2qpj
From Proteopedia
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|PDB= 2qpj |SIZE=350|CAPTION= <scene name='initialview01'>2qpj</scene>, resolution 2.05Å | |PDB= 2qpj |SIZE=350|CAPTION= <scene name='initialview01'>2qpj</scene>, resolution 2.05Å | ||
|SITE= | |SITE= | ||
| - | |LIGAND= | + | |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> |
| - | |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] | + | |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> |
|GENE= MME, EPN ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | |GENE= MME, EPN ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY= | ||
| + | |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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[[Category: Dale, G E.]] | [[Category: Dale, G E.]] | ||
[[Category: Oefner, C.]] | [[Category: Oefner, C.]] | ||
| - | [[Category: I20]] | ||
| - | [[Category: NAG]] | ||
| - | [[Category: ZN]] | ||
[[Category: glycoprotein]] | [[Category: glycoprotein]] | ||
[[Category: hydrolase]] | [[Category: hydrolase]] | ||
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[[Category: zinc-dependent metalloprotease]] | [[Category: zinc-dependent metalloprotease]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:51:47 2008'' |
Revision as of 01:51, 31 March 2008
| |||||||
| , resolution 2.05Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | , , | ||||||
| Gene: | MME, EPN (Homo sapiens) | ||||||
| Activity: | Neprilysin, with EC number 3.4.24.11 | ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| 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 Mon Mar 31 04:51:47 2008
