http://purl.uniprot.org/citations/37099539 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
http://purl.uniprot.org/citations/37099539 | http://www.w3.org/2000/01/rdf-schema#comment | "A member of THIK (two pore domain halothane-inhibited K+) channels, THIK-1, was reported as a target of Gi/o-coupled receptors (Gi/o-Rs) in neurons and microglia. We confirmed that in HEK293T cells the THIK-1 channel is activated by Gi/o-Rs and found that Gq-coupled receptors (Gq-Rs) also activates the channel. The effects of Gi/o-Rs and Gq-Rs were inhibited by the Gi/o inhibitor pertussis toxin and phospholipase C (PLC) inhibitor, respectively. The effects of Gi/o-Rs were attenuated when consensus Gβγ binding motif at the C-tail of the THIK-1 channel was mutated, suggesting that Gβγ serves as a THIK-1 channel activator upon the stimulation of Gi/o-Rs. As to the effects of Gq-Rs on the THIK-1 channel, a protein kinase C inhibitor and calcium chelators failed to inhibit the effect of a Gq coupled muscarinic M1R. Neither the hydrolysis of phosphatidyl inositol bisphosphate induced by voltage sensitive phosphatase nor the application of a diacylglycerol analogue, OAG, increased the channel current. The mediator of Gq-dependent activation of the THIK-1 channel remained unsolved. The effects of Gi/o- and Gq-Rs on the THIK-2 channel were also investigated, by using a THIK-2 mutant channel whose N-terminal domain is deleted to improve the surface membrane expression. We observed that Gi/o- and Gq-Rs activate the mutated THIK-2 channel, similarly to the THIK-1 channel. Interestingly, heterodimeric channels of THIK-1 and THIK-2 responded to Gi/o-R and Gq-R stimulation. Taken together, Gi/o- or Gq-Rs activates the THIK-1 and THIK-2 channels in a Gβγ or PLC dependent manner, respectively."xsd:string |
http://purl.uniprot.org/citations/37099539 | http://purl.org/dc/terms/identifier | "doi:10.1371/journal.pone.0284962"xsd:string |
http://purl.uniprot.org/citations/37099539 | http://purl.uniprot.org/core/author | "Kubo Y."xsd:string |
http://purl.uniprot.org/citations/37099539 | http://purl.uniprot.org/core/author | "Tateyama M."xsd:string |
http://purl.uniprot.org/citations/37099539 | http://purl.uniprot.org/core/date | "2023"xsd:gYear |
http://purl.uniprot.org/citations/37099539 | http://purl.uniprot.org/core/name | "PLoS One"xsd:string |
http://purl.uniprot.org/citations/37099539 | http://purl.uniprot.org/core/pages | "e0284962"xsd:string |
http://purl.uniprot.org/citations/37099539 | http://purl.uniprot.org/core/title | "Regulation of the two-pore domain potassium channel, THIK-1 and THIK-2, by G protein coupled receptors."xsd:string |
http://purl.uniprot.org/citations/37099539 | http://purl.uniprot.org/core/volume | "18"xsd:string |
http://purl.uniprot.org/citations/37099539 | http://www.w3.org/2004/02/skos/core#exactMatch | http://purl.uniprot.org/pubmed/37099539 |
http://purl.uniprot.org/citations/37099539 | http://xmlns.com/foaf/0.1/primaryTopicOf | https://pubmed.ncbi.nlm.nih.gov/37099539 |
http://purl.uniprot.org/uniprot/#_Q9HB14-mappedCitation-37099539 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/37099539 |
http://purl.uniprot.org/uniprot/#_Q9HB15-mappedCitation-37099539 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/37099539 |
http://purl.uniprot.org/uniprot/Q9HB14 | http://purl.uniprot.org/core/mappedCitation | http://purl.uniprot.org/citations/37099539 |
http://purl.uniprot.org/uniprot/Q9HB15 | http://purl.uniprot.org/core/mappedCitation | http://purl.uniprot.org/citations/37099539 |