Cross-Pharmacology Analysis of G Protein-Coupled Receptors

Author(s): Ferran Brianso, Maria C. Carrascosa, Tudor I. Oprea, Jordi Mestres.

Journal Name: Current Topics in Medicinal Chemistry

Volume 11 , Issue 15 , 2011

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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.

Keywords: GPCR network, ligand similarity, target profile, adverse effects, drug repositioning, pharmacological similarity, cross-pharmacology analysis, muscarinic receptors,, Clusters of non-GPCR targets, GPCR-directed chemical libraries, crosspharmacology signals, Chemogenomic Databases

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Article Details

Year: 2011
Page: [1956 - 1963]
Pages: 8
DOI: 10.2174/156802611796391285
Price: $65

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