (KCNE1), and acid-sensitive TASK2 (KCNK5) and TASK3 (KCNK9)...
- Inhibition of the cloned delayed rectifier K+ channels, Kv1.5 and Kv3.1, by riluzoleH S Ahn
Department of Physiology, Medical Research Center, College of Medicine, The Catholic University of Korea, 505 Banpo Dong, Socho gu, Seoul 137 701, Korea
Neuroscience 133:1007-19. 2005..Thus, riluzole inhibits both Kv1.5 and Kv3.1 currents in a concentration-dependent manner and interacts directly with Kv1.5 by preferentially binding to the inactivated and to the closed states of the channel...
- Association of Kv1.5 and Kv1.3 contributes to the major voltage-dependent K+ channel in macrophagesRubén Vicente
Molecular Physiology Laboratory, Departament de Bioquiámica i Biologia Molecular, Departament de Fisiologia, and Unitat de Reconeixement Molecular in situ, Serveis Cientificotècnics Universitat de Barcelona, E 08028 Barcelona, Spain
J Biol Chem 281:37675-85. 2006..Changes in the oligomeric composition of functional Kv channels would give rise to different biophysical and pharmacological properties, which could determine specific cellular responses...
- Benzopyran sulfonamides as KV1.5 potassium channel blockersJohn Lloyd
Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543 5400, USA
Bioorg Med Chem Lett 17:3271-5. 2007..K(V)1.5 blockers have the potential to be atrium-selective agents for treatment of atrial fibrillation. The benzopyrans provide a template for the synthesis of potent and selective K(V)1.5 blockers...
- Testosterone deprivation by castration impairs expression of voltage-dependent potassium channels in rat aortaPing Zhou
Geriatric Department, Second Affiliated Hospital, Harbin Medical University, Harbin, China
Eur J Pharmacol 593:87-91. 2008..Restoration of physiological concentrations of testosterone restored the impaired function of voltage-dependent potassium channels, which may provide evidence for the beneficial effects of clinical testosterone replacement...
- Can inhibition of IKur promote atrial fibrillation?Alexander Burashnikov
Masonic Medical Research Laboratory, Utica, New York 13501, USA
Heart Rhythm 5:1304-9. 2008..However, it has been shown that I(Kur) block may abbreviate atrial repolarization and that loss-of-function mutations in KCNA5, which encodes K(v) 1.5 channels responsible for I(Kur), is associated with familial AF.
- Kv1.5 open channel block by the antiarrhythmic drug disopyramide: molecular determinants of blockIván A Aréchiga
Unidad de Investigacion Carlos Mendez, Centro de Investigaciones Biomedicas de la Universidad de Colima, Colima, Mexico
J Pharmacol Sci 108:49-55. 2008..The single interaction between disopyramide and Val512 in the PVP region is able to change the mechanism of channel closure, reproducing the "foot-in-the-door" phenomenon...
- Kv1.1 and Kv1.3 channels contribute to the degeneration of retinal ganglion cells after optic nerve transection in vivoP D Koeberle
Division of Anatomy, Department of Surgery, University of Toronto, Ontario, Canada
Cell Death Differ 17:134-44. 2010..Kv1.1 depletion increased the antiapoptotic gene, Bcl-X(L), whereas Kv1.3 depletion reduced the proapoptotic genes, caspase-3, caspase-9 and Bad...
- Biochemical characterization of kappaM-RIIIJ, a Kv1.2 channel blocker: evaluation of cardioprotective effects of kappaM-conotoxinsPing Chen
Department of Biology, University of Utah, Salt Lake City, Utah 84112, USA
J Biol Chem 285:14882-9. 2010..2 alpha-subunit rather than antagonism to Kv1.2 homotetramers. Furthermore, kappaM-RIIIK and kappaM-RIIIJ provide a valuable set of probes for understanding the underlying mechanism of cardioprotection...
- Discovery of triarylethanolamine inhibitors of the Kv1.5 potassium channelDouglas C Beshore
Department of Medicinal Chemistry, Merck Research Laboratories, Merck and Co, Inc, West Point, PA 19486, USA
Bioorg Med Chem Lett 20:2493-6. 2010..The structure-activity relationship (SAR) studies described herein led to the development of potent, selective and orally active inhibitors of Kv1.5...
- MicroRNA-143 (miR-143) regulates cancer glycolysis via targeting hexokinase 2 geneRong Fang
State Key Laboratory of Cell Biology, Institute of Biochemistry and Cell Biology, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 200031, China
J Biol Chem 287:23227-35. 2012..Hexokinase 2 (HK2), coding for the first rate-limiting enzyme of glycolysis, is among the top list of genes predicted and potentially ..
