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Título: | Small molecules targeting glycogen synthase kinase 3 as potential drug candidates for the treatment of retinitis pigmentosa |
Autor: | Marchena, 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 clave: | GSK-3 inhibitors Retinal diseases Retinitis pigmentosa Glaucoma |
Fecha de publicación: | 23-ene-2017 | Editor: | Taylor & Francis | Citación: | Journal of Enzyme Inhibition and Medicinal Chemistry 32 (1) 522-526 (2017) | Resumen: | Retinitis 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. | Descripción: | 6 p.-5 fig. | Versión del editor: | http://dx.doi.org/10.1080/14756366.2016.1265522 | URI: | http://hdl.handle.net/10261/145647 | DOI: | 10.1080/14756366.2016.1265522 | ISSN: | 1475-6366 | E-ISSN: | 1475-6374 |
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J.Enz. Inhibit. Med. Chem. 2017.pdf | Artículo principal | 1,13 MB | Adobe PDF | Visualizar/Abrir |
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