Allosteric Modulation of G Protein-Coupled Receptors: An Emerging Approach of Drug Discovery.

Allosteric modulation of G protein-coupled receptors (GPCRs) confers several significant advantages over the traditional targeting of orthosteric sites. While the field of allosteric modulation of GPCRs as we now know it will benefit from continued investigation, the explosion of interest has led to a more in-depth understanding as to precisely how allosteric modulators may usher in a new paradigm for drug discovery.