- Regulation of ion channels by the serum- and glucocorticoid-inducible kinase SGK1Florian Lang
Department of Physiology, University of Tuebingen, Gmelinstrasse 5, 72076 Tuebingen, Germany
FASEB J 27:3-12. 2013..Therefore, SGK1 may be considered an attractive therapeutic target despite its broad range of functions...
- Tubular cell HIV-entry through apoptosed CD4 T cells: a novel pathwayPriyanka Singh
Center for Excellence for Immunology and Inflammation, Feinstein Institute for Medical Research, Hofstra North Shore Long Island Jewish Medical School, New Hyde Park, NY, USA
Virology 434:68-77. 2012..of programmed death-1 (PD-1) receptors on CD4 T cells and programmed death ligand-1 (PD-L1) on tubular cells (HK2 and HRPTEC, primary tubular cells)...
- Incretin-stimulated interaction between β-cell Kv1.5 and Kvβ2 channel proteins involves acetylation/deacetylation by CBP/SirT1Su Jin Kim
Department of Cellular and Physiological Sciences, Life Sciences Institute, University of British Columbia, 2350 Health Sciences Mall, Vancouver, BC, V6T 1Z3, Canada
Biochem J 451:227-34. 2013..5 in response to GIP or GLP-1. Incretin regulation of β-cell function therefore involves the acetylation of multiple Kvα and Kvβ subunits...
- High glucose induces CCL20 in proximal tubular cells via activation of the KCa3.1 channelChunling Huang
Kolling Institute of Medical Research, Royal North Shore Hospital, Sydney Medical School, University of Sydney, Sydney, NSW, Australia Xiamen Center of Clinical Laboratory, Xiamen Zhongshan Hospital, Medical College of Xiamen University, Xiamen, China
PLoS ONE 9:e95173. 2014..1 ameliorates renal fibrotic responses in DN through inhibition of the TGF-β1 pathway. The present study aimed to identify the role of KCa3.1 in the inflammatory responses inherent in DN...
- Reduced sialylation impacts ventricular repolarization by modulating specific K+ channel isoforms distinctlyAndrew R Ednie
From the Department of Molecular Pharmacology and Physiology, Morsani College of Medicine, University of South Florida, Tampa, Florida 33612
J Biol Chem 290:2769-83. 2015..These studies elucidate a novel role for individual glycogene products in contributing to a complex network of cardiac regulation under normal and pathologic conditions. ..
- Trp(250) -hK2 is defective in intracellular trafficking and activates the unfolded protein responseEun Ju Choi
College of Pharmacy, Yonsei Institute of Pharmaceutical Sciences, Yonsei University, 162 1 Songdo dong, Yeonsu gu, Incheon, 406 840, Korea
Genes Cells 20:512-20. 2015b>hK2, a member of the kallikrein protease family encoded by KLK2, is expressed exclusively in prostate and is a putative adjunct tumor marker for prostate cancer screening...
- Core Pluripotency Factors Directly Regulate Metabolism in Embryonic Stem Cell to Maintain PluripotencyHyunsoo Kim
Department of Biomedical Sciences, National Creative Research Center for Epigenome Reprogramming Network, Ischemic Hypoxic Disease Institute
Stem Cells 33:2699-711. 2015..Specifically, Oct4 directly governs Hk2 and Pkm2, which are important glycolytic enzymes that determine the rate of glycolytic flux...
- Effects and mechanism of miR-23b on glucose-mediated epithelial-to-mesenchymal transition in diabetic nephropathyHaifeng Liu
Department of Biotechnology, College of Life Science and Technology, Jinan University, Guangzhou, Guangdong 510632, PR China Heilongjiang Province Key Laboratory for Anti Fibrosis Biotherapy, Mudanjiang Medical University, Mudanjiang, Heilongjiang 157011, PR China
Int J Biochem Cell Biol 70:149-60. 2016..miR-23b) was significantly decreased in high glucose (HG)-induced human kidney proximal tubular epithelial cells (HK2) and in kidney tissues of db/db mice...
- Metabolic phenotype of bladder cancerFrancesco Massari
Division of Oncology, S Orsola Malpighi Hospital, Bologna, Italy Electronic address
Cancer Treat Rev 45:46-57. 2016..genes (SRC-3, glucose transporter type 1 [GLUT1], GLUT3, lactic dehydrogenase A [LDHA], LDHB, hexokinase 1 [HK1], HK2, pyruvate kinase type M [PKM], and hypoxia-inducible factor 1-alpha [HIF-1α]), resulting in an overproduction of ..
