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

Authors
  • Grunbeck, Amy
  • Huber, Thomas
  • Abrol, Ravinder
  • Trzaskowski, Bartosz
  • Goddard, William A 3rd
  • Sakmar, Thomas P
Type
Published Article
Journal
ACS Chemical Biology
Publisher
American Chemical Society
Publication Date
Jun 15, 2012
Volume
7
Issue
6
Pages
967–972
Identifiers
DOI: 10.1021/cb300059z
PMID: 22455376
Source
Medline
License
Unknown

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.

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