Activation Pathways of Agonists, Partial Agonists & Inverse Agonist in a G-Protein Coupled Receptor

Modulation of cell signaling by ligands of different efficacies via G-protein coupled receptors (GPCRs), depends intrinsically on the effect of the ligand on the dynamics between the multiple conformational states of these proteins. Ligands with different efficacies can remodel the energy landscape of the receptors, thereby perturbing this conformational equilibrium in many ways depending on the nature of the ligand, and the G-proteins that the receptor couples to, thereby conferring functional specificity. Understanding activation dynamics and pathways is vital in designing functionally specific drugs for GPCRs.