RT Journal Article
T1 Chemoproteomic Approach to Explore the Target Profile of GPCR ligands: Application to 5-HT1A and 5-HT6 Receptors
A1 Gamo, Ana M.
A1 González Vera, Juan Antonio
A1 Rueda-Zubiaurre, Ainoa
A1 Alonso, Dulce
A1 Vázquez Villa, María Del Henar
A1 Martín-Couce, Lidia
A1 Palomares Gracia, Óscar
A1 López, Juan A.
A1 Martín-Fontecha Corrales, María Del Mar
A1 Benhamú Salama, Bellinda
A1 López-Rodríguez, María L.
A1 Ortega Gutiérrez, Silvia
AB 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.
PB Wiley
SN 1521-3765 (Online)
YR 2015
FD 2015
LK https://hdl.handle.net/20.500.14352/34961
UL https://hdl.handle.net/20.500.14352/34961
LA eng
NO Gamo, Ana M., Gónzalez-Vera, J. A., Rueda-Zubiaurre, A. et al. «Chemoproteomic Approach to Explore the Target Profile of GPCR Ligands: Application to 5‐HT 1A and 5‐HT 6 Receptors». Chemistry – A European Journal, vol. 22, n.o 4, enero de 2016, pp. 1313-21. DOI.org (Crossref), https://doi.org/10.1002/chem.201503101.
NO Ministerio de Economía, Comercio y Empresa (España)
NO Comunidad de Madrid
DS Docta Complutense
RD 6 oct 2024