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| Sousa,M.O.; Miranda,T.L.S.; Costa,E.B.; Bittar,E.R.; Santoro,M.M.; Figueiredo,A.F.S.. |
| Hydrolysis of D-valyl-L-leucyl-L-arginine p-nitroanilide (7.5-90.0 µM) by human tissue kallikrein (hK1) (4.58-5.27 nM) at pH 9.0 and 37ºC was studied in the absence and in the presence of increasing concentrations of 4-aminobenzamidine (96-576 µM), benzamidine (1.27-7.62 mM), 4-nitroaniline (16.5-66 µM) and aniline (20-50 mM). The kinetic parameters determined in the absence of inhibitors were: Km = 12.0 ± 0.8 µM and k cat = 48.4 ± 1.0 min-1. The data indicate that the inhibition of hK1 by 4-aminobenzamidine and benzamidine is linear competitive, while the inhibition by 4-nitroaniline and aniline is linear mixed, with the inhibitor being able to bind both to the free enzyme with a dissociation constant Ki yielding an EI complex, and to the ES complex with... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Kinetics of human tissue kallikrein inhibition; Tissue kallikrein; 4-nitroaniline; Aniline; Benzamidine; 4-aminobenzamidine; Enzyme inhibition. |
| Ano: 2001 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2001000100004 |
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