Abstract
GPCRs are the largest family of human membrane proteins that play key roles in cellular signaling and serve as primary targets of ∼1/3 currently marketed drugs. Allosteric modulators are small molecules binding to topographically distant sites that are distinct from the primary agonist-binding (orthosteric) sites in GPCRs. They are able to selectively modulate the binding affinity and signaling of orthosteric ligands, including positive and negative allosteric modulators (PAMs and NAMs). However, it remains challenging to predict effects of allosteric modulators in GPCRs, for which the molecular determinants have been poorly understood.
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