Matlystatins, new inhibitors of typeIV collagenases from Actinomadura atramentaria. II. Biological activities.
Matlystatin A, the main component of matlystatins, inhibits 92 kDa and 72 kDa typeIV collagenases with IC50 values of 0.3 microM and 0.56 microM, respectively, while 7- to 11-fold greater concentrations are required to inhibit thermolysin and aminopeptidase M. The inhibition is reversible and competitive with respect to gelatin. It inhibits the invasion of basement membrane Matrigel by human fibrosarcoma HT1080 dose-dependently with an IC50 value of 21.6 microM.
Fermentation Research Laboratories, Sankyo Co., Ltd., Tokyo, Japan.
K
K
Tanzawa
M
M
Ishii
T
T
Ogita
K
K
Shimada
D000111:Acetylcysteine / Q000031:analogs & derivatives / Q000494:pharmacology; D000192:Actinomycetales / Q000378:metabolism*; D000626:Aminopeptidases / Q000037:antagonists & inhibitors; D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D001485:Basement Membrane / Q000473:pathology; D001667:Binding, Competitive; D018826:CD13 Antigens; D005354:Fibrosarcoma / Q000473:pathology; D005658:Fungi / Q000187:drug effects; D005780:Gelatin / Q000378:metabolism; D006801:Humans; D020780:Matrix Metalloproteinase 9; D061965:Matrix Metalloproteinase Inhibitors; D008970:Molecular Weight; D011724:Pyridazines / Q000494:pharmacology; D013820:Thermolysin / Q000037:antagonists & inhibitors; D014407:Tumor Cells, Cultured
D000900:Anti-Bacterial Agents; D061965:Matrix Metalloproteinase Inhibitors; D011724:Pyridazines; C078837:matlystatin A; C078838:matlystatin B; D005780:Gelatin; D000626:Aminopeptidases; D018826:CD13 Antigens; D013820:Thermolysin; D020780:Matrix Metalloproteinase 9; D000111:Acetylcysteine