2i47
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Crystal structure of catalytic domain of TACE with inhibitor
OverviewOverview
By focusing on the P1 portion of the piperidine beta-sulfone ligands we, identified a motif that induces selectivity and resulted in a series of, TACE inhibitors that demonstrated excellent in vitro potency against, isolated TACE enzyme and excellent selectivity over MMPs 1, 2, 9, 13, and, 14.
About this StructureAbout this Structure
2I47 is a Single protein structure of sequence from Homo sapiens with ZN, INN and KGY as ligands. Active as ADAM 17 endopeptidase, with EC number 3.4.24.86 Full crystallographic information is available from OCA.
ReferenceReference
Identification of potent and selective TACE inhibitors via the S1 pocket., Condon JS, Joseph-McCarthy D, Levin JI, Lombart HG, Lovering FE, Sun L, Wang W, Xu W, Zhang Y, Bioorg Med Chem Lett. 2007 Jan 1;17(1):34-9. Epub 2006 Oct 5. PMID:17064892
Page seeded by OCA on Mon Nov 12 22:40:37 2007