3vsx

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[[Image:3vsx.png|left|200px]]
 
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{{STRUCTURE_3vsx| PDB=3vsx | SCENE= }}
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==Human renin in complex with compound 18==
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<StructureSection load='3vsx' size='340' side='right'caption='[[3vsx]], [[Resolution|resolution]] 2.80&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[3vsx]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3VSX OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3VSX FirstGlance]. <br>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.8&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=R32:(2S,4S,5S)-5-AMINO-N-(3-AMINO-2,2-DIMETHYL-3-OXOPROPYL)-6-[4-(2-CHLOROPHENYL)-2,2-DIMETHYL-5-OXOPIPERAZIN-1-YL]-4-HYDROXY-2-(PROPAN-2-YL)HEXANAMIDE'>R32</scene></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=3vsx FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3vsx OCA], [https://pdbe.org/3vsx PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3vsx RCSB], [https://www.ebi.ac.uk/pdbsum/3vsx PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3vsx ProSAT]</span></td></tr>
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</table>
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== Disease ==
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[https://www.uniprot.org/uniprot/RENI_HUMAN RENI_HUMAN] Defects in REN are a cause of renal tubular dysgenesis (RTD) [MIM:[https://omim.org/entry/267430 267430]. RTD is an autosomal recessive severe disorder of renal tubular development characterized by persistent fetal anuria and perinatal death, probably due to pulmonary hypoplasia from early-onset oligohydramnios (the Potter phenotype).<ref>PMID:16116425</ref> Defects in REN are the cause of familial juvenile hyperuricemic nephropathy type 2 (HNFJ2) [MIM:[https://omim.org/entry/613092 613092]. It is a renal disease characterized by juvenile onset of hyperuricemia, slowly progressive renal failure and anemia.<ref>PMID:19664745</ref>
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== Function ==
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[https://www.uniprot.org/uniprot/RENI_HUMAN RENI_HUMAN] Renin is a highly specific endopeptidase, whose only known function is to generate angiotensin I from angiotensinogen in the plasma, initiating a cascade of reactions that produce an elevation of blood pressure and increased sodium retention by the kidney.
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Introduction of the 2,2-dimethyl-4-phenylpiperazin-5-one scaffold into the P(3)-P(1) portion of the (2S,4S,5S)-5-amino-6-dialkylamino-4-hydroxy-2-isopropylhexanamide backbone dramatically increased the renin inhibitory activity without using the interaction to the S(3)(sp) pocket. Compound 31 exhibited &gt;10,000-fold selectivity over other human proteases, and 18.5% oral bioavailability in monkey.
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===Human renin in complex with compound 18===
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Design and optimization of novel (2S,4S,5S)-5-amino-6-(2,2-dimethyl-5-oxo-4-phenylpiperazin-1-yl)-4-hydroxy-2-isop ropylhexanamides as renin inhibitors.,Nakamura Y, Sugita C, Meguro M, Miyazaki S, Tamaki K, Takahashi M, Nagai Y, Nagayama T, Kato M, Suemune H, Nishi T Bioorg Med Chem Lett. 2012 Jul 15;22(14):4561-6. Epub 2012 Jun 4. PMID:22726934<ref>PMID:22726934</ref>
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{{ABSTRACT_PUBMED_22726934}}
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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==About this Structure==
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<div class="pdbe-citations 3vsx" style="background-color:#fffaf0;"></div>
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[[3vsx]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3VSX OCA].
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==See Also==
==See Also==
*[[Renin|Renin]]
*[[Renin|Renin]]
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== References ==
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==Reference==
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<references/>
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<ref group="xtra">PMID:022726934</ref><references group="xtra"/>
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__TOC__
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</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Renin]]
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[[Category: Large Structures]]
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[[Category: Hanzawa, H.]]
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[[Category: Hanzawa H]]
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[[Category: Takahashi, M.]]
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[[Category: Takahashi M]]
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[[Category: Aspartyl protease]]
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[[Category: Hydrolase-hydrolase inhibitor complex]]
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[[Category: Hypertension]]
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[[Category: Inhibitor]]
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[[Category: Ra]]
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Current revision

Human renin in complex with compound 18

PDB ID 3vsx

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