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

Grunbeck, Amy and Huber, Thomas and Abrol, Ravinder and Trzaskowski, Bartosz and Goddard, William A., III and Sakmar, Thomas P. (2012) Genetically Encoded Photo-cross-linkers Map the Binding Site of an Allosteric Drug on a G Protein-Coupled Receptor. ACS Chemical Biology, 7 (6). pp. 967-972. ISSN 1554-8929. doi:10.1021/cb300059z. https://resolver.caltech.edu/CaltechAUTHORS:20120710-155247536

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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.


Item Type:Article
Related URLs:
URLURL TypeDescription
http://dx.doi.org/10.1021/cb300059zDOIArticle
http://pubs.acs.org/doi/abs/10.1021/cb300059zPublisherArticle
ORCID:
AuthorORCID
Abrol, Ravinder0000-0001-7333-6793
Goddard, William A., III0000-0003-0097-5716
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.
Funders:
Funding AgencyGrant Number
PharmSelexUNSPECIFIED
Tri-Institutional Training Program in Chemical BiologyUNSPECIFIED
Issue or Number:6
DOI:10.1021/cb300059z
Record Number:CaltechAUTHORS:20120710-155247536
Persistent URL:https://resolver.caltech.edu/CaltechAUTHORS:20120710-155247536
Official Citation: Genetically Encoded Photo-cross-linkers Map the Binding Site of an Allosteric Drug on a G Protein-Coupled Receptor Amy Grunbeck, Thomas Huber, Ravinder Abrol, Bartosz Trzaskowski, William A. Goddard, III, and Thomas P. Sakmar ACS Chemical Biology 2012 7 (6), 967-972
Usage Policy:No commercial reproduction, distribution, display or performance rights in this work are provided.
ID Code:32339
Collection:CaltechAUTHORS
Deposited By: Ruth Sustaita
Deposited On:11 Jul 2012 18:06
Last Modified:09 Nov 2021 21:26

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