Allosteric Regulation of G-Protein-Coupled Receptors: From Diversity of Molecular Mechanisms to Multiple Allosteric Sites and Their Ligands

International Journal of Molecular Sciences, Journal Year: 2023, Volume and Issue: 24(7), P. 6187 - 6187

Published: March 24, 2023

Allosteric regulation is critical for the functioning of G protein-coupled receptors (GPCRs) and their signaling pathways. Endogenous allosteric regulators GPCRs are simple ions, various biomolecules, protein components GPCR (G proteins β-arrestins). The stability functional activity complexes also due to multicenter interactions between protomers. complexity effects caused by numerous differing in structure, availability, mechanisms action predetermines multiplicity different topology sites GPCRs. These can be localized extracellular loops; inside transmembrane tunnel its upper lower vestibules; cytoplasmic on outer, membrane-contacting surface domain. They involved basal orthosteric agonist-stimulated receptor activity, biased agonism, GPCR-complex formation, endocytosis. targets a large number synthetic modulators, including those constructed using molecular docking. review devoted principles regulation, topology, endogenous regulators, autoantibodies pepducins. chemokine receptors, proteinase-activated thyroid-stimulating luteinizing hormone beta-adrenergic described more detail.

Language: Английский

---

Allosteric Sites and Allosteric Regulators of G Protein-Coupled Receptors: Gray Cardinals of Signal Transduction

Journal of Evolutionary Biochemistry and Physiology, Journal Year: 2023, Volume and Issue: 59(S1), P. S1 - S106

Published: Dec. 1, 2023

Language: Английский

---

ALLOSTERIC SITES AND ALLOSTERIC REGULATORS OF G-PROTEIN-COUPLED RECEPTORS: GRAY CARDINALS OF SIGNAL TRANSDUCTION

Журнал эволюционной биохимии и физиологии, Journal Year: 2023, Volume and Issue: 59(7), P. 559 - 658

Published: Dec. 1, 2023

Language: Английский

---