منابع مشابه
Bifunctional inhibitors of pepsin.
Two bifunctional reagents designed to probe the active site of pepsin and other acid proteinases are described. One of these, the bisdiazoketone 1,1-bis(diazoacetyl)-2-phenylethane inactivates pepsin at pH 5.0 much more rapidly than the corresponding monodiazoketon 1-diazoacetyl-2-phenylethane, whereas the other, the bromodiazoketone dl-1-diazoacetyl-1-bromo-2-phenylethane is less effective in ...
متن کاملPepsin Inhibitors from Ascaris Zumbricoides
Extracts of the body walls of the adult Ascaris lumbricoides var. suis inhibit pepsin between pH 1 and 6. Four inhibitors of pepsin were isolated and purified as follows. The crude extract of Ascaris was incubated at 37” and pH 2.0 for 75 min. The pepsin-inhibiting activity was obtained in a fraction precipitated at 0.65 saturation with ammonium sulfate at pH 5.35, and sequentially chromatograp...
متن کاملThe effect of acid proteinase inhibitors on chicken pepsin.
1. The activity of chicken pepsin was partially inhibited by dimethyl-(2-hydroxy-5-nitrobenzyl)sulphonium bromide, but was unaffected by p-bromophenacyl bromide. 2. In the presence of Cu2+, diazoacetylnorleucine methyl ester completely inactivated chicken pepsin with the incorporation of 1 mol/mol. The mechanism of the reaction was similar to that with pig pepsin. 3. Chicken pepsin was complete...
متن کاملBifunctional thrombin inhibitors based on the sequence of hirudin45-65.
The interaction of alpha-thrombin with the hirudin (HV1) fragment N alpha-acetyl desulfo hirudin45-65 (P51) was investigated. Kinetic analysis revealed that P51 inhibits the proteolysis of a tripeptidyl substrate with Ki = 0.72 +/- 0.13 and 0.11 +/- 0.03 microM for bovine and human alpha-thrombins, respectively. The inhibition was partially competitive, affecting substrate binding to the enzyme...
متن کاملBifunctional phenolic-choline conjugates as anti-oxidants and acetylcholinesterase inhibitors.
Because of the complex cascade of molecular events that can occur in the brain of an Alzheimer's disease (AD) patient, the therapy of this neurodegenerative disease seems more likely to be achieved by multifunctional drugs. Herein, a new series of dual-targeting ligands have been developed and in vitro bioevaluated. Their architecture is based on conjugating the acetylcholinesterase inhibition ...
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ژورنال
عنوان ژورنال: Proceedings of the National Academy of Sciences
سال: 1971
ISSN: 0027-8424,1091-6490
DOI: 10.1073/pnas.68.11.2765