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Literature summary extracted from

  • Cuffaro, D.; Nuti, E.; Gifford, V.; Ito, N.; Camodeca, C.; Tuccinardi, T.; Nencetti, S.; Orlandini, E.; Itoh, Y.; Rossello, A.
    Design, synthesis and biological evaluation of bifunctional inhibitors of membrane type 1 matrix metalloproteinase (MT1-MMP) (2019), Bioorg. Med. Chem., 27, 196-207 .
    View publication on PubMed

Application

EC Number Application Comment Organism
3.4.24.80 drug development dimeric MT1-MMP inhibitors might be further developed and exploited as an alternative tool to reduce cancer cell invasion Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.24.80 (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
3.4.24.80 (2R)-4-(acetylamino)-2-[(biphenyl-4-ylsulfonyl)amino]-N-hydroxybutanamide
-
Homo sapiens
3.4.24.80 CGS-27023A
-
Homo sapiens
3.4.24.80 additional information design, synthesis, and biological evaluation of bifunctional inhibitors of membrane type 1 matrix metalloproteinase (MT1-MMP), overview Homo sapiens
3.4.24.80 N,N'-bis(4-[[(3R)-3-[(biphenyl-4-ylsulfonyl)amino]-4-(hydroxyamino)-4-oxobutyl]amino]-4-oxobutyl)benzene-1,3-dicarboxamide
-
Homo sapiens
3.4.24.80 N,N'-bis[(3R)-3-[(biphenyl-4-ylsulfonyl)amino]-4-(hydroxyamino)-4-oxobutyl]benzene-1,3-dicarboxamide
-
Homo sapiens
3.4.24.80 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
3.4.24.80 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

EC Number Metals/Ions Comment Organism Structure
3.4.24.80 Zn2+ zinc-dependent endopeptidase Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.4.24.80 Collagen + H2O Homo sapiens
-
?
-
?
3.4.24.80 proMMP-2 + H2O Homo sapiens
-
MMP-2 + MMP-2 pro-peptide
-
?

Organism

EC Number Organism UniProt Comment Textmining
3.4.24.80 Homo sapiens P50281
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.24.80 fibrosarcoma cell
-
Homo sapiens
-
3.4.24.80 HT-1080 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.24.80 Collagen + H2O
-
Homo sapiens ?
-
?
3.4.24.80 Gelatin + H2O
-
Homo sapiens ?
-
?
3.4.24.80 proMMP-2 + H2O
-
Homo sapiens MMP-2 + MMP-2 pro-peptide
-
?

Synonyms

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

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.4.24.80 37
-
assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.4.24.80 7.5
-
assay at Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.24.80 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
3.4.24.80 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
3.4.24.80 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]
3.4.24.80 0.000023
-
pH 7.5, 37°C Homo sapiens CGS-27023A
3.4.24.80 0.000034
-
pH 7.5, 37°C Homo sapiens (2R)-4-(acetylamino)-2-[(biphenyl-4-ylsulfonyl)amino]-N-hydroxybutanamide
3.4.24.80 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
3.4.24.80 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

EC Number General Information Comment Organism
3.4.24.80 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