Property Summary

NCBI Gene PubMed Count 49
PubMed Score 264.70
PubTator Score 4098.25

Knowledge Summary

Patent (9,414)

Expression

 GWAS Trait (1)

Protein-protein Interaction (1)

MLP Assay (4)

AID Type Active / Inconclusive / Inactive Description
602410 screening 2843 / 0 / 337058 Primary cell-based screen for identification of compounds that inhibit the two-pore domain potassium channel KCNK3
602490 summary 0 / 0 / 0 Summary of assays for identification of compounds that inhibit the two-pore domain potassium channel KCNK3
651638 screening 2372 / 0 / 19 Confirmation assay for identification of compounds that inhibit the two-pore domain potassium channel KCNK3 [Primary Screening]
652212 confirmatory 94 / 0 / 4 SAR Analysis for the identification of inhibitors of the two-pore domain potassium channel TASK1 (KCNK3)

Gene RIF (44)

PMID Text
26912814 KCNK3 expression and function were reduced in pulmonary artery smooth muscle cells and endothelial cells in human pulmonary arterial hypertension.
25951834 Enhancement of atrium-selective K(2P)3.1 currents contributes to action potential shortening in atrial fibrillation patients.
25655935 TASK-1 and TASK-3 may form heterodimers in human atrial cardiomyocytes.
25420509 Diacylglycerol mediates regulation of TASK1 and TASK3 potassium channels by GNAQ.
24932805 A glucose-dependent role for beta-cell TASK-1 channels of limiting glucose-stimulated Deltapsip depolarization and insulin secretion, which modulates glucose homeostasis.
24743596 Syntaxin-8 regulates the endocytosis of TASK-1.
24374141 demonstrate the functional importance of ITASK in the atrium and suggest that inactivation of TASK-1 may have diverse effects on atrial size and electrophysiological properties that can contribute to an arrhythmogenic substrate
24035804 HIV-1 Vpu and TASK-1 decrease HIV-1 transcription by suppressing unintegrated HIV-1 DNA, which is inhibited by overexpression of RelA
24015703 Sec61 complex reorientation of the first signal-anchor sequence of TASK-1 determines membrane topology of the other membrane spanning regions.
23883380 Our study identified the association of a novel gene, KCNK3, with familial and idiopathic pulmonary arterial hypertension.
23831603 HIV-1 Vpu and TASK-1 decrease HIV-1 transcription by suppressing unintegrated HIV-1 DNA, which is inhibited by overexpression of RelA
23807092 K2P3.1 and K2P9.1 undergo rapid dynamin-dependent endocytosis
23305490 TASK and TREK-1 are involved in regulation of cell proliferation and in control of resting membrane potentials in endometrial epithelial cells.
23229553 Ability to induce atrial fibrillation in the peri-operative period is associated with phosphorylation-dependent inhibition of TWIK protein-related acid-sensitive potassium channel 1
23164059 TASK-1 suppresses HIV-1 replication.
23164059 HIV-1 Vpu and TASK-1 decrease HIV-1 transcription by suppressing unintegrated HIV-1 DNA, which is inhibited by overexpression of RelA
22893713 There were no associations between KCNK3 single nucleotide polymorphisms and blood pressure or aldosterone production.
22178873 I(TASK-1) contributes to the sustained outward current I(Ksus) and that I(TASK-1) is a major component of the background conductance in human atrial cardiomyocytes.
21838752 ET-1 inhibited TASK1-mediated I(KN) currents in hPASMC.
21710317 TASK-1 immunoreactivity was observed in astrocytes of temporal lobe epilepsy patients.
21540350 TASK-1- and TASK-3-mediated currents are not affected by depletion of plasma membrane PI4,5P2 either via the voltage-activated phosphatase Ci-VSP or via chemically triggered recruitment of a PI4,5P2-5'-phosphatase.
