Crystal Structures of the A Adenosine Receptor and Their Use in Medicinal Chemistry

Overview

Journal In Silico Pharmacol

Date 2014 Mar 25

PMID 24660138

Citations 3

Authors

Kenneth A Jacobson

Affiliations

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Abstract

New insights into drug design are derived from the X-ray crystallographic structures of G protein-coupled receptors (GPCRs), and the adenosine receptors (ARs) are at the forefront of this effort. The 3D knowledge of receptor binding and activation promises to enable drug discovery for GPCRs in general, and specifically for the ARs. The predictability of modeling based on the X-ray structures of the AAR has been well demonstrated in the identification, design and modification of both known and novel AR agonists and antagonists. It is expected that structure-based design of drugs acting through ARs will provide new avenues to clinically useful agents.

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