- [The role of hexokinase 2 in the metastasis of hepatocellular carcinoma cells]X L Geng
Department of Hepatobiliary Surgery, Shanxi Provincial People s Hospital, Xi an 710068, China
Zhonghua Zhong Liu Za Zhi 38:739-742. 2016b>Objective: To investigate the regulatory role of HK2 in the metastasis of hepatocellular carcinoma (HCC)...
- 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. ..
- ACTIVATION OF PROSTATE SPECIFIC ANTIGEN PRECURSORThomas 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...
- Geoffrey W Abbott; Fiscal Year: 2015....
- KALLIKREIN GENE EXPRESSION IN HUMAN PROSTATE CELLSCharles 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 ..
- Biacore T100 SPR system for studying and characterizing biomolecular interactionEwa Folta Stogniew; Fiscal Year: 2009....
- 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. ..
- Victoria L Seewaldt; Fiscal Year: 2015..PHS 398/2590 (Rev. 09/04, Reissued 4/2006) Page Continuation Format Page ..
- Modulation of Kir Channel Function by PhosphorylationDiomedes E Logothetis; Fiscal Year: 2012..This project aims to identify amino acid residues of cardiac potassium channel proteins that are phosphorylated...
- 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...
- SERINE PROTEASES IN PROSTATE CANCER METASTASISPeter 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...
- Potassium channels in myotonic dystrophy type 1Christine Beeton; Fiscal Year: 2012..Such new therapeutic targets would have tremendous benefits for public health. ..
- K+ channel protein complexes in auditory biologyWILLIAM 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. ..
- NOVEL MARKERS FOR PROSTATE CANCERCharles Young; Fiscal Year: 2005..Highly specific and sensitive immunoassays for serum human kallikrein 2 (hK2) have been developed for prostate cancer detection...
- Small Molecule Kv1.3 Blockers as New Therapeutics for Multiple SclerosisHeike 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. ..
- MOLECULAR DETERMINANTS OF POTASSIUM CHANNEL DRUG BLOCKDirk Snyders; Fiscal Year: 2003....
- REGULATORY MECHANISMS OF CARDIAC REPOLARIZATIONMichael 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. ..
- Targeting of Voltage-gated K+ Channels to Lipid RaftsMichael 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. ..
- NEW APPLICATIONS OF THE PROSTATE CANCER MARKER PSAPaul Lange; Fiscal Year: 2002..g. psm, hk2)...
- Cardiac KCNE2 (MIRP1) Regulation by Estrogen and Cardiac StressMansoureh 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. ..
- Trafficking and Regulation of Cardiovascular K+ ChannelsJEFFREY MARTENS; Fiscal Year: 2013....
- ERR-gamma-dependent mammary tumorigenesis in response to BPA and a high-fat dietRebecca 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...
- 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...
- 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. ..
- XIAOFENG FRANK YANG; Fiscal Year: 2016..ii) To determine the role of Hk2 in Rrp2 activation during tick transmission and mammalian infection...
- Nissim Hay; Fiscal Year: 2016DESCRIPTION (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...
- 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...
- Regulation of Kv Channels by AnorexigensBruce Pitt; Fiscal Year: 2007..1 proteins, inhibition of Kv1.5 gene transcription and blockade of Kv currents at plasma membrane. ..
- A Novel High Throughput Assay for Ion Channel ModulatorsBarbara Wible; Fiscal Year: 2006..The cardiac potassium channel hERG is the most common target of undesired drug interactions; block of hERG can predispose individuals ..
- REGULATION OF CARDIAC POTASSIUM CHANNEL GENE EXPRESSIONKoichi 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. ..
- A Novel High Throughput Assay for Ion Channel ModulatorsBarbara Wible; Fiscal Year: 2004..The cardiac potassium channel hERG is an example of frequent unwanted drug interactions; block of hERG can predispose individuals to ..
- MODULATION OF K+ CHANNEL FUNCTION BY PERMEANTIONSStephen 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. ..
- ITO IN DOGS WITH INHERITED VENTRICULAR ARRHYTHMIASBruce Kornreich; Fiscal Year: 2005..abstract_text> ..
- Postmortem PSA: role in epidemiology of prostate cancerGabriel 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...
- A High Throughput Assay for Cancer Drug CardiotoxicityBarbara 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 ..
- CARDIAC POTASSIUM CHANNEL SUBUNITS AND SUDDEN DEATHMartin 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. ..
- SNPs in Idopathic Pulmonary Artierial HypertensionJASON 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), ..
- Detection of occult prostate cancers in elderly menGabriel 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 ..
- VOLTAGE DEPENDENT K+ CHANNELS IN HEAT--KV15 ALPHA SUBUNIJoseph Hill; Fiscal Year: 2003..5. The methods to be used are biochemical and immunological (Western blots, immunoprecipitation) and electrophysiological (patch clamping, ambulatory electrocardiography). ..
