2qpj: Difference between revisions
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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.]] | ||
[[Category: | [[Category: Glycoprotein]] | ||
[[Category: | [[Category: Hydrolase]] | ||
[[Category: | [[Category: Lt3_9]] | ||
[[Category: | [[Category: Membrane]] | ||
[[Category: | [[Category: Metal-binding]] | ||
[[Category: | [[Category: Signal-anchor]] | ||
[[Category: | [[Category: Transmembrane]] | ||
[[Category: | [[Category: Zinc-dependent metalloprotease]] | ||
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Revision as of 12:22, 4 May 2008
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
