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TargetTNF-alpha-Converting Enzyme
LigandBDBM23490
Substrate/CompetitorBDBM23453
Meas. Tech.TACE Inhibition Assay
Ki 130±n/a nM
Citation Zhu ZMazzola RSinning LMcKittrick BNiu XLundell DSun JOrth PGuo ZMadison VIngram RBeyer BM Discovery of novel hydroxamates as highly potent tumor necrosis factor-alpha converting enzyme inhibitors: Part I--discovery of two binding modes. J Med Chem 51:725-36 (2008) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
TNF-alpha-Converting Enzyme
Name:TNF-alpha-Converting Enzyme
Synonyms:A disintegrin and metalloproteinase domain 17 | ADAM 17 | CD156b antigen | Snake venom-like protease
Type:Single-pass type I membrane protein; metalloprotease
Mol. Mass.:29695.98
Organism:Homo sapiens (Human)
Description:The catalytic domain of recombinant human TNF-converting enzyme (residues 215-477) with two mutations (S266A and N452Q) and a 6xHis was purified from the baculovirus/Hi5 cells expression system.
Residue:263
Sequence:
RADPDPMKNTCKLLVVADHRFYRYMGRGEESTTTNYLIELIDRVDDIYRNTAWDNAGFKG
YGIQIEQIRILKSPQEVKPGEKHYNMAKSYPNEEKDAWDVKMLLEQFSFDIAEEASKVCL
AHLFTYQDFDMGTLGLAYVGSPRANSHGGVCPKAYYSPVGKKNIYLNSGLTSTKNYGKTI
LTKEADLVTTHELGHNFGAEHDPDGLAECAPNEDQGGKYVMYPIAVSGDHENNKMFSQCS
KQSIYKTIESKAQECFQERSNKV
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  Blast E-value cutoff:
BDBM23490
BDBM23453
NameBDBM23490
Synonyms:hydroxamate deriv., 81 | methyl (1R,2S)-1-({4-[(3,4-dichlorophenyl)methoxy]phenyl}methyl)-2-(hydroxycarbamoyl)cyclopropane-1-carboxylate
TypeSmall organic molecule
Emp. Form.C20H19Cl2NO5
Mol. Mass.424.275
SMILESCOC(=O)[C@@]1(Cc2ccc(OCc3ccc(Cl)c(Cl)c3)cc2)C[C@@H]1C(=O)NO |r|
Structure
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