AI-driven innovations in GPCR ligand synthesis for treating inflammatory diseases
David F. Nippa, Julie Blaising · Open Access Government · 2025
AI-driven innovations in GPCR ligand synthesis for treating inflammatory diseases This article explores the significance of G Protein-Coupled Receptors (GPCRs) in therapeutic drug development and strategies for advancing GPCR-targeted therapies, including the use of agonists, antagonists, biased agonism, and allosteric modulators. G Protein-Coupled Receptors (GPCRs) are a large and diverse group of membrane proteins that play a crucial role in cellular communication and signal transduction. (1) Characterized by their seven transmembrane domains, GPCRs activate intracellular G proteins in response to extracellular signals such as hormones, neurotransmitters, and other signaling molecules. The GPCR superfamily consists of approximately 800 membrane proteins, sharing a common evolutionary origin and coupling primarily to intracellular transducers like G proteins and arrestins. These receptors are integral to complex signaling systems that modulate a wide array of physiological and pathophysiological processes. (2)