Overview of receptor allosterism.

  title={Overview of receptor allosterism.},
  author={Karen J. Gregory and Patrick M. Sexton and Arthur Christopoulos},
  journal={Current protocols in pharmacology},
  volume={Chapter 1},
          Unit 1.21
In addition to the orthosteric site, which recognizes endogenous ligands, most G protein-coupled receptors (GPCRs) possess topographically distinct allosteric sites that can be recognized by small molecules and accessory cellular proteins. Ligand binding to allosteric sites promotes a conformational change in the GPCR that can alter orthosteric ligand affinity and/or efficacy. Moreover, there has been an increase in recent years in the identification of allosteric agonists that can directly… CONTINUE READING

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