Abstract
Eight peptides of the general H-D-Ser-AA-Arg-OH formula, where AA = phenylglycine, phenylalanine, homophenylalanine, cyclohexylglycine, cyclohexylalanine, homocyclohexylalanine, α-methylphenylalanine and 1-aminocyclohexyl carboxylic acid were obtained and tested for their effect on the amidolytic activities of urokinase, thrombin, trypsin, plasmin, t-PA and kallikrein. We tested the hemolytic activity of the peptides against porcine erythrocytes and the antitumor activity against the human breast cancer cells, standard MCF-7 and estrogen-independent MDA-MB-231. The most active compounds were H-D-Ser-Chg-Arg-OH towards thrombin and H-D-Ser-Phg-Arg-OH towards plasmin with K(i) value 5.02 μM and 5.7 μM, respectively.
MeSH terms
-
Animals
-
Antineoplastic Agents / chemistry
-
Antineoplastic Agents / pharmacology
-
Breast Neoplasms / drug therapy
-
Breast Neoplasms / pathology
-
Cell Line, Tumor
-
Erythrocytes / drug effects
-
Female
-
Fibrinolysin / antagonists & inhibitors
-
Humans
-
Kallikreins / antagonists & inhibitors
-
Oligopeptides / chemistry*
-
Oligopeptides / pharmacology*
-
Serine Proteinase Inhibitors / chemistry*
-
Serine Proteinase Inhibitors / pharmacology*
-
Swine
-
Thrombin / antagonists & inhibitors
-
Tissue Plasminogen Activator / antagonists & inhibitors
-
Trypsin Inhibitors / chemistry
-
Trypsin Inhibitors / pharmacology
-
Urokinase-Type Plasminogen Activator / antagonists & inhibitors
Substances
-
Antineoplastic Agents
-
Oligopeptides
-
Serine Proteinase Inhibitors
-
Trypsin Inhibitors
-
Kallikreins
-
Thrombin
-
Tissue Plasminogen Activator
-
Fibrinolysin
-
Urokinase-Type Plasminogen Activator