2fjp

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[[Image:2fjp.gif|left|200px]]
[[Image:2fjp.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2fjp |SIZE=350|CAPTION= <scene name='initialview01'>2fjp</scene>, resolution 2.40&Aring;
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The line below this paragraph, containing "STRUCTURE_2fjp", 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=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=S14:6-(4-{(1S,2S)-2-AMINO-1-[(DIMETHYLAMINO)CARBONYL]-3-[(3S)-3-FLUOROPYRROLIDIN-1-YL]-3-OXOPROPYL}PHENYL)-1H-[1,2,4]TRIAZOLO[1,5-A]PYRIDIN-4-IUM'>S14</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_2fjp| PDB=2fjp | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2fjp FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2fjp OCA], [http://www.ebi.ac.uk/pdbsum/2fjp PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2fjp RCSB]</span>
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}}
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'''Human dipeptidyl peptidase IV/CD26 in complex with an inhibitor'''
'''Human dipeptidyl peptidase IV/CD26 in complex with an inhibitor'''
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[[Category: Patel, S B.]]
[[Category: Patel, S B.]]
[[Category: Scapin, G.]]
[[Category: Scapin, G.]]
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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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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 03:58:41 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:03:43 2008''
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Revision as of 00:58, 4 May 2008

Image:2fjp.gif

Template:STRUCTURE 2fjp

Human dipeptidyl peptidase IV/CD26 in complex with an inhibitor


Overview

A series of beta-substituted biarylphenylalanine amides were synthesized and evaluated as inhibitors of dipeptidyl peptidase IV (DPP-4) for the treatment of type 2 diabetes. Optimization of the metabolic profile of early analogues led to the discovery of (2S,3S)-3-amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1 ,2,4]triazolo[1,5-a]pyridin-6-ylphenyl)butanamide (6), a potent, orally active DPP-4 inhibitor (IC(50) = 6.3 nM) with excellent selectivity, oral bioavailability in preclinical species, and in vivo efficacy in animal models. Compound 6 was selected for further characterization as a potential new treatment for type 2 diabetes.

About this Structure

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

Reference

(2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1 ,2,4]triazolo[1,5-a]-pyridin-6-ylphenyl)butanamide: a selective alpha-amino amide dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes., Edmondson SD, Mastracchio A, Mathvink RJ, He J, Harper B, Park YJ, Beconi M, Di Salvo J, Eiermann GJ, He H, Leiting B, Leone JF, Levorse DA, Lyons K, Patel RA, Patel SB, Petrov A, Scapin G, Shang J, Roy RS, Smith A, Wu JK, Xu S, Zhu B, Thornberry NA, Weber AE, J Med Chem. 2006 Jun 15;49(12):3614-27. PMID:16759103 Page seeded by OCA on Sun May 4 03:58:41 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

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