2026-06-05T18:42:52Zhttps://docta.ucm.es/rest/oai/requestoai:docta.ucm.es:20.500.14352/719032024-10-03T15:58:32Zcom_20.500.14352_14col_20.500.14352_15
Docta Complutense
author
Khiar Fernández, Nora
author
Zian, Debora
author
Vázquez Villa, María Del Henar
author
Martínez, R. Fernando
author
Escobar Peña, Ana Andrea
author
Foronda Sainz, Román
author
Ray, Manisha
author
Puigdomenech Poch, Maria
author
Cincilla, Giovanni
author
Sánchez Martínez, Melchor
author
Kihara, Yasuyuki
author
Chun, Jerold
author
López Vales, Rubèn
author
López Rodríguez, María Luz
author
Ortega Gutiérrez, Silvia
2023-06-22T10:55:53Z
2023-06-22T10:55:53Z
2022-08-10
0022-2623
10.1021/acs.jmedchem.2c00046
https://hdl.handle.net/20.500.14352/71903
https://doi.org/10.1021/acs.jmedchem.2c00046
Spinal cord injuries (SCIs) irreversibly disrupt spinal connectivity, leading to permanent neurological disabilities. Current medical treatments for reducing the secondary damage that follows the initial injury are limited to surgical decompression and anti-inflammatory drugs, so there is a pressing need for new therapeutic strategies. Inhibition of the type 2 lysophosphatidic acid receptor (LPA2) has recently emerged as a new potential pharmacological approach to decrease SCIassociated damage. Toward validating this receptor as a target in SCI, we have developed a new series of LPA2 antagonists, among which compound 54 (UCM14216) stands out as a potent and selective LPA2 receptor antagonist (Emax = 90%, IC50 = 1.9 μM, KD = 1.3 nM; inactive at LPA1,3−6 receptors). This compound shows efficacy in an in vivo mouse model of SCI in an LPA2-dependent manner, confirming the potential of LPA2 inhibition for providing a new alternative for treating SCI.
eng
Atribución 3.0 España
Novel Antagonist of the Type 2 Lysophosphatidic Acid Receptor (LPA2), UCM-14216, Ameliorates Spinal Cord Injury in Mice
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