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ACS Chem Biol. 2012 Jun 15;7(6):967-72. doi: 10.1021/cb300059z. Epub 2012 Apr 10.

Genetically encoded photo-cross-linkers map the binding site of an allosteric drug on a G protein-coupled receptor.

Abstract

G protein-coupled receptors (GPCRs) are dynamic membrane proteins that bind extracellular molecules to transduce signals. Although GPCRs represent the largest class of therapeutic targets, only a small percentage of their ligand-binding sites are precisely defined. Here we describe the novel application of targeted photo-cross-linking using unnatural amino acids to obtain structural information about the allosteric binding site of a small molecule drug, the CCR5-targeted HIV-1 co-receptor blocker maraviroc.

PMID:
22455376
DOI:
10.1021/cb300059z
[Indexed for MEDLINE]

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