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Development of chiral fluorinated alkyl derivatives of emixustat as drug candidates for the treatment of retinal degenerative diseases.
Blum, Eliav; Zhang, Jianye; Korshin, Edward; Palczewski, Krzysztof; Gruzman, Arie.
Afiliação
  • Blum E; Department of Chemistry, Faculty of Exact Sciences, Bar-Ilan University, Ramat-Gan 5290002, Israel.
  • Zhang J; Gavin Herbert Eye Institute, Department of Ophthalmology, University of California, Irvine, CA 92697, USA.
  • Korshin E; Department of Chemistry, Faculty of Exact Sciences, Bar-Ilan University, Ramat-Gan 5290002, Israel.
  • Palczewski K; Gavin Herbert Eye Institute, Department of Ophthalmology, University of California, Irvine, CA 92697, USA; Departments of Physiology and Biophysics, and Chemistry, University of California, Irvine, CA 92697, USA.
  • Gruzman A; Department of Chemistry, Faculty of Exact Sciences, Bar-Ilan University, Ramat-Gan 5290002, Israel. Electronic address: gruzmaa@biu.ac.il.
Bioorg Med Chem Lett ; 30(18): 127421, 2020 09 15.
Article em En | MEDLINE | ID: mdl-32717613
The discovery of how a photon is converted into a chemical signal is one of the most important achievements in the field of vision. A key molecule in this process is the visual chromophore retinal. Several eye diseases are attributed to the abnormal metabolism of retinal in the retina and the retinal pigment epithelium. Also, the accumulation of two toxic retinal derivatives, N-retinylidene-N-retinylethanolamine and the retinal dimer, can damage the retina leading to blindness. RPE65 (Retinal pigment epithelium-specific 65 kDa protein) is one of the central enzymes that regulates the metabolism of retinal and the formation of its toxic metabolites. Its inhibition might decrease the rate of the retina's degeneration by limiting the amount of retinal and its toxic byproducts. Two RPE65 inhibitors, (R)-emixustat and (R)-MB001, were recently developed for this purpose.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Éteres Fenílicos / Propanolaminas / Degeneração Retiniana / Cis-trans-Isomerases / Inibidores Enzimáticos Idioma: En Ano de publicação: 2020 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Éteres Fenílicos / Propanolaminas / Degeneração Retiniana / Cis-trans-Isomerases / Inibidores Enzimáticos Idioma: En Ano de publicação: 2020 Tipo de documento: Article