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Snapshot of Activated G Proteins at the Membrane: The G[alpha][subscript q]-GRK2-G{szligbeta}[gamma] Complex

Author:
Tesmer, Valerie M., Kawano, Takeharu, Shankaranarayanan, Aruna, Kozasa, Tohru, Tesmer, John J. G.
Source:
Science 2005 v.310 no.5754 pp. 1686-1690
ISSN:
0036-8075
Subject:
G-protein coupled receptors, sequence homology
Abstract:
G protein-coupled receptor kinase 2 (GRK2) plays a key role in the desensitization of G protein-coupled receptor signaling by phosphorylating activated heptahelical receptors and by sequestering heterotrimeric G proteins. We report the atomic structure of GRK2 in complex with G[alpha][subscript q] and G{szligbeta}[gamma], in which the activated G[alpha] subunit of G[subscript q] is fully dissociated from G{szligbeta}[gamma] and dramatically reoriented from its position in the inactive G[alpha]{szligbeta}[gamma] heterotrimer. G[alpha][subscript q] forms an effector-like interaction with the GRK2 regulator of G protein signaling (RGS) homology domain that is distinct from and does not overlap with that used to bind RGS proteins such as RGS4.
Agid:
1530926