To Bind or Not to Bind: Unravelling GPCR Polypharmacology

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Abstract

Interaction of a single drug with multiple targets through “polypharmacology” is increasingly recognized as necessary for treatment of complex diseases, such as schizophrenia. G protein-coupled receptors (GPCRs) are major medicinal targets, and understanding the structural basis of both GPCR drug selectivity and promiscuity could provide novel avenues for drug development. Interaction of a single drug with multiple targets through “polypharmacology” is increasingly recognized as necessary for treatment of complex diseases, such as schizophrenia. G protein-coupled receptors (GPCRs) are major medicinal targets, and understanding the structural basis of both GPCR drug selectivity and promiscuity could provide novel avenues for drug development.

Original languageEnglish
Pages (from-to)636-638
Number of pages3
JournalCell
Volume172
Issue number4
DOIs
Publication statusPublished - 8 Feb 2018

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