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Literature summary for 3.4.24.80 extracted from

  • Hurst, D.R.; Schwartz, M.A.; Jin, Y.; Ghaffari, M.A.; Kozarekar, P.; Cao, J.; Sang, Q.X.
    Inhibition of enzyme activity of and cell-mediated substrate cleavage by membrane type 1 matrix metalloproteinase by newly developed mercaptosulphide inhibitors (2005), Biochem. J., 392, 527-536.
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
medicine some mercaptosulfide inhibitors effectively inhibit activation of proMMP-2 by endogenous MT1-MMP produced by HT1080 human fibrosarcoma cells, block fibronectin degradation by prostate cancer LNCaP cells stably transfected with MT1-MPP Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
additional information mercaptosulfide inhibitors, interacting exclusively at the enzyme active site, strong stereoselectivity at the P1' and zinc-binding groups, competitive and reverse inhibition Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
fibrosarcoma cell
-
Homo sapiens
-
HT-1080 cell
-
Homo sapiens
-
LNCaP cell
-
Homo sapiens
-
prostate cancer cell line
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
(7-methoxycoumarin-4-yl)acetyl-Pro-Leu-Gly-Leu-N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl-Ala-Arg-NH2 + H2O
-
Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
membrane type 1 matrix metalloproteinase
-
Homo sapiens
MT1-MMP
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
additional information between 0.000049 mM and 0.012 mM, significant decrease in inhibition potency with a homophenylalanine side chain compared with leucine, P1' substituent is interacting at the S1' pocket Homo sapiens