G beta gamma binds directly to the G protein-gated K+ channel, IKACh.

作者: Grigory Krapivinsky , Luba Krapivinsky , Kevin Wickman , David E. Clapham

DOI: 10.1074/JBC.270.49.29059

关键词: GuanosineGTP-binding protein regulatorsGTP'Potassium channelInward-rectifier potassium ion channelG beta-gamma complexHeterotrimeric G proteinBioinformaticsChemistryStereochemistryG protein

摘要: The cardiac G protein-gated K+ channel, IKACh, is activated by application of purified and recombinant beta gamma subunits (G gamma) heterotrimeric proteins to excised inside-out patches from atrial membranes (Logothetis, D. E., Kurachi, Y., Galper, J., Neer, Clapham, E. (1987) Nature 325, 321-326; Wickman, K., Iniguez-Lluhi, Davenport, P., Taussig, R. A., Krapivinsky, G. B., Linder, M. Gilman, D.E. (1994) 368, 255-257). Cardiac IKACh composed two inward rectifier channel subunits, GIRK1 CIR (Krapivinsky, G., Gordon, Velimirovic, L., (1995) 374, 135-141). We show that directly binds immunoprecipitated as well with dissociation constants (Kd) 55, 50, 125 nM, respectively. In each case, binding appeared specific judged competition unlabeled radiolabeled inhibition antigenic peptide or alpha-GDP, but not alpha-GTP S (guanosine 5'-3-O-(thio)triphosphate). contrast, alpha (GTP S- GDP-bound) did bind the native channel. conclude specifically via interactions both gate

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