RT Journal Article
T1 Novel Antagonist of the Type 2 Lysophosphatidic Acid Receptor (LPA2), UCM-14216, Ameliorates Spinal Cord Injury in Mice
A1 Khiar Fernández, Nora
A1 Zian, Debora
A1 Vázquez Villa, María Del Henar
A1 Martínez, R. Fernando
A1 Escobar Peña, Ana Andrea
A1 Foronda Sainz, Román
A1 Ray, Manisha
A1 Puigdomenech Poch, Maria
A1 Cincilla, Giovanni
A1 Sánchez Martínez, Melchor
A1 Kihara, Yasuyuki
A1 Chun, Jerold
A1 López Vales, Rubèn
A1 López Rodríguez, María Luz
A1 Ortega Gutiérrez, Silvia
AB 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.
PB ACS Publications
SN 0022-2623
YR 2022
FD 2022-08-10
LK https://hdl.handle.net/20.500.14352/71903
UL https://hdl.handle.net/20.500.14352/71903
LA eng
NO CRUE-CSIC (Acuerdos Transformativos 2022)
NO Ministerio de Ciencia e Innovación (MICINN)
DS Docta Complutense
RD 13 abr 2025