2rip

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[[Image:2rip.jpg|left|200px]]
[[Image:2rip.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2rip |SIZE=350|CAPTION= <scene name='initialview01'>2rip</scene>, resolution 2.90&Aring;
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The line below this paragraph, containing "STRUCTURE_2rip", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC1:Nag+Binding+Site+For+Residue+A+1085'>AC1</scene>, <scene name='pdbsite=AC2:Nag+Binding+Site+For+Residue+A+2085'>AC2</scene>, <scene name='pdbsite=AC3:Man+Binding+Site+For+Residue+A+3085'>AC3</scene>, <scene name='pdbsite=AC4:Man+Binding+Site+For+Residue+A+4085'>AC4</scene>, <scene name='pdbsite=AC5:Nag+Binding+Site+For+Residue+A+4086'>AC5</scene>, <scene name='pdbsite=AC6:Nag+Binding+Site+For+Residue+A+4087'>AC6</scene>, <scene name='pdbsite=AC7:Nag+Binding+Site+For+Residue+A+1219'>AC7</scene>, <scene name='pdbsite=AC8:Nag+Binding+Site+For+Residue+A+1229'>AC8</scene>, <scene name='pdbsite=AC9:Nag+Binding+Site+For+Residue+A+1281'>AC9</scene>, <scene name='pdbsite=BC1:Nag+Binding+Site+For+Residue+A+1321'>BC1</scene> and <scene name='pdbsite=BC2:34q+Binding+Site+For+Residue+A+800'>BC2</scene>
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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=34Q:(3R,4R)-4-(PYRROLIDIN-1-YLCARBONYL)-1-(QUINOXALIN-2-YLCARBONYL)PYRROLIDIN-3-AMINE'>34Q</scene>, <scene name='pdbligand=MAN:ALPHA-D-MANNOSE'>MAN</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</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= DPPIV ([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_2rip| PDB=2rip | 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=2rip FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2rip OCA], [http://www.ebi.ac.uk/pdbsum/2rip PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2rip RCSB]</span>
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}}
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'''Structure of DPPIV in complex with an inhibitor'''
'''Structure of DPPIV in complex with an inhibitor'''
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[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Qiu, X.]]
[[Category: Qiu, X.]]
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[[Category: aminopeptidase]]
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[[Category: Aminopeptidase]]
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[[Category: diabetes]]
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[[Category: Diabetes]]
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[[Category: dppiv]]
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[[Category: Dppiv]]
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[[Category: drug design]]
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[[Category: Drug design]]
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[[Category: glycoprotein]]
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[[Category: Glycoprotein]]
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[[Category: hydrolase]]
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[[Category: Hydrolase]]
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[[Category: membrane]]
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[[Category: Membrane]]
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[[Category: protease]]
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[[Category: Protease]]
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[[Category: secreted]]
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[[Category: Secreted]]
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[[Category: serine protease]]
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[[Category: Serine protease]]
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[[Category: signal-anchor]]
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[[Category: Signal-anchor]]
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[[Category: transmembrane]]
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[[Category: Transmembrane]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 16:58:57 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 05:00:55 2008''
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Revision as of 13:58, 4 May 2008

Image:2rip.jpg

Template:STRUCTURE 2rip

Structure of DPPIV in complex with an inhibitor


Overview

The cis-3-amino-4-(2-cyanopyrrolidide)-pyrrolidine template has been shown to afford low nanomolar inhibitors of human DPP-IV that exhibit a robust PK/PD profile. An X-ray co-crystal structure of 5 confirmed the proposed mode of binding. The potent single digit DPP-IV inhibitor 53 exhibited a preferred PK/PD profile in preclinical animal models and was selected for additional profiling.

About this Structure

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

Reference

Design and synthesis of potent amido- and benzyl-substituted cis-3-amino-4-(2-cyanopyrrolidide)pyrrolidinyl DPP-IV inhibitors., Corbett JW, Dirico K, Song W, Boscoe BP, Doran SD, Boyer D, Qiu X, Ammirati M, Vanvolkenburg MA, McPherson RK, Parker JC, Cox ED, Bioorg Med Chem Lett. 2007 Dec 15;17(24):6707-13. Epub 2007 Oct 22. PMID:17977724 Page seeded by OCA on Sun May 4 16:58:57 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

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