2ogz

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Image:2ogz.gif

2ogz, resolution 2.100Å

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Crystal structure of DPP-IV complexed with Lilly aryl ketone inhibitor

Overview

A series of non-covalent inhibitors of the serine protease dipeptidyl, peptidase IV (DPP-IV) were found to adopt a U-shaped binding conformation, in X-ray co-crystallization studies. Remarkably, Tyr547 undergoes a 70, degrees side-chain rotation to accommodate the inhibitor and allows access, to a previously unexposed area of the protein backbone for hydrogen, bonding.

About this Structure

2OGZ is a Single protein structure of sequence from Homo sapiens with U1N as ligand. Active as Dipeptidyl-peptidase IV, with EC number 3.4.14.5 Full crystallographic information is available from OCA.

Reference

Discovery of non-covalent dipeptidyl peptidase IV inhibitors which induce a conformational change in the active site., Sheehan SM, Mest HJ, Watson BM, Klimkowski VJ, Timm DE, Cauvin A, Parsons SH, Shi Q, Canada EJ, Wiley MR, Ruehter G, Evers B, Petersen S, Blaszczak LC, Pulley SR, Margolis BJ, Wishart GN, Renson B, Hankotius D, Mohr M, Zechel JC, Michael Kalbfleisch J, Dingess-Hammond EA, Boelke A, Weichert AG, Bioorg Med Chem Lett. 2007 Mar 15;17(6):1765-8. Epub 2006 Dec 24. PMID:17239592

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