G-Protein Coupled Receptor (GPCR)

GPCR
Targets & Receptors

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 34% of all FDA-approved drugs acting on them. Signal transduction involves activation of second messengers such as cAMP, IP3, and DAG.

Примеры

  • Beta-2 adrenergic receptor targeted by salbutamol (asthma)
  • Mu-opioid receptor targeted by morphine (pain)
  • Histamine H1 receptor targeted by cetirizine (allergy)

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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 …