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

Grunbeck, A.; Huber, T.; Abrol, R.; Trzaskowski, B.; Goddard, W.A.; Sakmar, T.P.

Acs Chemical Biology 7(6): 967-972


ISSN/ISBN: 1554-8937
PMID: 22455376
DOI: 10.1021/cb300059z
Accession: 053390033

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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.