gpcr conformations: implications for rational drug design

gpcr conformations: implications for rational drug design

;Abby L. Parrill;Debra L. Bautista
journal of cerebral blood flow and metabolism 2010 Vol. 4 pp. 7-43
270
parrill2010pharmaceuticalsgpcr

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.

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ID: 162009
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162009
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10.3390/ph4010007
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