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Bioorg Med Chem Lett. 2014 Sep 1;24(17):4073-9. doi: 10.1016/j.bmcl.2014.07.009. Epub 2014 Jul 10.

GPCR structures in drug design, emerging opportunities with new structures.

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Department for Lead Identification and Optimization Support, Boehringer Ingelheim Pharma GmbH & Co KG, Birkendorfer Straße 65, D-88397 Biberach an der Riss, Germany. Electronic address:


In recent years, GPCR targets from diverse regions of phylogenetic space have been determined. This effort has culminated this year in the determination of representatives of all major classes of GPCRs (A, B, C, and F). Although much of the now well established knowledge on GPCR structures has been known for some years, the new high-resolution structures allow structural insight into the causes of ligand efficacy, biased signaling, and allosteric modulation. In this digest the structural basis for GPCR signaling in the light of the new structures is reviewed and the use of the new non-class A GPCRs for drug design is discussed.


GPCR structure; Ligand bias; Structure based drug design

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