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1zxc
From Proteopedia
| 1zxc, resolution 2.28Å () | |||||||||
|---|---|---|---|---|---|---|---|---|---|
| Ligands: | , | ||||||||
| Gene: | ADAM17, CSVP, TACE (Homo sapiens) | ||||||||
| Activity: | ADAM 17 endopeptidase, with EC number 3.4.24.86 | ||||||||
| Domains: | ZnMc_TACE_like | ||||||||
| Related: | 1bkc | ||||||||
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| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||
Crystal structure of catalytic domain of TNF-alpha converting enzyme (TACE) with inhibitor
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.
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
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
About this Structure
1ZXC is a 2 chains structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.
Reference
- Levin JI, Chen JM, Laakso LM, Du M, Du X, Venkatesan AM, Sandanayaka V, Zask A, Xu J, Xu W, Zhang Y, Skotnicki JS. Acetylenic TACE inhibitors. Part 2: SAR of six-membered cyclic sulfonamide hydroxamates. Bioorg Med Chem Lett. 2005 Oct 1;15(19):4345-9. PMID:16084720 doi:10.1016/j.bmcl.2005.06.072
Page seeded by OCA on Mon Feb 16 20:20:07 2009
