CaltechAUTHORS
Published June 2012 | Version Supplemental Material
Journal Article Open

Genetically Encoded Photo-cross-linkers Map the Binding Site of an Allosteric Drug on a G Protein-Coupled Receptor

Creators

  • 1. ROR icon Rockefeller University
  • 2. ROR icon California Institute of Technology

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.

Additional Information

© 2012 American Chemical Society. Received: February 8, 2012. Accepted: March 28, 2012. Publication Date (Web): March 28, 2012. We wish to thank M. Teintze and E. Dratz for helpful discussions and for providing reagents for use in ongoing work. We also thank M. Kazmi and K. Thapa for scientific assistance. W.A.G. acknowledges support in part through funding from PharmSelex and in part through gifts to the Materials and Process Simulation Center at Caltech. The Tri-Institutional Training Program in Chemical Biology supports A.G. The authors declare no competing financial interest.

Attached Files

Supplemental Material - cb300059z_si_001.pdf

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cb300059z_si_001.pdf

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Additional details

Identifiers

Eprint ID
32339
DOI
10.1021/cb300059z
Resolver ID
CaltechAUTHORS:20120710-155247536

Related works

Describes
10.1021/cb300059z (DOI)

Funding

PharmSelex
Tri-Institutional Training Program in Chemical Biology

Dates

Created
2012-07-11
Created from EPrint's datestamp field
Updated
2021-11-09
Created from EPrint's last_modified field