What are the current trends in G protein-coupled receptor targeted drug discovery?

G protein-coupled receptors (GPCRs) constitute a superfamily of membrane proteins which have in common the presence of 7 transmembrane α-helices linked by several intra- and extracellular loops. This particular structure is important for extracellular stimulus recognition through the amino acids for...

Descripción completa

Detalles Bibliográficos
Autores: Casadó, Vicent, Casadó Anguera, Verònica
Tipo de recurso: artículo
Estado:Versión aceptada para publicación
Fecha de publicación:2023
País:España
Institución:Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)
Repositorio:Recercat. Dipósit de la Recerca de Catalunya
OAI Identifier:oai:recercat.cat:2445/225834
Acceso en línea:https://hdl.handle.net/2445/225834
Access Level:acceso abierto
Palabra clave:Proteïnes G
Enzims al·lostèrics
G Proteins
Allosteric enzymes
Descripción
Sumario:G protein-coupled receptors (GPCRs) constitute a superfamily of membrane proteins which have in common the presence of 7 transmembrane α-helices linked by several intra- and extracellular loops. This particular structure is important for extracellular stimulus recognition through the amino acids forming the extracellular loops (class B, C and F of GPCRs) or by the transmembrane α-helices (class A and B of GPCRs). Their structure is also essential for signal transduction via intracellular proteins (G proteins, arrestins and kinases – GRKs-) [Citation1]. These proteins are attached to the intracellular loops and/or to the intracellular regions of the α-helices of the GPCRs, even when they are not activated by extracellular ligands or drugs.