21362619 analysis of how the specific two-pore domain potassium channel blocker A1899 defines the structure of the TASK-1 open pore
21357689 cAMP-dependent protein kinase is responsible for the phosphorylation of the terminal serine in both K(2P)3.1 and K(2P)9.1
20931182 Western analysis confirms expression of TASK1 and TASK3 in medulloblastoma cells.
20049674 TASK-1 and 3 are determinant of aldosterone secretion and adrenocortical zonation.
20012522 HIV-1 Vpu and TASK-1 decrease HIV-1 transcription by suppressing unintegrated HIV-1 DNA, which is inhibited by overexpression of RelA
19657056 O2 binding with NOX4 per se controls TASK-1 activity. In this process, the heme moiety and FBD seem to be responsible for the NOX4 regulation of TASK-1, and p22 might support the NOX4-TASK-1 interaction
19188660 ET-1 depolarized human primary pulmonary artery smooth muscle cells by phosphorylating TASK-1. This effect was abrogated by TASK-1 siRNA. This might represent a novel pathologic mechanism related to pulmonary arterial hypertension.
18824070 Thus, regulated expression of TASK channels might contribute to a molecular switch between death and survival of neurons in autoimmune CNS inflammation.
18375952 K(2)P channels as novel potassium conductance on T lymphocytes critically influencing T cell effector function and identify a possible molecular target for immunomodulation in T cell-mediated autoimmune disorders
17945357 the role of TASK channels in sensing physiological stimuli.
16574908 TASK-1 is hypoxia-sensitive and controls the resting membrane potential, thus implicating an important role for TASK-1 K+ channels in the regulation of pulmonary vascular tone.
15695101 Human cytotrophoblast cells from term placenta are a site of expression for various K2P genes, two of which, namely, TASK1 and TREK1, are transcribed into protein.
15197476 TASK1 is expressed in pia mater, astrocytes, Purkinje and granule cells
15099524 Host TASK-1 protein and HIV-1 Vpu undergo mutual functional destruction.
15099524 HIV-1 Vpu and TASK-1 decrease HIV-1 transcription by suppressing unintegrated HIV-1 DNA, which is inhibited by overexpression of RelA
15099514 HIV-1 Vpu and TASK-1 decrease HIV-1 transcription by suppressing unintegrated HIV-1 DNA, which is inhibited by overexpression of RelA
12837685 hOAT1-expressing cell line showed extensive para-aminohippuric acid transport. hOAT1 also demonstrated 1:1 coupling between organic anion and dicarboxylate.
12437930 KCNK3 potassium channels are shown to bear two cytoplasmic trafficking motifs: an N-terminal dibasic site that binds beta-COP to hold channels in ER and a C-terminal "release" site that binds the ubiquitous intracellular regulator 14-3-3beta
12198146 Association with p11 is essential for trafficking of TASK-1 to the plasma membrane. This association masks an ER retention signal identified as Lys-Arg-Arg that precedes the Ser-Ser-Val sequence.
12003807 C-PAF blocks TASK-1 or a closely related channel, the effect is PKC dependent, and the inhibition alters the electrical activity of myocytes in ways that would be arrhythmogenic in the intact heart.
11907168 Renal Oat1 expression gradually increased throughout development, approaching adult levels at 30 days of age, where at days 40 and 45 Oat1 levels were greater in males than females
11886861 TASK-1 and TASK-3 differed insofar as a large portion of the C terminus was necessary for the full effects of halothane and TRH on TASK-3 but not on TASK-1
11803450 Observational study of gene-disease association. (HuGE Navigator)

