HOMEPRODUCTSCOMPANYCONTACTFAQResearchDictionaryPharmaSign Up FREE or Login

Development of chiral fluorinated alkyl derivatives of emixustat as drug candidates for the treatment of retinal degenerative diseases.

Abstract
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.
AuthorsEliav Blum, Jianye Zhang, Edward Korshin, Krzysztof Palczewski, Arie Gruzman
JournalBioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 30 Issue 18 Pg. 127421 (09 15 2020) ISSN: 1464-3405 [Electronic] England
PMID32717613 (Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2020 Elsevier Ltd. All rights reserved.
Chemical References
  • Alkanes
  • Enzyme Inhibitors
  • Pharmaceutical Preparations
  • Phenyl Ethers
  • Propanolamines
  • retinal dimer
  • emixustat
  • retinoid isomerohydrolase
  • cis-trans-Isomerases
  • Retinaldehyde
Topics
  • Alkanes (chemistry)
  • Enzyme Inhibitors (chemical synthesis, pharmacology)
  • Halogenation
  • Humans
  • Isomerism
  • Models, Molecular
  • Molecular Conformation
  • Pharmaceutical Preparations (chemical synthesis)
  • Phenyl Ethers (chemical synthesis, pharmacology)
  • Propanolamines (chemical synthesis, pharmacology)
  • Retina (metabolism)
  • Retinal Degeneration (drug therapy)
  • Retinaldehyde (analogs & derivatives, metabolism)
  • Structure-Activity Relationship
  • cis-trans-Isomerases (antagonists & inhibitors)

Join CureHunter, for free Research Interface BASIC access!

Take advantage of free CureHunter research engine access to explore the best drug and treatment options for any disease. Find out why thousands of doctors, pharma researchers and patient activists around the world use CureHunter every day.
Realize the full power of the drug-disease research graph!


Choose Username:
Email:
Password:
Verify Password:
Enter Code Shown: