Person:
Khiar Fernández, Nora

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First Name
Nora
Last Name
Khiar Fernández
URI
https://hdl.handle.net/20.500.14352/80861
Affiliation
Universidad Complutense de Madrid
Faculty / Institute
Ciencias Químicas
Department
Química Orgánica
Area
Química Orgánica
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    Validation of the LPA2 receptor as new therapeutic target for the treatment spinal of cord injury
    (2023) Khiar Fernández, Nora; López Rodríguez, María Luz; Ortega Gutiérrez, Silvia; Vázquez Villa, María Del Henar
    Spinal cord injury (SCI) involves a permanent damage to the spinal cord which can lead into permanent neurological impairments that have an enormous impact in the quality of life of affected people. The pathology of SCI is multifaceted, complex, and yet to be fully understood. Once produced the primary injury responsible of the SCI, normally related with a traumatic impact or with the appearance of a tumor, infections or degenerative processes, the only pharmacological option is to treat the secondary damage and to limit the disruption of spinal connectivity. However, there is no effective clinical treatment for SCI, since current therapies are limited to surgical decompression and the administration of anti-inflammatory drugs. Hence, it is clear that new pharmacological approaches are needed to improve SCI patient condition. In this regard, inhibition of the type 2 lysophosphatidic acid (LPA2) receptor signaling has recently emerged as a new therapeutic option to limit the SCI associated damage. However, the validation of this approach has been limited by the lack of antagonists of the LPA2 receptor. In this regard, only one compound (Cpd35, Figure 1) has been characterized as a potent (IC50 value at LPA2 of 0.017 μM) and selective LPA2 antagonist (IC50 values >50 μM at LPA1 and LPA3 receptors)...