2qpj

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[[Image:2qpj.jpg|left|200px]]
[[Image:2qpj.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2qpj |SIZE=350|CAPTION= <scene name='initialview01'>2qpj</scene>, resolution 2.05&Aring;
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The line below this paragraph, containing "STRUCTURE_2qpj", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=I20:(2S)-2-({(2S)-3-[(R)-[(1R)-1-({(4S)-4-AMINO-5-[(2S)-2-CYANOPYRROLIDIN-1-YL]-5-OXOPENTANOYL}AMINO)ETHYL](HYDROXY)PHOSPHORYL]-2-BENZYLPROPANOYL}AMINO)PROPANOIC+ACID'>I20</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Neprilysin Neprilysin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.24.11 3.4.24.11] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= MME, EPN ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_2qpj| PDB=2qpj | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2qpj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2qpj OCA], [http://www.ebi.ac.uk/pdbsum/2qpj PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2qpj RCSB]</span>
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}}
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'''Human NEP complexed with a bifunctional NEP/DPP IV inhibitor'''
'''Human NEP complexed with a bifunctional NEP/DPP IV inhibitor'''
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[[Category: Dale, G E.]]
[[Category: Dale, G E.]]
[[Category: Oefner, C.]]
[[Category: Oefner, C.]]
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[[Category: glycoprotein]]
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[[Category: Glycoprotein]]
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[[Category: hydrolase]]
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[[Category: Hydrolase]]
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[[Category: lt3_9]]
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[[Category: Lt3_9]]
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[[Category: membrane]]
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[[Category: Membrane]]
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[[Category: metal-binding]]
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[[Category: Metal-binding]]
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[[Category: signal-anchor]]
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[[Category: Signal-anchor]]
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[[Category: transmembrane]]
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[[Category: Transmembrane]]
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[[Category: zinc-dependent metalloprotease]]
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[[Category: Zinc-dependent metalloprotease]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 15:22:00 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:51:47 2008''
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Revision as of 12:22, 4 May 2008

Image:2qpj.jpg

Template:STRUCTURE 2qpj

Human NEP complexed with a bifunctional NEP/DPP IV inhibitor


Overview

Neutral endopeptidase (NEP) is the major enzyme involved in the metabolic inactivation of a number of bioactive peptides including the enkephalins, substance P, endothelin, bradykinin and atrial natriuretic factor, as well as the incretin hormone glucagon-like peptide 1 (GLP-1), which is a potent stimulator of insulin secretion. The activity of GLP-1 is also rapidly abolished by the serine protease dipeptidyl peptidase IV (DPP-IV), which led to an elevated interest in inhibitors of this enzyme for the treatment of type II diabetes. A dual NEP/DPP-IV inhibitor concept is proposed, offering an alternative strategy for the treatment of type 2 diabetes. Here, the synthesis and crystal structures of the soluble extracellular domain of human NEP (residues 52-749) complexed with the NEP, competitive and potent dual NEP/DPP-IV inhibitor MCB3937 are described.

About this Structure

2QPJ is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Structural studies of a bifunctional inhibitor of neprilysin and DPP-IV., Oefner C, Pierau S, Schulz H, Dale GE, Acta Crystallogr D Biol Crystallogr. 2007 Sep;63(Pt 9):975-81. Epub 2007, Aug 17. PMID:17704566 Page seeded by OCA on Sun May 4 15:22:00 2008

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OCA

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