2a8h

From Proteopedia

Revision as of 13:46, 20 March 2008 by OCA (Talk | contribs)
Jump to: navigation, search
Image:2a8h.gif


PDB ID 2a8h

Drag the structure with the mouse to rotate
, resolution 2.30Å
Ligands: and
Gene: ADAM17, CSVP, TACE (Homo sapiens)
Activity: ADAM 17 endopeptidase, with EC number 3.4.24.86
Coordinates: save as pdb, mmCIF, xml



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. 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 Mar 20 15:46:41 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

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