RGS2/G0S8 is a selective inhibitor of Gqα function
作者： S. P. Heximer , N. Watson , M. E. Linder , K. J. Blumer , J. R. Hepler
关键词: GTPase-activating protein 、 Biology 、 Regulator of G protein signaling 、 RGS2 、 GTP-binding protein regulators 、 Cell biology 、 G protein 、 RGS Proteins 、 Biochemistry 、 RGS4 、 Heterotrimeric G protein
摘要: RGS (regulators of G protein signaling) proteins are GTPase activating that inhibit signaling by heterotrimeric proteins. All studied to date act on members the Giα family, but not Gsα or G12α. RGS4 regulates family and Gqα. RGS2 (G0S8) is exceptional because it have been identified. We report a selective potent inhibitor Gqα function. selectively binds Gqα, other Gα (Gi, Go, Gs, G12/13) in brain membranes; members. purified recombinant Goα, whereas either. does stimulate activities members, even at concentration 3000-fold higher than sufficient observe effects In contrast, completely Gq-directed activation phospholipase C cell membranes. When reconstituted with phospholipid vesicles, 10-fold more blocking Gqα-directed Cβ1. These results identify clear physiological role for RGS2, describe first example an
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