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prenyl transferase

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PEB 3233 TIAB SA-3409 AZD-3409 yog ib qho muaj zog prenyl transferase inhibitor. AZD-3409 pom muaj zog dua li lonafarnib. Qhov nruab nrab IC (50) rau cytotoxicity ntawm AZD3409 yog 510 hauv MEF hlwb, 10,600 hauv A549 hlwb thiab 6,170 hauv MCF7 hlwb, feem. Hauv cov hlwb no, IC(50) rau FTase kev ua ntawm AZD3409 ranged ntawm 3.0 txog 14.2 nM thiab ntawm lonafarnib los ntawm 0.26 txog 31.3 nM. AZD3409 inhibits farnesylation mus rau ntau dua li geranylgeranylation. Ob leeg inhibition ntawm farnesylation thiab geranylgeranylation tsis tuaj yeem cuam tshuam nrog kev ua haujlwm ntawm cov tshuaj tiv thaiv kab mob. AZD3409 tej zaum yuav ua haujlwm hauv gefitinib-resistant mis carcinoma.
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