Recombinant Human Potassium voltage-gated channel subfamily A member 5 (KCNA5)

1. Molecular dynamics simulations are employed to determine the inhibitory mechanisms of three drugs, 5-(4-phenoxybutoxy)psoralen (PAP-1), vernakalant, and flecainide, on the voltage-gated K(+) channel Kv1.5, a target for the treatment of cardiac arrhythmia. PMID: 29652491
2. This study adds insights to the functional impact of KCNA5 mutations in modulating atrial contractile functions. PMID: 28803858
3. In addition, as IKur is an atrial-specific channel and a number of IKur-selective blockers have been developed as anti-AF agents, this study also helps to understand some contradictory results on both pro- and anti-arrhythmic effects of blocking IKur. PMID: 28622331
4. our finding indicated that KCNA5 protein may interact with Cav-1, thereby contributing to the proliferation and early transformation of mammary cells. PMID: 27075359
5. Putative binding sites for arachidonic acid on the human cardiac Kv 1.5 channel PMID: 26292661
6. Studies demonstrate that DNA hypermethylation contributes to epigenetic repression of the KCNA5 locus and that the resulting suppression of the Kv1.5 ion channel supports cancer cell proliferation. PMID: 26573141
7. Kv1.5 expression is increased in osteosarcoma cells and tissues and shRNA mediated silencing of Kv1.5 results in cell proliferation inhibition, cell cycle arrest, and induces cell apoptosis. PMID: 26569226
8. Direct interaction with specific amino acids underlies the blocking action of propofol on voltage-gated hKv1.5 channel. PMID: 26256861
9. demonstrate that PK treatment cleaved mature membrane-bound (75kDa) Kv1.5 channels at a single locus in the S1-S2 linker, producing 42-kDa N-terminal fragments and 33-kDa C-terminal fragments PMID: 26874203
10. These results indicate that CHIP decreases the Kv1.5 protein level and functional channel by facilitating its degradation in concert with chaperone Hsc70 PMID: 26232501
11. The expression of Kv1.5 channel protein changes with atrial fibrillation but not with age, rheumatic heart diseases, and sex in atrial fibrillation. PMID: 25918274
12. One KCNA5 variant, H463R, was a novel mutation; the histidine at codon 463 is located in the S5-pore loop, in the vicinity of the pore of KV1.5 subunit. The other variant, T527M, showed a gain-of-function effect with an enhanced steady-state activation. PMID: 26129877
13. The KCNA5 promoter is marked in cancer cells with PcG-dependent chromatin repressive modifications that increase in hypoxia. PMID: 25435365
14. Mutations in KCNA5 gene is not associated with pulmonary arterial hypertension. PMID: 24936649
15. Protein kinase C inhibition results in a Kv 1.5 and Kv beta 1.3 pharmacology closer to Kv 1.5 channels PMID: 24946104
16. Data do not indicate an important role of potassium voltage-gated channel shaker-related subfamily member 5 (KCNA5) as a sclerosis (SSc)-susceptibility factor or as a pulmonary arterial hypertension (PAH)-development genetic marker for SSc patients. PMID: 23270786
17. These results indicate that low temperature exposure stabilizes the protein in the cellular organelles or on the plasma membrane, and modulates its maturation and trafficking, thus enhancing the currents of hKv1.5 and its trafficking defect mutants. PMID: 24663680
18. Kv1.5 is a determinant of human B cell proliferation and migration, thereby identifying this channel as a new target for immunomodulation. PMID: 23847097
19. Results identified gain and loss of function mutations which lead to increased and decreased potassium currents enhancing AF. PMID: 23264583
20. AMPK is a potent regulator of Kv1.5. AMPK inhibits Kv1.5 presumably in part by activation of Nedd4- 2 with subsequent clearance of channel protein from the cell membrane. PMID: 23221389
21. Incretin regulation of beta-cell function involves the acetylation of Kv1.5. PMID: 23390957
22. Kv1.5 may play an important role in oxidative vascular endothelial injury PMID: 23185428
23. Ethanol prologned the action potential duration in isolated myocardium, which may be due to inhibition of Kv1.5 channel currents. PMID: 21681339
24. The experiments disclose a completely novel function of beta-catenin, i.e. the regulation of Kv1.5 channel activity. PMID: 22166221
25. In order to substantiate a possible relation between K(v1.5) and FHL1C, a pull-down assay was performed. PMID: 22053194
