2a8h

From Proteopedia

Revision as of 14:25, 21 February 2008 by OCA (Talk | contribs)
Jump to: navigation, search
Image:2a8h.gif

2a8h, resolution 2.30Å

Drag the structure with the mouse to rotate

Crystal structure of catalytic domain of TACE with Thiomorpholine Sulfonamide Hydroxamate inhibitor

Overview

A series of thiomorpholine sulfonamide hydroxamate TACE inhibitors, all bearing propargylic ether P1' groups, was explored. In particular, compound 5h has excellent in vitro potency against isolated TACE enzyme and in cells, oral activity in a model of TNF-alpha production and a collagen-induced arthritis model, was selected as a clinical candidate for the treatment of RA.

About this Structure

2A8H is a Single protein structure of sequence from Homo sapiens with and 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 3: Thiomorpholine sulfonamide hydroxamates., Levin JI, Chen JM, Laakso LM, Du M, Schmid J, Xu W, Cummons T, Xu J, Jin G, Barone D, Skotnicki JS, Bioorg Med Chem Lett. 2006 Mar 15;16(6):1605-9. Epub 2006 Jan 19. PMID:16426848

Page seeded by OCA on Thu Feb 21 16:24:49 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/2a8h"
Personal tools