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==Human renin in complex with inhibitor 7== | ==Human renin in complex with inhibitor 7== | ||
<StructureSection load='3vye' size='340' side='right' caption='[[3vye]], [[Resolution|resolution]] 2.70Å' scene=''> | <StructureSection load='3vye' size='340' side='right' caption='[[3vye]], [[Resolution|resolution]] 2.70Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[3vye]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/ | <table><tr><td colspan='2'>[[3vye]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3VYE OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3VYE FirstGlance]. <br> | ||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=VYE:(3S,5R)-5-[4-(2-CHLOROPHENYL)-2,2-DIMETHYL-5-OXOPIPERAZIN-1-YL]-N-(3-METHYLBUTYL)PIPERIDINE-3-CARBOXAMIDE'>VYE</scene></td></tr> | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=VYE:(3S,5R)-5-[4-(2-CHLOROPHENYL)-2,2-DIMETHYL-5-OXOPIPERAZIN-1-YL]-N-(3-METHYLBUTYL)PIPERIDINE-3-CARBOXAMIDE'>VYE</scene></td></tr> | ||
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[3vyd|3vyd]], [[3vyf|3vyf]]</td></tr> | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[3vyd|3vyd]], [[3vyf|3vyf]]</td></tr> | ||
<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">REN ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">REN ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr> | ||
<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Renin Renin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.23.15 3.4.23.15] </span></td></tr> | <tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Renin Renin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.23.15 3.4.23.15] </span></td></tr> | ||
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3vye FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3vye OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3vye RCSB], [http://www.ebi.ac.uk/pdbsum/3vye PDBsum]</span></td></tr> | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3vye FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3vye OCA], [http://pdbe.org/3vye PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=3vye RCSB], [http://www.ebi.ac.uk/pdbsum/3vye PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=3vye ProSAT]</span></td></tr> | ||
</table> | </table> | ||
== Disease == | == Disease == | ||
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
</div> | </div> | ||
<div class="pdbe-citations 3vye" style="background-color:#fffaf0;"></div> | |||
==See Also== | ==See Also== | ||
| Line 28: | Line 30: | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
[[Category: | [[Category: Human]] | ||
[[Category: Renin]] | [[Category: Renin]] | ||
[[Category: Hanzawa, H]] | [[Category: Hanzawa, H]] | ||
Revision as of 12:13, 5 August 2016
Human renin in complex with inhibitor 7Human renin in complex with inhibitor 7
Structural highlights
Disease[RENI_HUMAN] Defects in REN are a cause of renal tubular dysgenesis (RTD) [MIM: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).[1] Defects in REN are the cause of familial juvenile hyperuricemic nephropathy type 2 (HNFJ2) [MIM:613092]. It is a renal disease characterized by juvenile onset of hyperuricemia, slowly progressive renal failure and anemia.[2] Function[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. Publication Abstract from PubMedUtilizing X-ray crystal structure analysis, (3S,5R)-5-[4-(2-chlorophenyl)-2,2-dimethyl-5-oxopiperazin-1-yl]piperidine-3-carbo xamides were designed and identified as renin inhibitors. The most potent compound 15 demonstrated favorable pharmacokinetic and pharmacodynamic profiles in rat. Design and discovery of new (3S,5R)-5-[4-(2-chlorophenyl)-2,2-dimethyl-5-oxopiperazin-1-yl]piperidine-3-carbo xamides as potent renin inhibitors.,Mori Y, Ogawa Y, Mochizuki A, Nakamura Y, Sugita C, Miyazaki S, Tamaki K, Matsui Y, Takahashi M, Nagayama T, Nagai Y, Inoue S, Nishi T Bioorg Med Chem Lett. 2012 Dec 15;22(24):7677-82. doi:, 10.1016/j.bmcl.2012.09.103. Epub 2012 Oct 17. PMID:23122821[3] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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