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1zxc

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(New page: 200px<br /> <applet load="1zxc" size="450" color="white" frame="true" align="right" spinBox="true" caption="1zxc, resolution 2.28&Aring;" /> '''Crystal structure o...)
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Revision as of 18:36, 12 November 2007

Image:1zxc.gif

1zxc, resolution 2.28Å

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Crystal structure of catalytic domain of TNF-alpha converting enzyme (TACE) with inhibitor

Overview

The SAR of a series of potent sulfonamide hydroxamate TACE inhibitors, bearing a butynyloxy P1' group was explored. In particular, compound 5k, has excellent in vitro potency against TACE enzyme and in cells, and oral, activity in an in vivo model of TNF-alpha production and a, collagen-induced arthritis model.

About this Structure

1ZXC is a Single protein structure of sequence from Homo sapiens with ZN and IH6 as ligands. Active as ADAM 17 endopeptidase, with EC number 3.4.24.86 Full crystallographic information is available from OCA.

Reference

Acetylenic TACE inhibitors. Part 2: SAR of six-membered cyclic sulfonamide hydroxamates., Levin JI, Chen JM, Laakso LM, Du M, Du X, Venkatesan AM, Sandanayaka V, Zask A, Xu J, Xu W, Zhang Y, Skotnicki JS, Bioorg Med Chem Lett. 2005 Oct 1;15(19):4345-9. PMID:16084720

Page seeded by OCA on Mon Nov 12 20:42:48 2007

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