Cross-pharmacology Analysis of G Protein-coupled Receptors

Overview

Journal Curr Top Med Chem

Publisher Bentham Science Publishers

Specialty Chemistry

Date 2011 Aug 20

PMID 21851335

Citations 13

Authors

Ferran Brianso

Maria C Carrascosa

Tudor I Oprea

Jordi Mestres

Affiliations

Soon will be listed here.

Abstract

The degree of applicability of chemogenomic approaches to protein families depends on the accuracy and completeness of pharmacological data and the corresponding level of pharmacological similarity observed among their protein members. The recent public domain availability of pharmacological data for thousands of small molecules on 204 G protein-coupled receptors (GPCRs) provides a firm basis for an in-depth cross-pharmacology analysis of this superfamily. The number of protein targets included in the cross-pharmacology profile of the different GPCRs changes significantly upon varying the ligand similarity and binding affinity criteria. However, with the exception of muscarinic receptors, aminergic GPCRs distinguish themselves from the rest of the members in the family by their remarkably high levels of pharmacological similarity among them. Clusters of non-GPCR targets related by cross-pharmacology with particular GPCRs are identified and the implications for unwanted side-effects, as well as for repurposing opportunities, discussed.

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