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April 15, 2011 (Vol. 31, No. 8)

Refining GPCR Discovery Approaches

Emerging Platforms Afford Timelines More Comparable to Those for Soluble Targets

  • GPCRs constitute the largest class of known targets in commercial drug discovery today—collectively the targets of at least 30% of currently marketed drugs. Yet, as heptahelical transmembrane proteins involved in divergent and manifold signaling pathways, they can confound conventional drug discovery techniques. The recent “Congress on G Protein-Coupled ...

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