G-Protein-Coupled Receptor (GPCR)

G-Protein-Coupled Receptors (GPCRs) constitute a large family of cell surface receptors that transduce extracellular signals into intracellular responses through interaction with G proteins. These receptors regulate diverse physiological processes including neurotransmission, hormone signalling, immune responses, and sensory perception. GPCR activation triggers downstream signalling cascades influencing cellular behaviour and gene expression.

The pharmaceutical industry targets GPCRs extensively, as they represent one of the most druggable receptor families. A significant proportion of approved medicines modulate GPCR activity to treat cardiovascular, neurological, respiratory, and metabolic diseases. Drug development focuses on receptor selectivity, biased signalling, and allosteric modulation to improve efficacy and reduce side effects. Advances in structural biology and receptor pharmacology continue expanding GPCR-targeted therapeutic opportunities, with cryo-EM enabling atomic-resolution structures guiding rational drug design.