2rgu
From Proteopedia
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| , resolution 2.600Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | and | ||||||
| Gene: | DPP4, ADCP2, CD26 (Homo sapiens) | ||||||
| Activity: | Dipeptidyl-peptidase IV, with EC number 3.4.14.5 | ||||||
| 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 Thu Mar 20 18:35:59 2008
Categories: Dipeptidyl-peptidase IV | Homo sapiens | Single protein | Eckhardt, M. | Himmelsbach, F. | Nar, H. | 356 | NAG | Aminopeptidase | Glycoprotein | Hydrolase | Inhibitor | Membrane | Peptidase | Protease | Secreted | Serine protease | Signal-anchor | Transmembrane
