2qpj: Difference between revisions

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[[Image:2qpj.jpg|left|200px]]
{{Seed}}
[[Image:2qpj.png|left|200px]]


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{{STRUCTURE_2qpj|  PDB=2qpj  |  SCENE=  }}  
{{STRUCTURE_2qpj|  PDB=2qpj  |  SCENE=  }}  


'''Human NEP complexed with a bifunctional NEP/DPP IV inhibitor'''
===Human NEP complexed with a bifunctional NEP/DPP IV inhibitor===




==Overview==
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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.
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{{ABSTRACT_PUBMED_17704566}}


==About this Structure==
==About this Structure==
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[[Category: Transmembrane]]
[[Category: Transmembrane]]
[[Category: Zinc-dependent metalloprotease]]
[[Category: Zinc-dependent metalloprotease]]
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May  4 15:22:00 2008''
 
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 12:49:19 2008''

Revision as of 09:49, 29 July 2008

File:2qpj.png

Template:STRUCTURE 2qpj

Human NEP complexed with a bifunctional NEP/DPP IV inhibitor

Template:ABSTRACT PUBMED 17704566

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

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