PROTEASE-INHIBITORY ACTIVITIES OF LEUPEPTIN ANALOGUES

Thirty analogues of leupeptin were synthesized and examined for their inhibitory activities against trypsin, papain, plasmin, kallikrein, thrombin and urokinase in vitro. Benzoyland α-naphthalenesulfonyl-L-leucyl-L-argininal were 8 times more inhibitory to papain, benzyloxycarbonyl-L-pyroglutamyl-L-...

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Bibliographic Details
Published in:Journal of antibiotics 1988/02/25, Vol.41(2), pp.220-225
Main Authors: SAINO, TETSUSHI, SOMENO, TETSUYA, ISHII, SHIN-ICHI, AOYAGI, TAKAAKI, UMEZAWA, HAMAO
Format: Article
Language:English
Subjects:
Analytical, structural and metabolic biochemistry
Biological and medical sciences
Enzymes and enzyme inhibitors
Fibrinolysin - antagonists & inhibitors
Fundamental and applied biological sciences. Psychology
Hydrolases
Kallikreins - antagonists & inhibitors
Leupeptins - chemical synthesis
Leupeptins - pharmacology
Oligopeptides - chemical synthesis
Papain - antagonists & inhibitors
Thrombin - antagonists & inhibitors
Trypsin Inhibitors
Urokinase-Type Plasminogen Activator - antagonists & inhibitors
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Summary:Thirty analogues of leupeptin were synthesized and examined for their inhibitory activities against trypsin, papain, plasmin, kallikrein, thrombin and urokinase in vitro. Benzoyland α-naphthalenesulfonyl-L-leucyl-L-argininal were 8 times more inhibitory to papain, benzyloxycarbonyl-L-pyroglutamyl-L-leucyl-L-argininal 10 times more to trypsin and plasmin, and DL-2-pipecolyl-L-leucyl-L-argininal 25 times more to kallikrein than leupeptin. Against urokinase, only L-pyroglutamyl-L-leucyl-L-argininal exhibited a potent inhibitory activity. α-Naphthalenesulfonyl-, dansyl- and benzyloxycarbonyl-(2S, 3R)-3-ammo-2-hydroxy-4-phenylbutyryl-L-leucyl-L-argininal were inhibitory to thrombin.
ISSN:0021-8820
1881-1469
DOI:10.7164/antibiotics.41.220