2yb9
From Proteopedia
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(New page: '''Unreleased structure''' The entry 2yb9 is ON HOLD Authors: Glossop, M.S., Bazin, R., Dack, K.N., Done, S., Fox, D.N.A., MacDonald, G.A., Mills, M., Owen, D.R., Phillips, C., Reeves, ...) |
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| - | '''Unreleased structure''' | ||
| - | + | ==Crystal Structure of Human Neutral Endopeptidase complexed with a heteroarylalanine diacid.== | |
| + | <StructureSection load='2yb9' size='340' side='right'caption='[[2yb9]], [[Resolution|resolution]] 2.40Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[2yb9]] is a 1 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=2YB9 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2YB9 FirstGlance]. <br> | ||
| + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.4Å</td></tr> | ||
| + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=HA0:HETEROARYLALANINE+5-PHENYL+OXAZOLE'>HA0</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</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=2yb9 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2yb9 OCA], [https://pdbe.org/2yb9 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2yb9 RCSB], [https://www.ebi.ac.uk/pdbsum/2yb9 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2yb9 ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | == Function == | ||
| + | [https://www.uniprot.org/uniprot/NEP_HUMAN NEP_HUMAN] Thermolysin-like specificity, but is almost confined on acting on polypeptides of up to 30 amino acids. Biologically important in the destruction of opioid peptides such as Met- and Leu-enkephalins by cleavage of a Gly-Phe bond. Able to cleave angiotensin-1, angiotensin-2 and angiotensin 1-9. Involved in the degradation of atrial natriuretic factor (ANF). Displays UV-inducible elastase activity toward skin preelastic and elastic fibers.<ref>PMID:2531377</ref> <ref>PMID:15283675</ref> <ref>PMID:20876573</ref> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Heteroarylalanine derivatives 4 were designed as potential inhibitors of neutral endopeptidase (NEP EC 3.4.24.11). Selectivity over other zinc metalloproteinases was explored through occupation of the S2' subsite within NEP. Structural optimisation led to the identification of 5-phenyl oxazole 4f, a potent and selective NEP inhibitor. A crystal structure of the inhibitor bound complex is reported. | ||
| - | + | Synthesis and evaluation of heteroarylalanine diacids as potent and selective neutral endopeptidase inhibitors.,Glossop MS, Bazin RJ, Dack KN, Fox DN, Macdonald GA, Mills M, Owen DR, Phillips C, Reeves KA, Ringer TJ, Strang RS, Watson CA Bioorg Med Chem Lett. 2011 Jun 1;21(11):3404-6. Epub 2011 Apr 5. PMID:21515054<ref>PMID:21515054</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| + | </div> | ||
| + | <div class="pdbe-citations 2yb9" style="background-color:#fffaf0;"></div> | ||
| + | |||
| + | ==See Also== | ||
| + | *[[Neprilysin|Neprilysin]] | ||
| + | == References == | ||
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Homo sapiens]] | ||
| + | [[Category: Large Structures]] | ||
| + | [[Category: Bazin RJ]] | ||
| + | [[Category: Dack KN]] | ||
| + | [[Category: Done S]] | ||
| + | [[Category: Fox DNA]] | ||
| + | [[Category: Glossop MS]] | ||
| + | [[Category: MacDonald GA]] | ||
| + | [[Category: Mills M]] | ||
| + | [[Category: Owen DR]] | ||
| + | [[Category: Phillips C]] | ||
| + | [[Category: Reeves KA]] | ||
| + | [[Category: Ringer TJ]] | ||
| + | [[Category: Strang RS]] | ||
| + | [[Category: Watson CAL]] | ||
Current revision
Crystal Structure of Human Neutral Endopeptidase complexed with a heteroarylalanine diacid.
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Categories: Homo sapiens | Large Structures | Bazin RJ | Dack KN | Done S | Fox DNA | Glossop MS | MacDonald GA | Mills M | Owen DR | Phillips C | Reeves KA | Ringer TJ | Strang RS | Watson CAL
