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User:Ivan E. Wang/Sandbox Reserved 895
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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=''> | <StructureSection load='4rsc' size='500' side='right' caption='Figure 1: Emixustat and palmitate bound in the active site of RPE65' scene=''> | ||
| - | Retinal pigment epithelium 65 (RPE65) also known as retinoid isomerohydrolase (IMH) is a 65 kDa enzyme located within the human retinal pigment epithelium (hRPE) cells. RPE65 is exclusively expressed within hRPE cells and is not expressed anywhere else within the body which makes RPE65 a useful drug target. | + | Retinal pigment epithelium 65 (RPE65) also known as retinoid isomerohydrolase (IMH) is a 65 kDa enzyme located within the human retinal pigment epithelium (hRPE) cells. RPE65 is exclusively expressed within hRPE cells and is not expressed anywhere else within the body which makes RPE65 a useful drug target. RPE65 is responsible for the chemical conversion of ''all-trans''-retinyl ester to ''11-cis''-retinol, the rate limiting step, in the canonical visual cycle. |
</StructureSection> | </StructureSection> | ||
Revision as of 21:54, 3 March 2020
Contents |
Introduction to the RPE65
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Structure and Activity
Classification and Structural Analysis of RPE65
Classification nomenclature for RPE65 is as follow according to <insert classification type>
Retinal pigment epithelium 65 (RPE65) resembles a 7-bladed propeller with two deep binding pockets that contains a lipophilic binding pocket (which binds to endogenous palmitoyl acid) as well as an charged iron(II) atom stabilized by 4 histidine residues (His180, His241, His313 and His527) which binds to the carboxylic acid functional group of endogenous palmitoyl acid.
Enzymatic Activity of RPE65
(PLACEHOLDER)
Protein-Ligand Interaction
Endogenous Ligand
(PLACEHOLDER)
Exogenous Ligand
(R)-Emixustat (ACU-4429)
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(S)-Emixustat
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R/S Enantiomers Differences
(PLACEHOLDER)
Disease Implications
(PLACEHOLDER)
Medical Relevance
Dry (atrophic) age related macular degeneration
Stargadt's Disease
This is a sample scene created with SAT to by Group, and another to make of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.
References
- ↑ Shin Y, Moiseyev G, Petrukhin K, Cioffi CL, Muthuraman P, Takahashi Y, Ma JX. A novel RPE65 inhibitor CU239 suppresses visual cycle and prevents retinal degeneration. Biochim Biophys Acta Mol Basis Dis. 2018 Jul;1864(7):2420-2429. doi:, 10.1016/j.bbadis.2018.04.014. Epub 2018 Apr 21. PMID:29684583 doi:http://dx.doi.org/10.1016/j.bbadis.2018.04.014
