G protein coupled-receptors (GPCRs) or seven-transmembrane receptors (7TMRs) are the most prevailing class of signaling transduction molecules in human organism, being activated by a diversity of ligands such as peptides, large proteins, lipids, small organic molecules, ions, and others. Classically, GPCRs transduce signals by means of heterotrimeric G proteins but more recently other mechanisms and signaling pathways have been reported. GPCRs are involved in plethora of pathophysiological processes and many drugs act by modulating GPCRs’ activities. It is estimated that ca. 40% of all drugs in the market act on GPCRs. In the last years key advances concerning to GPCRs’ structure, signaling properties, and evidences of their involvement in many pathophysiological events were achieved; which shall impact the development of next-generation drugs.
G protein coupled-receptors (GPCRs) or seven-transmembrane receptors (7TMRs) are the most prevailing class of signaling transduction molecules in human organism, being activated by a diversity of ligands such as peptides, large proteins, lipids, small organic molecules, ions, and others. Classically, GPCRs transduce signals by means of heterotrimeric G proteins but more recently other mechanisms and signaling pathways have been reported. GPCRs are involved in plethora of pathophysiological processes and many drugs act by modulating GPCRs’ activities. It is estimated that ca. 40% of all drugs in the market act on GPCRs. In the last years key advances concerning to GPCRs’ structure, signaling properties, and evidences of their involvement in many pathophysiological events were achieved; which shall impact the development of next-generation drugs.