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Title

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

AuthorsMarchena, Miguel; Villarejo-Zori, Beatriz ; Zaldívar-Díez, Josefa; Palomo, Valle ; Gil, Carmen ; Hernández-Sánchez, Catalina ; Martínez, Ana ; De la Rosa, Enrique J.
KeywordsGSK-3 inhibitors
Retinal diseases
Retinitis pigmentosa
Glaucoma
Issue Date23-Jan-2017
PublisherTaylor & Francis
CitationJournal of Enzyme Inhibition and Medicinal Chemistry 32 (1) 522-526 (2017)
AbstractRetinitis 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.
Description6 p.-5 fig.
Publisher version (URL)http://dx.doi.org/10.1080/14756366.2016.1265522
URIhttp://hdl.handle.net/10261/145647
DOIhttp://dx.doi.org/10.1080/14756366.2016.1265522
ISSN1475-6366
E-ISSN1475-6374
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