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http://purl.uniprot.org/citations/35212627 | http://www.w3.org/2000/01/rdf-schema#comment | "ATP-sensitive K+ (KATP) channels in pancreatic β cells are comprised of pore-forming subunits (Kir6.2) and modulatory sulfonylurea receptor subunits (SUR1). The ATP sensitivity of these channels enables them to couple metabolic state to insulin secretion in β cells. Antidiabetic sulfonylureas such as glibenclamide target SUR1 and indirectly suppress Kir6.2 activity. Glibenclamide acts as both a primary and a secondary secretagogue to trigger insulin secretion and potentiate glucose-stimulated insulin secretion, respectively. We tested whether blocking Kir6.2 itself causes the same effects as glibenclamide, and found that the Kir6.2 pore-blocking venom toxin SpTx1 acts as a strong secondary, but not a strong primary, secretagogue. SpTx1 triggered a transient rise of plasma insulin and lowered the elevated blood glucose of diabetic mice overexpressing Kir6.2 but did not affect those of nondiabetic mice. This proof-of-concept study suggests that blocking Kir6.2 may serve as an effective treatment for diabetes and other diseases stemming from KATP hyperactivity that cannot be adequately suppressed with sulfonylureas."xsd:string |
http://purl.uniprot.org/citations/35212627 | http://purl.org/dc/terms/identifier | "doi:10.7554/elife.77026"xsd:string |
http://purl.uniprot.org/citations/35212627 | http://purl.uniprot.org/core/author | "Lu Z."xsd:string |
http://purl.uniprot.org/citations/35212627 | http://purl.uniprot.org/core/author | "Zhou Y."xsd:string |
http://purl.uniprot.org/citations/35212627 | http://purl.uniprot.org/core/author | "Hoshi T."xsd:string |
http://purl.uniprot.org/citations/35212627 | http://purl.uniprot.org/core/author | "Yamakaze J."xsd:string |
http://purl.uniprot.org/citations/35212627 | http://purl.uniprot.org/core/author | "Ramu Y."xsd:string |
http://purl.uniprot.org/citations/35212627 | http://purl.uniprot.org/core/date | "2022"xsd:gYear |
http://purl.uniprot.org/citations/35212627 | http://purl.uniprot.org/core/name | "Elife"xsd:string |
http://purl.uniprot.org/citations/35212627 | http://purl.uniprot.org/core/pages | "e77026"xsd:string |
http://purl.uniprot.org/citations/35212627 | http://purl.uniprot.org/core/title | "Blocking Kir6.2 channels with SpTx1 potentiates glucose-stimulated insulin secretion from murine pancreatic beta cells and lowers blood glucose in diabetic mice."xsd:string |
http://purl.uniprot.org/citations/35212627 | http://purl.uniprot.org/core/volume | "11"xsd:string |
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