26. Our data implicate abnormal atrial repolarization control due to variable TK signaling as a mechanism in familial AF and thereby suggest a role for modulation of this pathway in AF and its treatment. PMID: 20638934
27. In Kv1.5 H+ and Ni2+ differentially enhance a slow inactivation process that involves at least two inactivated states and that resting inactivation is probably a close variant of slow inactivation. PMID: 20581043
28. an association was found solely for Pulmonary arterial hypertension associated with Systemic Sclerosis in KCNA5 ((potassium voltage-gated channel subfamily A member 5) rs10744676 variants PMID: 20556823
29. Kv1.5 channel is blocked by diphenyl phosphine oxide-1 PMID: 20184887
30. KCNA5 T527M mutation exerted a predominant negative effect on potassium currents but no effect on the subcellular location of the encoded ion channel. PMID: 20646426
31. Biolistically introduced exogenous voltage-gated potassium channel, Kv1.5, is functional and, like endogenous Kv1.5, localizes to the intercalated disc, where it is expressed at the surface of that structure. PMID: 20357183
32. Anandamide structure may a determinant of cannabinoid receptor-independent modulation. PMID: 20133392
33. Data support a role for the T1 domain in channel kinetics as well as in KCNA5 channel subcellular localization. PMID: 20018952
34. Overexpression of Kv1.5 is associated with cancer. PMID: 20025600
35. In the absence of potassium ion, significant N-methyl-D-glucamine (NMDG)-positive currents could be recorded from human embryonic kidney cells expressing Kv3.1 or Kv3.2b channels and Kv1.5 Arg487Tyr/Val, but not wild-type channels. PMID: 19332619
36. These findings expand the spectrum of mutations in KCNA5 linked to atrial fibrillation (AF) and provide new insight into the molecular mechanism involved in AF. PMID: 19343045
37. characterization of a truncated form of Kv1.5 PMID: 12021261
38. Modulation by protein kinase C activation: role of the Kvbeta1.2 subunit. PMID: 12130714
39. co-localization of Kv1.5 with PSD95 at the cell surface is similarly independent of the canonical PDZ-binding motif PMID: 12435606
40. Reduction in the activation energy for the inactivation transition from the open state underlies the inhibition of hKv1.5 Na(+) current at low pH. PMID: 12601085
41. Kv1.5 potassium channel mRNA expression correlates with glioma entities and malignancy grades; expression is high in astrocytomas, moderate in oligodendrogliomas, and low in glioblastomas. PMID: 12850541
42. multiple isoforms of SAP97 were identifed in human heart atrium specimens; isoforms were found to co-immunoprecipiate with hKv1.5; isoforms were found to have distinct effect on hKv1.5 current and spatial channel organization PMID: 12970345
43. the destabilization or bending of the S6 alpha-helix of KV1.5 caused by the PXP motif apparently creates a flexible "hinge" that allows movement of the lower S6 segment during channel gating and opening PMID: 13679372
44. No electrical remodeling is evident in Kv1.5DN-expressing ventricular myocytes, and the (Kv1.5DN-induced) elimination of IK,slow1 does not result in spontaneous ventricular arrhythmias. PMID: 14527939
45. an examination of the effect of K channel blocker S0100176) on the structure of the Kv1.5 channel PMID: 14578345
46. Overexpression of the human KCNA5 gene increases K+ currents (i.e., K+ efflux or loss), accelerates apoptotic volume decrease (AVD), increases caspase-3 activity, and induces apoptosis PMID: 15140747
47. Heterologously expressed human pulmonary arterial smooth muscle cells (PASMC) Kv1.5 generated an O2- and correolide-sensitive I(K) like that in resistance PASMCs. PMID: 15217912
48. There is a central role for developmentally regulated ductus arteriosus SMC O2-sensitive Kv channels in the functional closure of the DA. PMID: 15353504
49. This suggests that for Kv channels, the coupling between voltage sensing and gating reflects primarily an intrasubunit interaction. PMID: 15623896
50. P. 142: "An aligment of KCNA5 among human, mouse, and rat shows 86% amino acid identity, and no monogenicc human arrhythmia syndrome has been linked to KCNA5" PMID: 15735608

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HGNC: 6224

OMIM: 176267

KEGG: hsa:3741

STRING: 9606.ENSP00000252321

UniGene: Hs.150208