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  • About
  • The Global ETD Search service is a free service for researchers to find electronic theses and dissertations. This service is provided by the Networked Digital Library of Theses and Dissertations.
    Our metadata is collected from universities around the world. If you manage a university/consortium/country archive and want to be added, details can be found on the NDLTD website.

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Spelling suggestions: "subject:"antitumor antibiotic"" "subject:"intitumor antibiotic""

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Probing cytochrome P450-mediated activation with a truncated azinomycin analogue

Vinader, Victoria, Sadiq, Maria, Sutherland, Mark, Huang, M.Y., Loadman, Paul, Elsalem, Lina M.I., Shnyder, Steven, Cui, H.J., Afarinkia, Kamyar, Searcey, M., Patterson, Laurence H., Pors, Klaus 2014 October 1922 (has links)
Yes / A deactivated alkene precursor (IC50=81 mu M) to the azinomycin epoxide natural product can be bioactivated by several cytochromes P450 (CYP) to generate antiproliferative metabolites with increased potency (IC50=1-30 mu M) in CHOwt cells. CYP1A1 and 3A4 were shown to generate exclusively the unnatural and the natural-configured azinomycin epoxide diastereoisomer respectively, while CYP1B1 produced both epoxides in a 3:1 mixture. The antiproliferative activity is linked to DNA damage as demonstrated using the comet assay.
Antitumor antibiotics
Sequence selectivity
Colon-cancer
cyp2w1
DNA
Cytotoxicity
Expression
Mechanism
Epoxide
Liver

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