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- W2017011840 abstract "To evaluate the available peptidic and pseudopeptidic inhibitors of HIV protease for their possiblein vivoactivity, a screening test usingEscherichia coliwas established.E. colicells carrying the plasmid pET9c-PR containing the gene for HIV-1 protease under the control of a T7-promotor are grown in the absence and in the presence of inhibitors. The action of the toxic protease produced by the cells is counteracted by the inhibitors. Provided sufficient membrane permeability of the inhibitors exists, this results in accelerated cell growth. From the peptides known to be active in anin-vitroenzyme test, most compounds inhibit HIV protease only to a limited degree in this test. However, two short peptides (Ac-Ser-Tyr-Glu-Leu and Lys-Ile-Ser-Tyr-Asp-Tyr) protect cell growth to an considerabe extent, thus indicating that they reach theE. colicytosol and there block HIV protease. Two pseudopeptides known to be very potent in the enzyme test (SDZ PRI 053 and CIBA 61755) also inhibit HIV-1 protease strongly in this cell growth test." @default.
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- W2017011840 date "1997-04-01" @default.
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- W2017011840 title "Screening of Inhibitors of HIV-1 Protease Using anEscherichia coliCell Assay" @default.
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- W2017011840 doi "https://doi.org/10.1006/bbrc.1997.6403" @default.
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