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- W4377029300 abstract "<b>Abstract ID 25473</b> <b>Poster Board 149</b> The angiotensin II type 1 receptor 1 (AT<sub>1</sub>R) is a G protein-coupled receptor that is a critical regulator of blood pressure and a validated drug target for cardiovascular disease. AT1R signaling is initiated when binding of an extracellular ligand allosterically changes the conformation of the intracellular transducer binding site to activate transducers like heterotrimeric G proteins, GRKs, and <i>ss</i>-arrestins. The AT<sub>1</sub>R is known to activate several different G protein subfamilies, including G<sub>q/11</sub> and G<sub>i/o</sub>. However, these subfamilies exhibit very distinct patterns of allostery at the AT1R. Gq shows strong allosteric coupling to a select few AT1R ligands, but Gi shows relatively weak allosteric coupling to a much broader range of AT1R ligands. Here, we employ mini G proteins, built on a G<sub>s</sub> protein scaffold, to demonstrate that eight subtype-specific residues from the C-terminal a5 helix of G<sub>q</sub> and G<sub>i</sub> are sufficient to recapitulate ligand-specific patterns of allosteric coupling to the AT1R. Within this subset of G protein residues, a few key sites disproportionately contribute to G<sub>q</sub>’s strong allosteric effects on ligand binding. These data provide insights into the specific conformational features that different transducers recognize and could ultimately contribute to the design of ligands biased towards the activation of specific G protein subtypes. LMW is a Whitehead Scholar and a Pew Scholar in the Biomedical Sciences, supported by The Pew Charitable Trusts." @default.
- W4377029300 created "2023-05-19" @default.
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- W4377029300 date "2023-05-18" @default.
- W4377029300 modified "2023-09-29" @default.
- W4377029300 title "Molecular Determinants of Ligand-Induced Allosteric Coupling to Gq and Gi at the Angiotensin II Type 1 Receptor" @default.
- W4377029300 doi "https://doi.org/10.1124/jpet.122.254730" @default.
- W4377029300 hasPublicationYear "2023" @default.
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