2026-06-14T03:39:15Zhttps://repisalud.isciii.es/rest/oai/request

oai:repisalud.isciii.es:20.500.12105/66382024-09-27T10:12:21Zcom_20.500.12105_19604com_20.500.12105_2051col_20.500.12105_19607

00925njm 22002777a 4500 dc 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 author 2016-01-22 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. 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 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