- Molecular Recognition of Potassium ChannelsDirk 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. ..
- MODULATION OF VOLTAGE DEPENDENT POTASSIUM CHANNELSIRWIN LEVITAN; Fiscal Year: 2000....
- A Parallel High-Throughput Pharmacogenetic Profiling Assay for Clinical UseGao 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 ..
- HYPERTENSION: CONTRIBUTION OF ARTERIAL WALL CHANGESRobert 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. ..
- Methodology of Phase I and II trials of anticancer CAMAndrew Vickers; Fiscal Year: 2004....
- 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. ..
- A New Biomarker for Ovarian Cancer DetectionEleftherios 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. ..
- KALLIKREINS AS DIAGNOSTIC MARKERS OF OVARIAN CARCINOMAEleftherios Diamandis; Fiscal Year: 2008..unreadable] [unreadable] [unreadable]..
- Thyroid Hormone Receptor Function in Cardiac HypertrophyKaie Ojamaa; Fiscal Year: 2006..abstract_text> ..
- CARDIAC GROWTH REGULATIONKaie Ojamaa; Fiscal Year: 2002..End of Abstract) ..
- Long-term prediction of prostate cancer death from kallikreins measured in bloodHans 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...
- Role of Molecular Chaperones in hERG ProcessingEckhard Ficker; Fiscal Year: 2008..abstract_text> ..
- Genetic Aspects of Vestibular DysfunctionStephen 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. ..
- Breast Cancer Prediction Using Nipple Aspirate FluidEdward Sauter; Fiscal Year: 2007..unreadable] [unreadable]..
- MOLECULAR AND CHEMICAL DESCRIPTION OF CFTR FUNCTIONPeter 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. ..
- Pathogenesis of HIVAN: the role of NefJOHN 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. ..
- Genetic Epidemiology of Aging Skeletal MuscleStephen Roth; Fiscal Year: 2007..abstract_text> ..
- FORMS OF PROSTATE SPECIFIC ANTIGEN AND HK2 IN CANCERMARY HEEB; Fiscal Year: 2003We 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 ..
- THROMBOGENIC FACTORS AND RECURRENT CORONARY EVENTSArthur Moss; Fiscal Year: 2003..abstract_text> ..
- Defective trafficking Mechanisms in a Cardiac K+ ChannelSabina 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...
- Novel Anticoagulant MechanismsMARY HEEB; Fiscal Year: 2006..We will find whether a ZPI polymorphism we identified affects function. ..
- THERAPUTIC TRIAL IN PATIENTS WITH LQTS 3 GENE MUTATIONArthur 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. ..
- Genetic Architecture of Aging Skeletal MuscleStephen Roth; Fiscal Year: 2005..abstract_text> ..
- Cancer-Related Glycolytic Gene:Regulation and TargetingPeter Pedersen; Fiscal Year: 2008..abstract_text> ..
- Protein Profiling in Nipple Aspirate FluidEdward Sauter; Fiscal Year: 2007..abstract_text> ..
- Cytoskeletal Basis of Ventricular ArrhythmiasMatteo 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. ..
- Altered Breast Methylation after Low/Hi Dose IsoflavonesEdward Sauter; Fiscal Year: 2005..abstract_text> ..
- The Effect of Black Cohosh Extract on the Human BreastEdward 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. ..
- New drugs for treatment of atrial fibrillationAntonio Lacerda; Fiscal Year: 2004..ChanTest believes that this drug will offer great relief to the many people who are debilitated by atrial fibrillation. ..
- Fibroblast Activation Protein-alpha Activated Anti-Stromal Prodrug Therpay for CaSamuel 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. ..
- DEVELOPMENT OF VESTIBULAR NUCLEI NEURONSKENNA PEUSNER; Fiscal Year: 2005..abstract_text> ..
- ION CHANNELS IN DEMYELINATING DISEASESBetty Soliven; Fiscal Year: 2003..In addition, there may be ways to promote remyelination using the K+ channels of OP cells/OLGs as drug targets. ..
- CONTROL OF ENZYMATIC PHOSPHATE TRANSFER IN MITOCHONDRIAPeter 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. ..
- Identification of compounds that protect HERG from block by proarrhythmic agentsSabina 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 ..
- Novel therapeutic targets in inflammatory neuropathiesBetty Soliven; Fiscal Year: 2006..abstract_text> ..
- LONG QT SYNDROME--GENETIC STUDIESArthur Moss; Fiscal Year: 2002....
- Mutant ZASP in Cytoskeletal Remodeling and ArrhythmiaMatteo 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. ..