< User:Ivan E. Wang(Difference between revisions)
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| - | = Introduction to the RPE65 = | + | [[Media:RPE65_with_emixustat.mp4|PLACEHOLDER] width="576" height="324"] |
| | + | [[/Media:RPE65_with_emixustat.mp4]] |
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| - | <StructureSection load='4rsc' size='500' side='right' caption='Figure 1: Emixustat and palmitate bound in the active site of RPE65' scene=''> | |
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| - | Retinal pigment epithelium 65 (RPE65) also known as retinoid isomerohydrolase is a 65 kDa enzyme located within the human retinal pigment epithelium cells. PRE65 is responsible for the chemical conversion of ''all-trans''-retinyl ester to ''11-cis''-retinol in the visual cycle. | |
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| - | </StructureSection>
| + | [[Media:RPE65_with_emixustat.mp4|PLACEHOLDER]] |
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| - | = Function = | |
| - | == Structural Features of RPE65 == | |
| - | (PLACEHOLDER) | |
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| - | == Enzymatic Catalyzed Reaction ==
| + | [[Media:RPE65_with_emixustat.mp4]] |
| - | (PLACEHOLDER)
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| - | [[Image:Visual Cycle.jpg|thumb|right|512 px|alt=Figure 2: Human Visual Cycle| Figure 2: The canonical Visual Cycle in Humans <ref>DOI 10.1016/j.bbadis.2018.04.014</ref>]] | + | |
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| - | = Protein-Ligand Interaction =
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| - | == Endogenous Ligand ==
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| - | (PLACEHOLDER)
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| - | == Exogenous Ligand ==
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| - | <StructureSection load='4ryy' size='340' side='right' caption='Figure 3:(R)-emixustat and palmitate bound in the active site of RPE65' scene=''>
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| - | === (''R'')-Emixustat (ACU-4429) ===
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| - | (''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.
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| - | 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.
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| - | </StructureSection>
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| - | <StructureSection load='4ryz' size='340' side='right' caption='Figure 4:(S)-emixustat and palmitate bound in the active site of RPE65' scene=''>
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| - | === (''S'')-Emixustat ===
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| - | (PLACEHOLDER)
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| - | </StructureSection>
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| - | == ''R/S'' Enantiomers Differences ==
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| - | (PLACEHOLDER)
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| - | = Disease Implications =
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| - | (PLACEHOLDER)
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| - | = Medical Relevance =
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| - | (PLACEHOLDER)
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| - | This is a sample scene created with SAT to <scene name="/12/3456/Sample/1">color</scene> by Group, and another to make <scene name="/12/3456/Sample/2">a transparent representation</scene> of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.
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| - | = References =
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| - | <references/>
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