Products/Services Used | Details | Operation |
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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 |
Insect Expression System > | Get A Quote |
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