To Bind or Not to Bind: Unravelling GPCR Polypharmacology

Patrick M. Sexton; Arthur Christopoulos

doi:10.1016/j.cell.2018.01.018

To Bind or Not to Bind: Unravelling GPCR Polypharmacology

Patrick M. Sexton, Arthur Christopoulos

Drug Discovery Biology

Research output: Contribution to journal › Short Survey › Other › peer-review

18 Citations (Scopus)

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 language	English
Pages (from-to)	636-638
Number of pages	3
Journal	Cell
Volume	172
Issue number	4
DOIs	https://doi.org/10.1016/j.cell.2018.01.018
Publication status	Published - 8 Feb 2018

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To Bind or Not to Bind: Unravelling GPCR Polypharmacology

Abstract

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