New paradigms in GPCR drug discovery.

  title={New paradigms in GPCR drug discovery.},
  author={Kenneth A. Jacobson},
  journal={Biochemical pharmacology},
  volume={98 4},
G protein-coupled receptors (GPCRs) remain a major domain of pharmaceutical discovery. The identification of GPCR lead compounds and their optimization are now structure-based, thanks to advances in X-ray crystallography, molecular modeling, protein engineering and biophysical techniques. In silico screening provides useful hit molecules. New pharmacological approaches to tuning the pleotropic action of GPCRs include: allosteric modulators, biased ligands, GPCR heterodimer-targeted compounds… CONTINUE READING
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