2026-06-14T03:33:00Zhttps://repisalud.isciii.es/rest/oai/requestoai:repisalud.isciii.es:20.500.12105/66382024-09-27T10:12:21Zcom_20.500.12105_19604com_20.500.12105_2051col_20.500.12105_19607
Repisalud
author
Gamo, Ana M
author
González-Vera, Juan A
author
Rueda-Zubiaurre, Ainoa
author
Alonso, Dulce
author
Vázquez-Villa, Henar
author
Martín-Couce, Lidia
author
Palomares, Óscar
author
Lopez, Juan Antonio
author
Martín-Fontecha, Mar
author
Benhamú, Bellinda
author
López-Rodríguez, María L
author
Ortega-Gutiérrez, Silvia
funder
Ministerio de Economía y Competitividad (España)
funder
Comunidad de Madrid (España)
funder
Complutense University of Madrid (España)
funder
Unión Europea. Fondo Europeo de Desarrollo Regional (FEDER/ERDF)
funder
Fundación ProCNIC
2018-11-20T10:52:36Z
2018-11-20T10:52:36Z
2016-01-22
Chemistry. 2016; 22(4):1313-21
10.1002/chem.201503101
1521-3765
0947-6539
Chemistry - A European Journal
26560738
http://hdl.handle.net/20.500.12105/6638
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.
eng
GPCRS
chemical probes
drug discovery
selectivity profiling
serotonin receptors
Chemoproteomic Approach to Explore the Target Profile of GPCR ligands: Application to 5-HT1A and 5-HT6 Receptors
journal article
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