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Structural Basis for Ligand Recognition and Functional Selectivity at Angiotensin Receptor.

J Biol Chem.. 2015-12; 
Zhang H, Unal H, Desnoyer R, Han GW, Patel N, Katritch V, Karnik SS, Cherezov V, Stevens RC.
Products/Services Used Details Operation
Peptide Synthesis ... peptide ligand TRV120027. EXPERIMENTAL PROCEDURES Protein engineering for structural studies–DNA encoding the human AT1R was optimized for insect cells expression and synthesized by GenScript. The construct used ... Get A Quote
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摘要

Angiotensin II type 1 receptor (AT1R) is the primary blood pressure regulator. AT1R blockers (ARBs) have been widely used in clinical settings as anti-hypertensive drugs and share a similar chemical scaffold, although even minor variations can lead to distinct therapeutic efficacies toward cardiovascular etiologies. The structural basis for AT1R modulation by different peptide and non-peptide ligands has remained elusive. Here, we report the crystal structure of the human AT1R in complex with an inverse agonist olmesartan (Benicar(TM)), a highly potent anti-hypertensive drug. Olmesartan is anchored to the receptor primarily by the residues Tyr-35(1.39), Trp-84(2.60), and Arg-167(ECL2), similar to the antagonist... More

关键词

G protein-coupled receptor (GPCR); angiotensin; biased ligands; crystal structure; hypertension; protein-drug interaction; sodium ion