Application | Comment | Organism |
---|---|---|
drug development | dimeric MT1-MMP inhibitors might be further developed and exploited as an alternative tool to reduce cancer cell invasion | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(2R)-4-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-hydroxy-2-[[(4'-methoxybiphenyl-4-yl)sulfonyl](propan-2-yloxy)amino]butanamide | - |
Homo sapiens | |
(2R)-4-(acetylamino)-2-[(biphenyl-4-ylsulfonyl)amino]-N-hydroxybutanamide | - |
Homo sapiens | |
CGS-27023A | - |
Homo sapiens | |
additional information | design, synthesis, and biological evaluation of bifunctional inhibitors of membrane type 1 matrix metalloproteinase (MT1-MMP), overview | Homo sapiens | |
N,N'-bis(4-[[(3R)-3-[(biphenyl-4-ylsulfonyl)amino]-4-(hydroxyamino)-4-oxobutyl]amino]-4-oxobutyl)benzene-1,3-dicarboxamide | - |
Homo sapiens | |
N,N'-bis[(3R)-3-[(biphenyl-4-ylsulfonyl)amino]-4-(hydroxyamino)-4-oxobutyl]benzene-1,3-dicarboxamide | - |
Homo sapiens | |
N,N'-bis[4-[(2-[[(2R)-4-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-1-(hydroxyamino)-1-oxobutan-2-yl][(4'-methoxybiphenyl-4-yl)sulfonyl]amino]ethyl)amino]-4-oxobutyl]benzene-1,3-dicarboxamide | - |
Homo sapiens | |
N-(2-[[(2R)-4-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-1-(hydroxyamino)-1-oxobutan-2-yl][(4'-methoxybiphenyl-4-yl)sulfonyl]amino]ethyl)-N'-(2-[[4-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-1-(hydroxyamino)-1-oxobutan-2-yl][(4'-methoxybiphenyl-4-yl)sulfonyl] | modelling ofcompound 6 binding to dimeric MT1-MMP (catalytic domains) | Homo sapiens |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Zn2+ | zinc-dependent endopeptidase | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
Collagen + H2O | Homo sapiens | - |
? | - |
? | |
proMMP-2 + H2O | Homo sapiens | - |
MMP-2 + MMP-2 pro-peptide | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P50281 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
fibrosarcoma cell | - |
Homo sapiens | - |
HT-1080 cell | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
Collagen + H2O | - |
Homo sapiens | ? | - |
? | |
Gelatin + H2O | - |
Homo sapiens | ? | - |
? | |
proMMP-2 + H2O | - |
Homo sapiens | MMP-2 + MMP-2 pro-peptide | - |
? |
Synonyms | Comment | Organism |
---|---|---|
membrane type 1 matrix metalloproteinase | - |
Homo sapiens |
MT1-MMP | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.5 | - |
assay at | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0000039 | - |
pH 7.5, 37°C | Homo sapiens | (2R)-4-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-hydroxy-2-[[(4'-methoxybiphenyl-4-yl)sulfonyl](propan-2-yloxy)amino]butanamide | |
0.000007 | - |
pH 7.5, 37°C | Homo sapiens | N,N'-bis[4-[(2-[[(2R)-4-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-1-(hydroxyamino)-1-oxobutan-2-yl][(4'-methoxybiphenyl-4-yl)sulfonyl]amino]ethyl)amino]-4-oxobutyl]benzene-1,3-dicarboxamide | |
0.000014 | - |
pH 7.5, 37°C | Homo sapiens | N-(2-[[(2R)-4-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-1-(hydroxyamino)-1-oxobutan-2-yl][(4'-methoxybiphenyl-4-yl)sulfonyl]amino]ethyl)-N'-(2-[[4-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-1-(hydroxyamino)-1-oxobutan-2-yl][(4'-methoxybiphenyl-4-yl)sulfonyl] | |
0.000023 | - |
pH 7.5, 37°C | Homo sapiens | CGS-27023A | |
0.000034 | - |
pH 7.5, 37°C | Homo sapiens | (2R)-4-(acetylamino)-2-[(biphenyl-4-ylsulfonyl)amino]-N-hydroxybutanamide | |
0.000041 | - |
pH 7.5, 37°C | Homo sapiens | N,N'-bis(4-[[(3R)-3-[(biphenyl-4-ylsulfonyl)amino]-4-(hydroxyamino)-4-oxobutyl]amino]-4-oxobutyl)benzene-1,3-dicarboxamide | |
0.00008 | - |
pH 7.5, 37°C | Homo sapiens | N,N'-bis[(3R)-3-[(biphenyl-4-ylsulfonyl)amino]-4-(hydroxyamino)-4-oxobutyl]benzene-1,3-dicarboxamide |
General Information | Comment | Organism |
---|---|---|
physiological function | collagen degradation and proMMP-2 activation are major functions of MT1-MMP to promote cancer cell invasion. Both processes require MT1-MMP homodimerization on the cell surface | Homo sapiens |