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Título

Small molecules targeting glycogen synthase kinase 3 as potential drug candidates for the treatment of retinitis pigmentosa

AutorMarchena, Miguel CSIC; Villarejo-Zori, Beatriz CSIC ORCID ; Zaldívar-Díez, Josefa CSIC ORCID; Palomo, Valle CSIC ORCID ; Gil, Carmen CSIC ORCID ; Hernández-Sánchez, Catalina ; Martínez Gil, Ana CSIC ORCID ; De la Rosa, Enrique J. CSIC ORCID
Palabras claveGSK-3 inhibitors
Retinal diseases
Retinitis pigmentosa
Glaucoma
Fecha de publicación23-ene-2017
EditorTaylor & Francis
CitaciónJournal of Enzyme Inhibition and Medicinal Chemistry 32 (1) 522-526 (2017)
ResumenRetinitis pigmentosa (RP) is an inherited retinal dystrophy that courses with progressive degeneration of retinal tissue and loss of vision. Currently, RP is an unpreventable, incurable condition. We propose glycogen synthase kinase 3 (GSK-3) inhibitors as potential leads for retinal cell neuroprotection, since the retina is also a part of the central nervous system and GSK-3 inhibitors are potent neuroprotectant agents. Using a chemical genetic approach, diverse small molecules with different potency and binding mode to GSK-3 have been used to validate and confirm GSK-3 as a pharmacological target for RP. Moreover, this medicinal chemistry approach has provided new leads for the future disease-modifying treatment of RP.
Descripción6 p.-5 fig.
Versión del editorhttp://dx.doi.org/10.1080/14756366.2016.1265522
URIhttp://hdl.handle.net/10261/145647
DOI10.1080/14756366.2016.1265522
ISSN1475-6366
E-ISSN1475-6374
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