2ole
From Proteopedia
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Crystal Structure Of Human Dipeptidyl Peptidase IV (DPPIV) Complex With Cyclic Hydrazine Derivatives
Overview
Inhibitors of dipeptidyl peptidase IV (DPP-IV) have been shown to be, effective treatments for type 2 diabetes. A series of, beta-aminoacyl-containing cyclic hydrazine derivatives were synthesized, and evaluated as DPP-IV inhibitors. One member of this series, (R)-3-amino-1-(2-benzoyl-1,2-diazepan-1-yl)-4-(2,4,5-trifluorophenyl)butan, -1-one (10f), showed potent in vitro activity, good selectivity and in, vivo efficacy in mouse models. Also, the binding mode of compound 10f was, determined by X-ray crystallography.
About this Structure
2OLE is a Single protein structure of sequence from Homo sapiens with as ligand. Active as Dipeptidyl-peptidase IV, with EC number 3.4.14.5 Full crystallographic information is available from OCA.
Reference
Synthesis, biological evaluation and structural determination of beta-aminoacyl-containing cyclic hydrazine derivatives as dipeptidyl peptidase IV (DPP-IV) inhibitors., Ahn JH, Shin MS, Jun MA, Jung SH, Kang SK, Kim KR, Rhee SD, Kang NS, Kim SY, Sohn SK, Kim SG, Jin MS, Lee JO, Cheon HG, Kim SS, Bioorg Med Chem Lett. 2007 May 1;17(9):2622-8. Epub 2007 Feb 8. PMID:17331715
Page seeded by OCA on Wed Jan 23 10:49:49 2008
