2rgu
From Proteopedia
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|PDB= 2rgu |SIZE=350|CAPTION= <scene name='initialview01'>2rgu</scene>, resolution 2.600Å | |PDB= 2rgu |SIZE=350|CAPTION= <scene name='initialview01'>2rgu</scene>, resolution 2.600Å | ||
|SITE= | |SITE= | ||
| - | |LIGAND= | + | |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> |
| - | |ACTIVITY= [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] | + | |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> |
|GENE= DPP4, ADCP2, CD26 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | |GENE= DPP4, ADCP2, CD26 ([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=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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[[Category: Himmelsbach, F.]] | [[Category: Himmelsbach, F.]] | ||
[[Category: Nar, H.]] | [[Category: Nar, H.]] | ||
| - | [[Category: 356]] | ||
| - | [[Category: NAG]] | ||
[[Category: aminopeptidase]] | [[Category: aminopeptidase]] | ||
[[Category: glycoprotein]] | [[Category: glycoprotein]] | ||
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[[Category: transmembrane]] | [[Category: transmembrane]] | ||
| - | ''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 05:00:16 2008'' |
Revision as of 02:00, 31 March 2008
| |||||||
| , resolution 2.600Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | , | ||||||
| Gene: | DPP4, ADCP2, CD26 (Homo sapiens) | ||||||
| Activity: | Dipeptidyl-peptidase IV, with EC number 3.4.14.5 | ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
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 Mon Mar 31 05:00:16 2008
