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Retinal Pigment Epithelium 65 (Retinoid Isomerohydrolase) complex with (R/S)-emixustat and palmitate

spinqualitylabelsall models Emixustat bound in the active site of RPE65 Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image Retinal pigment epithelium 65 (RPE65) also known as retinoid isomerohydrolase is a 65 kDa enzyme located within the human retinal pigment epithelium cells responsible for the chemical conversion of all-trans-retinyl ester to 11-cis-retinol in the visual cycle.

(PLACEHOLDER This is a default text for your page Ivan E. Wang/Sandbox 1. Click above on edit this page to modify. Be careful with the < and > signs. You may include any references to papers as in: the use of JSmol in Proteopedia ^[1] or to the article describing Jmol ^[2] to the rescue.)

Contents 1 Function 1.1 Structural Features of RPE65 1.2 Enzymatic Catalyzed Reaction 2 Protein-Ligand Interaction 2.1 Endogenous Ligand 2.2 Exogenous Ligand 2.3 R/S Enantiomers Differences 3 Disease Implications 4 Medical Relevance 5 References

Function

Structural Features of RPE65

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Enzymatic Catalyzed Reaction

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Protein-Ligand Interaction

Endogenous Ligand

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Exogenous Ligand

spinqualitylabelsall models PDB ID 4ryy Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image (R)-Emixustat (ACU-4429) (R)-emixustat (ACU-4429) is an investigational small molecule inhibitor of RPE65 first invented by a British-American chemist, Ian L. Scott. Formulated as an hydrochloride salt, (R)-emixustat hydrochloride is taken by mouth and functions as a visual cycle modulator (VCM) to reduce toxic retinal byproducts such as A2E. In 2008, Acucela Inc. partnered with Otsuka Pharmaceutical Company for the continued development of (R)-emixustat as a potential inhibitor of RPE65. Currently (R)-emixustat is in Phase III clinical trials in the United States for the potential treatment of Stargard's disease, a juvenile form of atrophic (dry) age dependent macular degeneration (AMD). Additionally, (R)-emixustat is investigated as potential therapy for diabetic retinopathy and diabetic macular edema.

spinqualitylabelsall models PDB ID 4ryz Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image (S)-Emixustat (PLACEHOLDER)

R/S Enantiomers Differences

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Disease Implications

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Medical Relevance

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References

1. ↑ Hanson, R. M., Prilusky, J., Renjian, Z., Nakane, T. and Sussman, J. L. (2013), JSmol and the Next-Generation Web-Based Representation of 3D Molecular Structure as Applied to Proteopedia. Isr. J. Chem., 53:207-216. doi:http://dx.doi.org/10.1002/ijch.201300024
2. ↑ Herraez A. Biomolecules in the computer: Jmol to the rescue. Biochem Mol Biol Educ. 2006 Jul;34(4):255-61. doi: 10.1002/bmb.2006.494034042644. PMID:21638687 doi:10.1002/bmb.2006.494034042644