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TargetDisintegrin and metalloproteinase domain-containing protein 17 [215-477,S266A,N452Q]
LigandBDBM26525
Substrate/CompetitorTACE substrate peptide
Meas. Tech.TACE Inhibition Assay
pH7.3±n/a
Temperature295.15±n/a K
Ki 0.18±n/a nM
Citation Guo, Z; Orth, P; Wong, SC; Lavey, BJ; Shih, NY; Niu, X; Lundell, DJ; Madison, V; Kozlowski, JA Discovery of novel spirocyclopropyl hydroxamate and carboxylate compounds as TACE inhibitors. Bioorg Med Chem Lett19:54-7 (2009) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Disintegrin and metalloproteinase domain-containing protein 17 [215-477,S266A,N452Q]
Name:Disintegrin and metalloproteinase domain-containing protein 17 [215-477,S266A,N452Q]
Synonyms:A disintegrin and metalloproteinase domain 17 | ADA17_HUMAN | ADAM 17 | ADAM17 | CD156b antigen | CSVP | Snake venom-like protease | TACE | TNF-alpha-Converting Enzyme
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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM26525
TACE substrate peptide
Name:TACE substrate peptide
Synonyms:n/a
Type:Internally quenched peptide
Mol. Mass.:4119.10
Organism:n/a
Description:MCA, (7-methoxycoumarin-4-yl)acetyl. Dpa, N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl.
Residue:39
Sequence:
MCA-Pro-Leu-Ala-Gln-Ala-Val-Arg-Ser-Ser-Ser-Dpa-Arg-NH2