Development of plasmin and plasma kallikrein selective inhibitors and their effect on M1 (melanoma) and HT29 cell lines.
trans-4-Aminomethylcyclohexanecarbonyl-Tyr(O-Pic)-octylamide (YO-2) inhibited plasmin (PL) selectively, while trans-4-aminomethylcyclohexanecarbonyl-Phe-4-carboxymethylanili de (YO-1) inhibited plasma kallikrein (PK). YO-2 induced apoptosis of M1 (melanoma) cell line and HT29 colon carcinoma cells during 24 h through activation of caspase-3, while YO-1 did not affect either cell line even during 48 h.
Okada
Y
Y
Faculty of Pharmaceutical Sciences, Kobe Gakuin University, Japan. okada@pharm.kobegakuin.ac.jp
Tsuda
Y
Y
Wanaka
K
K
Tada
M
M
Okamoto
U
U
Okamoto
S
S
Hijikata-Okunomiya
A
A
Bokonyi
G
G
Szende
B
B
Keri
G
G
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D053148:Caspase 3; D020169:Caspases / Q000378:metabolism; D004151:Dipeptides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D005341:Fibrinolysin / Q000037:antagonists & inhibitors*; D019073:HT29 Cells; D006801:Humans; D015394:Molecular Structure; D020842:Plasma Kallikrein / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D004151:Dipeptides; C419204:YO 1 compound; C419205:YO 2 compound; D020842:Plasma Kallikrein; D005341:Fibrinolysin; C505407:CASP3 protein, human; D053148:Caspase 3; D020169:Caspases