3b2z | pdb_00003b2z
Crystal Structure of ADAMTS4 (apo form)
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Overview
Aggrecanases are now believed to be the principal proteinases responsible, for aggrecan degradation in osteoarthritis. Given their potential as a, drug target, we solved crystal structures of the two most active human, aggrecanase isoforms, ADAMTS4 and ADAMTS5, each in complex with bound, inhibitor and one wherein the enzyme is in apo form. These structures show, that the unliganded and inhibitor-bound enzymes exhibit two essentially, different catalytic-site configurations: an autoinhibited, nonbinding, closed form and an open, binding form. On this basis, we propose that, mature aggrecanases exist as an ensemble of at least two isomers, only one, of which is proteolytically active.
About this Structure
3B2Z is a Single protein structure of sequence from Homo sapiens with ZN and CA as ligands. Active as ADAMTS-4 endopeptidase, with EC number 3.4.24.82 Full crystallographic information is available from OCA.
Reference
Crystal structures of the two major aggrecan degrading enzymes, ADAMTS4 and ADAMTS5., Mosyak L, Georgiadis K, Shane T, Svenson K, Hebert T, McDonagh T, Mackie S, Olland S, Lin L, Zhong X, Kriz R, Reifenberg EL, Collins-Racie LA, Corcoran C, Freeman B, Zollner R, Marvell T, Vera M, Sum PE, Lavallie ER, Stahl M, Somers W, Protein Sci. 2007 Nov 27;. PMID:18042673
Page seeded by OCA on Mon Jan 14 18:23:23 2008
