2rgu

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[[Image:2rgu.jpg|left|200px]]
[[Image:2rgu.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2rgu |SIZE=350|CAPTION= <scene name='initialview01'>2rgu</scene>, resolution 2.600&Aring;
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The line below this paragraph, containing "STRUCTURE_2rgu", 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=356:8-[(3R)-3-AMINOPIPERIDIN-1-YL]-7-BUT-2-YN-1-YL-3-METHYL-1-[(4-METHYLQUINAZOLIN-2-YL)METHYL]-3,7-DIHYDRO-1H-PURINE-2,6-DIONE'>356</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= 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_2rgu| PDB=2rgu | 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=2rgu FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2rgu OCA], [http://www.ebi.ac.uk/pdbsum/2rgu PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2rgu RCSB]</span>
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}}
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'''Crystal structure of complex of human DPP4 and inhibitor'''
'''Crystal structure of complex of human DPP4 and inhibitor'''
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[[Category: Himmelsbach, F.]]
[[Category: Himmelsbach, F.]]
[[Category: Nar, H.]]
[[Category: Nar, H.]]
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[[Category: aminopeptidase]]
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[[Category: Aminopeptidase]]
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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: inhibitor]]
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[[Category: Inhibitor]]
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[[Category: membrane]]
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[[Category: Membrane]]
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[[Category: peptidase]]
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[[Category: Peptidase]]
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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 16:53:18 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 05:00:16 2008''
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Revision as of 13:53, 4 May 2008

Image:2rgu.jpg

Template:STRUCTURE 2rgu

Crystal structure of complex of human DPP4 and inhibitor


Overview

A new chemical class of potent DPP-4 inhibitors structurally derived from the xanthine scaffold for the treatment of type 2 diabetes has been discovered and evaluated. Systematic structural variations have led to 1 (BI 1356), a highly potent, selective, long-acting, and orally active DPP-4 inhibitor that shows considerable blood glucose lowering in different animal species. 1 is currently undergoing clinical phase IIb trials and holds the potential for once-daily treatment of type 2 diabetics.

About this Structure

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

Reference

8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin -2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes., Eckhardt M, Langkopf E, Mark M, Tadayyon M, Thomas L, Nar H, Pfrengle W, Guth B, Lotz R, Sieger P, Fuchs H, Himmelsbach F, J Med Chem. 2007 Dec 27;50(26):6450-3. Epub 2007 Dec 1. PMID:18052023 Page seeded by OCA on Sun May 4 16:53:18 2008

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OCA

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