G-Protein Coupled Receptor (GPCR)
GPCRA large family of seven-transmembrane domain receptors that transduce extracellular signals via heterotrimeric G proteins (Gs, Gi, Gq). GPCRs are the most common target class in drug discovery, with approximately 34% of all FDA-approved drugs acting on them. Signal transduction involves activation of second messengers such as cAMP, IP3, and DAG.
Examples
- Beta-2 adrenergic receptor targeted by salbutamol (asthma)
- Mu-opioid receptor targeted by morphine (pain)
- Histamine H1 receptor targeted by cetirizine (allergy)
Did You Know?
A large family of seven-transmembrane domain receptors that transduce extracellular signals via heterotrimeric G proteins (Gs, Gi, Gq). GPCRs are the most common target class in drug discovery, with approximately …