5sy2: Difference between revisions
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==Structure-based design of a new series of N-piperidin-3-ylpyrimidine-5-carboxamides as renin inhibitors== | ==Structure-based design of a new series of N-piperidin-3-ylpyrimidine-5-carboxamides as renin inhibitors== | ||
<StructureSection load='5sy2' size='340' side='right' caption='[[5sy2]], [[Resolution|resolution]] 2.25Å' scene=''> | <StructureSection load='5sy2' size='340' side='right'caption='[[5sy2]], [[Resolution|resolution]] 2.25Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[5sy2]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5SY2 OCA]. For a <b>guided tour on the structure components</b> use [ | <table><tr><td colspan='2'>[[5sy2]] 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=5SY2 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5SY2 FirstGlance]. <br> | ||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=1PE:PENTAETHYLENE+GLYCOL'>1PE</scene>, <scene name='pdbligand=74V:N-ETHYL-4-{[(FURAN-2-YL)METHYL]AMINO}-2-METHYL-N-[(3S)-PIPERIDIN-3-YL]PYRIMIDINE-5-CARBOXAMIDE'>74V</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=PGE:TRIETHYLENE+GLYCOL'>PGE</scene | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.25Å</td></tr> | ||
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=1PE:PENTAETHYLENE+GLYCOL'>1PE</scene>, <scene name='pdbligand=74V:N-ETHYL-4-{[(FURAN-2-YL)METHYL]AMINO}-2-METHYL-N-[(3S)-PIPERIDIN-3-YL]PYRIMIDINE-5-CARBOXAMIDE'>74V</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=PGE:TRIETHYLENE+GLYCOL'>PGE</scene></td></tr> | |||
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=5sy2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5sy2 OCA], [https://pdbe.org/5sy2 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5sy2 RCSB], [https://www.ebi.ac.uk/pdbsum/5sy2 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5sy2 ProSAT]</span></td></tr> | |||
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[ | |||
</table> | </table> | ||
== Disease == | == Disease == | ||
[ | [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> | ||
== Function == | == Function == | ||
[ | [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. | ||
<div style="background-color:#fffaf0;"> | <div style="background-color:#fffaf0;"> | ||
== Publication Abstract from PubMed == | == Publication Abstract from PubMed == | ||
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</div> | </div> | ||
<div class="pdbe-citations 5sy2" style="background-color:#fffaf0;"></div> | <div class="pdbe-citations 5sy2" style="background-color:#fffaf0;"></div> | ||
==See Also== | |||
*[[Renin|Renin]] | |||
== References == | == References == | ||
<references/> | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
[[Category: | [[Category: Homo sapiens]] | ||
[[Category: Behnke | [[Category: Large Structures]] | ||
[[Category: Hideyuki | [[Category: Behnke CA]] | ||
[[Category: Lane | [[Category: Hideyuki O]] | ||
[[Category: Okada | [[Category: Lane W]] | ||
[[Category: Sang | [[Category: Okada K]] | ||
[[Category: Snell | [[Category: Sang BC]] | ||
[[Category: Snell GP]] | |||