2rgu

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Image:2rgu.jpg

2rgu, resolution 2.600Å

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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 with and as ligands. Active as Dipeptidyl-peptidase IV, with EC number 3.4.14.5 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

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