4.7 Review

Angiotensin II receptor type 1-An update on structure, expression and pathology

Journal

BIOCHEMICAL PHARMACOLOGY
Volume 192, Issue -, Pages -

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bcp.2021.114673

Keywords

AT(1) receptor; AT1R; AGTR1; Angiotensin II; X-ray crystallography; Protein structure; Biased agonists; Cardiovascular pathology

Funding

  1. Deutsche Forschungsgemeinschaft [DFG BE 3246/6-1, DFG GE 905/24-1]

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The AT(1) receptor plays a significant role in cardiovascular and renal diseases, and is a major target for angiotensin receptor blockers such as sartans. Recent studies have provided new insights into the structure and biased signaling of this receptor, which could lead to the development of novel therapeutic approaches.
The AT(1) receptor, a major effector of the renin-angiotensin system, has been extensively studied in the context of cardiovascular and renal disease. Moreover, angiotensin receptor blockers, sartans, are among the most frequently prescribed drugs for the treatment of hypertension, chronic heart failure and chronic kidney disease. However, precise molecular insights into the structure of this important drug target have not been available until recently. In this context, seminal studies have now revealed exciting new insights into the structure and biased signaling of the receptor and may thus foster the development of novel therapeutic approaches to enhance the efficacy of pharmacological angiotensin receptor antagonism or to enable therapeutic induction of biased receptor activity. In this review, we will therefore highlight these and other seminal publications to summarize the current understanding of the tertiary structure, ligand binding properties and downstream signal transduction of the AT(1) receptor.

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