2oph

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[[Image:2oph.jpg|left|200px]]
[[Image:2oph.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2oph |SIZE=350|CAPTION= <scene name='initialview01'>2oph</scene>, resolution 2.40&Aring;
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The line below this paragraph, containing "STRUCTURE_2oph", 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=277:N-(TRANS-4-{(1S,2S)-2-AMINO-3-[(3S)-3-FLUOROPYRROLIDIN-1-YL]-1-METHYL-3-OXOPROPYL}CYCLOHEXYL)-N-METHYLACETAMIDE'>277</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=NDG:2-(ACETYLAMINO)-2-DEOXY-A-D-GLUCOPYRANOSE'>NDG</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/Dipeptidyl-peptidase_IV Dipeptidyl-peptidase IV], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.14.5 3.4.14.5] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= DPP4, ADCP2, CD26 ([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_2oph| PDB=2oph | SCENE= }}
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|RELATEDENTRY=[[1x70|1X70]], [[2iiv|2IIV]], [[2iit|2IIT]], [[2fjp|2FJP]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2oph FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2oph OCA], [http://www.ebi.ac.uk/pdbsum/2oph PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2oph RCSB]</span>
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}}
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'''Human dipeptidyl peptidase IV in complex with an alpha amino acid inhibitor'''
'''Human dipeptidyl peptidase IV in complex with an alpha amino acid inhibitor'''
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[[Category: Scapin, G.]]
[[Category: Scapin, G.]]
[[Category: Weber, A E.]]
[[Category: Weber, A E.]]
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[[Category: alpha/beta]]
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[[Category: Alpha/beta]]
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[[Category: beta-propeller]]
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[[Category: Beta-propeller]]
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[[Category: dimer]]
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[[Category: Dimer]]
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[[Category: selective inhibitor]]
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[[Category: Selective inhibitor]]
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[[Category: type 2 diabetes]]
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[[Category: Type 2 diabetes]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 11:23:33 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:21:14 2008''
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Revision as of 08:23, 4 May 2008

Image:2oph.jpg

Template:STRUCTURE 2oph

Human dipeptidyl peptidase IV in complex with an alpha amino acid inhibitor


Overview

A novel series of 4-aminophenylalanine and 4-aminocyclohexylalanine derivatives were designed and evaluated as inhibitors of dipeptidyl peptidase IV (DPP-4). The phenylalanine series afforded compounds such as 10 that were potent and selective (DPP-4, IC(50)=28nM), but exhibited limited oral bioavailability. The corresponding cyclohexylalanine derivatives such as 25 afforded improved PK exposure and efficacy in a murine OGTT experiment. The X-ray crystal structure of 25 bound to the DPP-4 active site is presented.

About this Structure

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

Reference

4-aminophenylalanine and 4-aminocyclohexylalanine derivatives as potent, selective, and orally bioavailable inhibitors of dipeptidyl peptidase IV., Duffy JL, Kirk BA, Wang L, Eiermann GJ, He H, Leiting B, Lyons KA, Patel RA, Patel SB, Petrov A, Scapin G, Wu JK, Thornberry NA, Weber AE, Bioorg Med Chem Lett. 2007 May 15;17(10):2879-85. Epub 2007 Feb 25. PMID:17350841 Page seeded by OCA on Sun May 4 11:23:33 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

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