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Pharmaceuticals 2011, 4(1), 7-43; doi:10.3390/ph4010007
Review

GPCR Conformations: Implications for Rational Drug Design

1,*  and 2
Received: 24 November 2010 / Revised: 20 December 2010 / Accepted: 21 December 2010 / Published: 23 December 2010
(This article belongs to the Special Issue GPCR Based Drug Discovery)
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Abstract

G protein-coupled receptors (GPCRs) comprise a large class of transmembrane proteins that play critical roles in both normal physiology and pathophysiology. These critical roles offer targets for therapeutic intervention, as exemplified by the substantial fraction of current pharmaceutical agents that target members of this family. Tremendous contributions to our understanding of GPCR structure and dynamics have come from both indirect and direct structural characterization techniques. Key features of GPCR conformations derived from both types of characterization techniques are reviewed.
Keywords: G protein-coupled receptor; GPCR; structure; crystallography; NMR; modeling G protein-coupled receptor; GPCR; structure; crystallography; NMR; modeling
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Parrill, A.L.; Bautista, D.L. GPCR Conformations: Implications for Rational Drug Design. Pharmaceuticals 2011, 4, 7-43.

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