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Mechanism-based isocoumarin inhibitors for trypsin and blood coagulation serine proteases: new anticoagulants.
Kam CM, Fujikawa K, Powers JC. Kam CM, et al. Biochemistry. 1988 Apr 5;27(7):2547-57. doi: 10.1021/bi00407a042. Biochemistry. 1988. PMID: 3164217
The inhibition of these serine proteases by the substituted isocoumarins are time dependent, and the inactivation of trypsin by 3-alkoxy-4-chloro-7-guanidinoisocoumarins and 7-amino-4-chloro-3-(3-isothiureidopropoxy)isocoumarin …
The inhibition of these serine proteases by the substituted isocoumarins are time dependent, and the inactivation of trypsin by 3-alkoxy-4-c …
Human and murine cytotoxic T lymphocyte serine proteases: subsite mapping with peptide thioester substrates and inhibition of enzyme activity and cytolysis by isocoumarins.
Odake S, Kam CM, Narasimhan L, Poe M, Blake JT, Krahenbuhl O, Tschopp J, Powers JC. Odake S, et al. Biochemistry. 1991 Feb 26;30(8):2217-27. doi: 10.1021/bi00222a027. Biochemistry. 1991. PMID: 1998680
DCI, 3-(3-amino-propoxy)-4-chloroisocoumarin, 4-chloro-3-(3-isothiureidopropoxy)isocoumarin, and 7-amino-4-chloro-3-(3-isothiureidopropoxy)isocoumarin inhibited Q31 cytotoxic T lymphocyte mediated lysis of human JY lymphobla …
DCI, 3-(3-amino-propoxy)-4-chloroisocoumarin, 4-chloro-3-(3-isothiureidopropoxy)isocoumarin, and 7-amino-4-chloro …
A serine proteinase inactivator inhibits chondrocyte-mediated cartilage proteoglycan breakdown occurring in response to proinflammatory cytokines.
Bryson H, Bunning RA, Feltell R, Kam CM, Kerrigan J, Powers JC, Buttle DJ. Bryson H, et al. Arch Biochem Biophys. 1998 Jul 1;355(1):15-25. doi: 10.1006/abbi.1998.0696. Arch Biochem Biophys. 1998. PMID: 9647662
The role played by serine proteinases with trypsin-like specificity in chondrocyte-mediated cartilage proteoglycan breakdown was investigated by use of a selective proteinase inactivator, 7-amino-4-chloro-3-(-3-isothiureidopropoxy) …
The role played by serine proteinases with trypsin-like specificity in chondrocyte-mediated cartilage proteoglycan breakdown was investigate …
Activation of procollagenases is a key control point in cartilage collagen degradation: interaction of serine and metalloproteinase pathways.
Milner JM, Elliott SF, Cawston TE. Milner JM, et al. Arthritis Rheum. 2001 Sep;44(9):2084-96. doi: 10.1002/1529-0131(200109)44:9<2084::AID-ART359>3.0.CO;2-R. Arthritis Rheum. 2001. PMID: 11592371 Free article.
Addition of alpha1-proteinase inhibitor or a urokinase-type PA inhibitor, 7-amino-4-chloro-3-(3-isothiureidopropoxy) isocoumarin, partially blocked the breakdown of collagen from IL-1alpha/OSM-treated bovine cartilage. ...
Addition of alpha1-proteinase inhibitor or a urokinase-type PA inhibitor, 7-amino-4-chloro-3-(3- …
Thioester chromogenic substrates for human factor VIIa: substituted isocoumarins are inhibitors of factor VIIa and in vitro anticoagulants.
Kam CM, Vlasuk GP, Smith DE, Arcuri KE, Powers JC. Kam CM, et al. Thromb Haemost. 1990 Aug 13;64(1):133-7. Thromb Haemost. 1990. PMID: 2274918
With normal citrated human plasma, 4-chloro-3-ethoxy-7-guanidinoisocoumarin (3) and 7-amino-4-chloro-3-(3-isothiureidopropoxy) isocoumarin (ACITIC, 6) prolonged the prothrombin time (PT) ca. two-fold and prolonged the activa …
With normal citrated human plasma, 4-chloro-3-ethoxy-7-guanidinoisocoumarin (3) and 7-amino-4-chloro-3-( …