Gene Symbol: KCNG3
Description: potassium voltage-gated channel modifier subfamily G member 3
Alias: KV10.1, KV6.3, potassium voltage-gated channel subfamily G member 3, potassium channel, voltage gated modifier subfamily G, member 3, potassium voltage-gated channel, subfamily G, member 3, voltage-gated potassium channel 6.3, voltage-gated potassium channel Kv10.1, voltage-gated potassium channel subunit Kv10.1, voltage-gated potassium channel subunit Kv6.3, voltage-gated potassium channel subunit Kv6.4
- Pardo L, Gomez Varela D, Major F, Sansuk K, Leurs R, Downie B, et al. Approaches targeting K(V)10.1 open a novel window for cancer diagnosis and therapy. Curr Med Chem. 2012;19:675-82 pubmed..1 opens a novel window for treating cancer. In this review we will give an overview of the current status of data linking K(V)10.1 to cancer, and propose techniques that could exploit K(V)10.1's properties for the management of cancer. ..
- Moreels L, Peigneur S, Yamaguchi Y, Vriens K, Waelkens E, Zhu S, et al. Expanding the pharmacological profile of κ-hefutoxin 1 and analogues: A focus on the inhibitory effect on the oncogenic channel Kv10.1. Peptides. 2016;: pubmed publisher..Hefutoxin 1 showed low activity against the plant pathogen Fusarium culmorum and no activity against three other yeast and fungal species, even at high concentrations (∼100μM). ..
- Sano Y, Mochizuki S, Miyake A, Kitada C, Inamura K, Yokoi H, et al. Molecular cloning and characterization of Kv6.3, a novel modulatory subunit for voltage-gated K(+) channel Kv2.1. FEBS Lett. 2002;512:230-4 pubmed..1 channels. Immunoprecipitation studies indicated that Kv6.3 bound with Kv2.1 in co-transfected cells. These results indicate that Kv6.3 is a novel member of the voltage-gated K(+) channel which functions as a modulatory subunit. ..
- Vega Saenz de Miera E. Modification of Kv2.1 K+ currents by the silent Kv10 subunits. Brain Res Mol Brain Res. 2004;123:91-103 pubmed..The gene that encodes for Kv10.1 mRNAs maps to chromosome 2p22.1 in human, 6q12 in rat and 17E4 in mouse, locations consistent with the known systeny for human, rat and mouse chromosomes. ..
- Barriga Montoya C, Huanosta Gutiérrez A, Reyes Vaca A, Hernandez Cruz A, Picones A, Gomez Lagunas F. Inhibition of the K+ conductance and Cole-Moore shift of the oncogenic Kv10.1 channel by amiodarone. Pflugers Arch. 2017;: pubmed publisher..Our observations are interpreted considering the structural-functional characteristics of these channels. We conclude that amiodarone possibly binds with high affinity to the voltage sensor module, altering the gating of Kv10.1...
- Ottschytsch N, Raes A, Van Hoorick D, Snyders D. Obligatory heterotetramerization of three previously uncharacterized Kv channel alpha-subunits identified in the human genome. Proc Natl Acad Sci U S A. 2002;99:7986-91 pubmed..Including the subunits described here, the "silent subunits" represent one-third of all Kv subunits, suggesting that obligatory heterotetramer formation is more widespread than previously thought. ..
- Moreels L, Bhat C, Voráčová M, Peigneur S, Goovaerts H, Mäki Lohiluoma E, et al. Synthesis of novel purpurealidin analogs and evaluation of their effect on the cancer-relevant potassium channel KV10.1. PLoS ONE. 2017;12:e0188811 pubmed publisher..1 inhibitors can be interesting anticancer drug lead compounds, the effect of 5 was evaluated on cancerous and non-cancerous cell lines. Compound 5 showed to be cytotoxic and appeared to induce apoptosis in all the evaluated cell lines...
- Mederos y Schnitzler M, Rinné S, Skrobek L, Renigunta V, Schlichthörl G, Derst C, et al. Mutation of histidine 105 in the T1 domain of the potassium channel Kv2.1 disrupts heteromerization with Kv6.3 and Kv6.4. J Biol Chem. 2009;284:4695-704 pubmed publisher..1 is required for functional heteromerization with members of the Kv6 subfamily. We conclude from our findings that Kv2.1 and Kv6.x subunits have complementary T1 domains that control selective heteromerization. ..
- Martinez R, Stuhmer W, Martin S, Schell J, Reichmann A, Rohde V, et al. Analysis of the expression of Kv10.1 potassium channel in patients with brain metastases and glioblastoma multiforme: impact on survival. BMC Cancer. 2015;15:839 pubmed publisher..1 expression to patients with brain metastases or GBMs and, moreover, they strongly suggest a role of tricyclic antidepressants for personalized therapy of brain malignancies. ..
- Moreels L, Peigneur S, Galan D, De Pauw E, Béress L, Waelkens E, et al. APETx4, a Novel Sea Anemone Toxin and a Modulator of the Cancer-Relevant Potassium Channel KV10.1. Mar Drugs. 2017;15: pubmed publisher..This newly identified KV10.1 inhibitor can be used as a tool to further characterize the oncogenic channel KV10.1 or as a scaffold for the design and synthesis of more potent and safer anticancer drugs. ..