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2qpj

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[[Image:2qpj.jpg|left|200px]]<br /><applet load="2qpj" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:2qpj.jpg|left|200px]]
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caption="2qpj, resolution 2.05&Aring;" />
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'''Human NEP complexed with a bifunctional NEP/DPP IV inhibitor'''<br />
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{{Structure
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|PDB= 2qpj |SIZE=350|CAPTION= <scene name='initialview01'>2qpj</scene>, resolution 2.05&Aring;
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|SITE=
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|LIGAND= <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene> and <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>
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|ACTIVITY= [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]
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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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'''Human NEP complexed with a bifunctional NEP/DPP IV inhibitor'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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2QPJ is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=NAG:'>NAG</scene>, <scene name='pdbligand=ZN:'>ZN</scene> and <scene name='pdbligand=I20:'>I20</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [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] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2QPJ OCA].
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2QPJ is a [[Single protein]] structure of 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=2QPJ OCA].
==Reference==
==Reference==
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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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=17704566 17704566]
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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:[http://www.ncbi.nlm.nih.gov/pubmed/17704566 17704566]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Neprilysin]]
[[Category: Neprilysin]]
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[[Category: zinc-dependent metalloprotease]]
[[Category: zinc-dependent metalloprotease]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:41:10 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 18:28:10 2008''

Revision as of 16:28, 20 March 2008

Image:2qpj.jpg


PDB ID 2qpj

Drag the structure with the mouse to rotate
, resolution 2.05Å
Ligands: , and
Gene: MME, EPN (Homo sapiens)
Activity: Neprilysin, with EC number 3.4.24.11
Coordinates: save as pdb, mmCIF, xml



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 Thu Mar 20 18:28:10 2008

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