In vitro embryotoxicity of the cysteine proteinase inhibitors benzyloxycarbonyl-phenylalanine-alanine-diazomethane (Z-Phe-Ala-CHN2) and benzyloxycarbony1-phenylalanine-phenylalanine-diazomethane (Z-Phe-Phe-CHN2)
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منابع مشابه
Inhibition of cysteine proteinases in lysosomes and whole cells.
Inhibitors of cysteine proteinases have been used extensively to dissect the roles of these proteinases in cells. Surprisingly though, little work has been performed to demonstrate unequivocally that the inhibitors reach and inactivate their target proteinases in cell culture or in vivo. In the present study, the permeability of lysosomes and whole cells has been studied. Benzyloxycarbonyl (Z)-...
متن کاملThe cysteine proteinase inhibitor Z-Phe-Ala-CHN2 alters cell morphology and cell division activity of Trypanosoma brucei bloodstream forms in vivo
BACKGROUND Current chemotherapy of human African trypanosomiasis or sleeping sickness relies on drugs developed decades ago, some of which show toxic side effects. One promising line of research towards the development of novel anti-trypanosomal drugs are small-molecule inhibitors of Trypanosoma brucei cysteine proteinases. RESULTS In this study, we demonstrate that treatment of T. brucei-inf...
متن کاملSynthesis and properties of Cbz-Phe-Arg-CHN2 (benzyloxycarbonylphenylalanylarginyldiazomethane) as a proteinase inhibitor.
The preparation of peptides terminating in -Arg-CHN2 has been attempted because of their potential value as proteinase inactivators. We have succeeded in one case, converting Cbz-Phe-ArgOH to the diazomethane without blocking the guanidino group. As expected from previous results with such reagents, the new derivative was extremely effective in inactivating a cysteine proteinase specific for cl...
متن کاملInfinite pleated -sheet formed by the -hairpin Boc- -Phe- -Phe-D-Pro-Gly- -Phe- -Phe-OMe
A -hairpin conformation and extended -pleated sheet assembly have been characterized by single crystal x-ray diffraction for the synthetic peptide t-butoxycarbonyl— -Phe-Phe-D-Pro-GlyPhe-Phe-methyl ester [ -Phe: (S)3 homophenylalanine]. The centrally located D-Pro-Gly segment nucleates a chain reversal in a type II -turn conformation. Two intramolecular cross-strand hydrogen bonds stabilize the...
متن کاملZ-Phe-Gly-NHO-Bz, an inhibitor of cysteine cathepsins, induces apoptosis in human cancer cells.
An increasing number of studies indicate that cysteine cathepsins contribute to cancer progression, invasion, and metastasis. Here we provide experimental evidence that the cathepsin inhibitor Z-Phe-Gly-NHO-Bz induces rapid apoptotic death in human cancer cell lines. Notably, the Z-Phe-Gly-NHO-Bz-induced apoptosis exhibited independence of p53, caspases, and mitogen-activated protein (MAP) kina...
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ژورنال
عنوان ژورنال: Teratology
سال: 1994
ISSN: 0040-3709,1096-9926
DOI: 10.1002/tera.1420500307