Literature summary for 3.4.24.86 extracted from

  • Milla, M.E.; Leesnitzer, M.A.; Moss, M.L.; Clay, W.C.; Carter, H.L.; Miller, A.B.; Su, J.L.; Lambert, M.H.; Willard, D.H.; Sheeley, D.M.; Kost, T.A.; Burkhart, W.; Moyer, M.; Blackburn, R.K.; Pahel, G.L.; Mitchell, J.L.; Hoffman, C.R.; Becherer, J.D.
    Specific sequence elements are required for the expression of functional tumor necrosis factor-alpha-converting enzyme (TACE) (1999), J. Biol. Chem., 274, 30563-30570.
    View publication on PubMed

Application

Application Comment Organism
medicine targeting this key enzyme for therapeutic intervention in inflammatory diseases, cancer and AIDS Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
cDNA encoding TACE, full-length human TACE, inefficiently expressed in insect cells, baculovirus particles in Sf9 cell line from Spodoptera frugiperda Homo sapiens

General Stability

General Stability Organism
extreme salt sensitivity Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
APMA inhibits TACE completely Homo sapiens
GW9471 hydroxamic acid competitive inhibitor that totally blocks TACE activity Homo sapiens
NaCl dramatic inhibitory effect on the activity of TACE Homo sapiens
TACE-pro domain pro domain is an inhibitor of the catalytic domain Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
membrane
-
Homo sapiens
-
-
cytosol cytosolic tail of TACE precedes TACE activation Homo sapiens
-
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
TNF-alpha + H2O Homo sapiens
-
soluble TNF-alpha
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
human
-
Homo sapiens
-
MonoMac 6 cells
-

Purification (Commentary)

Purification (Comment) Organism
-
Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
monocyte
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
proTNF-alpha + H2O
-
Homo sapiens soluble TNF-alpha release of proTNFalpha from cellular membranes ?
transforming growth factor alpha + H2O
-
Homo sapiens ?
-
?
TNF-alpha + H2O
-
Homo sapiens soluble TNF-alpha
-
?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
5
-
NaCl
-
Homo sapiens