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1rwq
From Proteopedia
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(New page: 200px<br /> <applet load="1rwq" size="450" color="white" frame="true" align="right" spinBox="true" caption="1rwq, resolution 2.20Å" /> '''Human Dipeptidyl pe...)
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Revision as of 17:01, 12 November 2007
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Human Dipeptidyl peptidase IV in complex with 5-aminomethyl-6-(2,4-dichloro-phenyl)-2-(3,5-dimethoxy-phenyl)-pyrimidin-4-ylamine
Overview
The influence of aromatic substitution on a newly discovered class of, inhibitors of dipeptidyl peptidase IV was investigated. A 10(5)-fold, increase in potency was achieved by the optimization of aromatic, substituents in a parallel chemistry program. The observed SAR could be, explained by an X-ray structure of the protein-ligand complex.
About this Structure
1RWQ is a Single protein structure of sequence from Homo sapiens with NAG and 5AP as ligands. Active as Dipeptidyl-peptidase IV, with EC number 3.4.14.5 Full crystallographic information is available from OCA.
Reference
Aminomethylpyrimidines as novel DPP-IV inhibitors: a 10(5)-fold activity increase by optimization of aromatic substituents., Peters JU, Weber S, Kritter S, Weiss P, Wallier A, Boehringer M, Hennig M, Kuhn B, Loeffler BM, Bioorg Med Chem Lett. 2004 Mar 22;14(6):1491-3. PMID:15006388
Page seeded by OCA on Mon Nov 12 19:07:51 2007