AA Sequence

MKRQNVRTLALIVCTFTYLLVGAAVFDALESEPELIERQRLELRQQELRARYNLSQGGYEELERVVLRLK      1 - 70
PHKAGVQWRFAGSFYFAITVITTIGYGHAAPSTDGGKVFCMFYALLGIPLTLVMFQSLGERINTLVRYLL     71 - 140
HRAKKGLGMRRADVSMANMVLIGFFSCISTLCIGAAAFSHYEHWTFFQAYYYCFITLTTIGFGDYVALQK    141 - 210
DQALQTQPQYVAFSFVYILTGLTVIGAFLNLVVLRFMTMNAEDEKRDAEHRALLTRNGQAGGGGGGGSAH    211 - 280
TTDTASSTAAAGGGGFRNVYAEVLHFQSMCSCLWYKSREKLQYSIPMIIPRDLSTSDTCVEQSHSSPGGG    281 - 350
GRYSDTPSRRCLCSGAPRSAISSVSTGLHSLSTFRGLMKRRSSV                              351 - 394
//

Text Mined References (50)

PMID Year Title
26912814 2016 Potassium Channel Subfamily K Member 3 (KCNK3) Contributes to the Development of Pulmonary Arterial Hypertension.
25951834 2015 Upregulation of K(2P)3.1 K+ Current Causes Action Potential Shortening in Patients With Chronic Atrial Fibrillation.
25655935 2015 TASK-1 and TASK-3 may form heterodimers in human atrial cardiomyocytes.
25420509 2014 Diacylglycerol mediates regulation of TASK potassium channels by Gq-coupled receptors.
24932805 2014 Pancreatic ?-cell-specific ablation of TASK-1 channels augments glucose-stimulated calcium entry and insulin secretion, improving glucose tolerance.
24743596 2014 Cooperative endocytosis of the endosomal SNARE protein syntaxin-8 and the potassium channel TASK-1.
24374141 2014 Genetic variation in the two-pore domain potassium channel, TASK-1, may contribute to an atrial substrate for arrhythmogenesis.
24015703 2013 Reorientation of the first signal-anchor sequence during potassium channel biogenesis at the Sec61 complex.
23883380 2013 A novel channelopathy in pulmonary arterial hypertension.
23807092 Acid sensitive background potassium channels K2P3.1 and K2P9.1 undergo rapid dynamin-dependent endocytosis.
23305490 2013 A role for two-pore potassium (K2P) channels in endometrial epithelial function.
23229553 2013 Ability to induce atrial fibrillation in the peri-operative period is associated with phosphorylation-dependent inhibition of TWIK protein-related acid-sensitive potassium channel 1 (TASK-1).
23169818 2012 SUMOylation silences heterodimeric TASK potassium channels containing K2P1 subunits in cerebellar granule neurons.
23164059 2012 Human immunodeficiency virus type 1 Vpu and cellular TASK proteins suppress transcription of unintegrated HIV-1 DNA.
22893713 2012 Variations in the potassium channel genes KCNK3 and KCNK9 in relation to blood pressure and aldosterone production: an exploratory study.
22178873 2011 TASK-1 channels may modulate action potential duration of human atrial cardiomyocytes.
22020285 2011 Image-based genome-wide siRNA screen identifies selective autophagy factors.
21838752 2012 TASK1 (K(2P)3.1) K(+) channel inhibition by endothelin-1 is mediated through Rho kinase-dependent phosphorylation.
21710317 2011 Changes in TWIK-related acid sensitive K+-1 and -3 channel expressions from neurons to glia in the hippocampus of temporal lobe epilepsy patients and experimental animal model.
21540350 2011 Probing the regulation of TASK potassium channels by PI4,5P? with switchable phosphoinositide phosphatases.
21362619 2011 A specific two-pore domain potassium channel blocker defines the structure of the TASK-1 open pore.
21357689 2011 Protein kinase A is central for forward transport of two-pore domain potassium channels K2P3.1 and K2P9.1.
20931182 2010 Biophysical properties of human medulloblastoma cells.
20049674 2010 TASK1 and TASK3 potassium channels: determinants of aldosterone secretion and adrenocortical zonation.
19657056 2009 Identification of subdomains in NADPH oxidase-4 critical for the oxygen-dependent regulation of TASK-1 K+ channels.
19188660 2009 Endothelin-1 inhibits background two-pore domain channel TASK-1 in primary human pulmonary artery smooth muscle cells.
18824070 2008 Altered neuronal expression of TASK1 and TASK3 potassium channels in rodent and human autoimmune CNS inflammation.
18678320 2008 Maternally inherited Birk Barel mental retardation dysmorphism syndrome caused by a mutation in the genomically imprinted potassium channel KCNK9.
18375952 2008 TWIK-related acid-sensitive K+ channel 1 (TASK1) and TASK3 critically influence T lymphocyte effector functions.
17945357 2007 The TASK background K2P channels: chemo- and nutrient sensors.
16574908 2006 Impact of TASK-1 in human pulmonary artery smooth muscle cells.
16382106 2005 International Union of Pharmacology. LV. Nomenclature and molecular relationships of two-P potassium channels.
15815621 2005 Generation and annotation of the DNA sequences of human chromosomes 2 and 4.
15695101 2005 Localization of TASK and TREK, two-pore domain K+ channels, in human cytotrophoblast cells.
15197476 2004 Differential distribution of TASK-1, TASK-2 and TASK-3 immunoreactivities in the rat and human cerebellum.
15099524 2004 Mutual functional destruction of HIV-1 Vpu and host TASK-1 channel.
12837685 2003 Stoichiometry of organic anion/dicarboxylate exchange in membrane vesicles from rat renal cortex and hOAT1-expressing cells.
12477932 2002 Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences.
12437930 2002 Forward transport. 14-3-3 binding overcomes retention in endoplasmic reticulum by dibasic signals.
12198146 2002 p11, an annexin II subunit, an auxiliary protein associated with the background K+ channel, TASK-1.
11907168 2002 Gender-specific and developmental influences on the expression of rat organic anion transporters.
11886861 2002 Modulation of TASK-1 (Kcnk3) and TASK-3 (Kcnk9) potassium channels: volatile anesthetics and neurotransmitters share a molecular site of action.
11803450 2002 Association between anorexia nervosa and the hsKCa3 gene: a family-based and case control study.
11680614 2001 TASK-5, a novel member of the tandem pore K+ channel family.
11256078 2001 Potassium leak channels and the KCNK family of two-P-domain subunits.
10748056 2000 Proton block and voltage gating are potassium-dependent in the cardiac leak channel Kcnk3.
10575216 1999 Assignment of the 2P domain, acid-sensitive potassium channel OAT1 gene KCNK3 to human chromosome bands 2p24.1-->p23.3 and murine 5B by in situ hybridization.
10321245 1999 Inhalational anesthetics activate two-pore-domain background K+ channels.
9721223 1998 Mapping of human potassium channel genes TREK-1 (KCNK2) and TASK (KCNK3) to chromosomes 1q41 and 2p23.
9312005 1997 TASK, a human background K+ channel to sense external pH variations near physiological pH.