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...
| Autores: | , |
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| Formato: | artículo |
| Estado: | Versión aceptada para publicación |
| Fecha de publicación: | 2023 |
| País: | España |
| Recursos: | 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 |
| Acesso em linha: | https://hdl.handle.net/2445/225834 |
| Access Level: | acceso abierto |
| Palavra-chave: | Proteïnes G Enzims al·lostèrics G Proteins Allosteric enzymes |
| Resumo: | 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. |
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