To Bind or Not to Bind: Unravelling GPCR Polypharmacology.

Sexton, Patrick M; Christopoulos, Arthur · Cell · 2018

basic_science · Level V

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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.

Medical subject headings