Por favor, use este identificador para citar o enlazar este Item:http://hdl.handle.net/20.500.12105/6638
Título
Chemoproteomic Approach to Explore the Target Profile of GPCR ligands: Application to 5-HT1A and 5-HT6 Receptors
Autor(es)
Fecha de publicación
2016-01-22
Cita
Chemistry. 2016; 22(4):1313-21
Idioma
Inglés
Tipo de documento
journal article
Resumen
Determination of the targets of a compound remains an essential aspect in drug discovery. A complete understanding of all binding interactions is critical to recognize in advance both therapeutic effects and undesired consequences. However, the complete polypharmacology of many drugs currently in clinical development is still unknown, especially in the case of G protein-coupled receptor (GPCR) ligands. In this work we have developed a chemoproteomic platform based on the use of chemical probes to explore the target profile of a compound in biological systems. As proof of concept, this methodology has been applied to selected ligands of the therapeutically relevant serotonin 5-HT1A and 5-HT6 receptors, and we have identified and validated some of their off-targets. This approach could be extended to other drugs of interest to study the targeted proteome in disease-relevant systems.
Palabras clave
MESH
Drug Design | Drug Discovery | Humans | Ligands | Receptor, Serotonin, 5-HT1A | Receptors, G-Protein-Coupled | Receptors, Serotonin
Versión en línea
DOI
Aparece en las colecciones