BRADFORD SCHOLARS

    • Sign in
    View Item 
    •   Bradford Scholars
    • Life Sciences
    • Life Sciences Publications
    • View Item
    •   Bradford Scholars
    • Life Sciences
    • Life Sciences Publications
    • View Item
    JavaScript is disabled for your browser. Some features of this site may not work without it.

    Browse

    All of Bradford ScholarsCommunitiesAuthorsTitlesSubjectsPublication DateThis CollectionAuthorsTitlesSubjectsPublication Date

    My Account

    Sign in

    HELP

    Bradford Scholars FAQsCopyright Fact SheetPolicies Fact SheetDeposit Terms and ConditionsDigital Preservation Policy

    Statistics

    Most Popular ItemsStatistics by CountryMost Popular Authors

    Probing cytochrome P450-mediated activation with a truncated azinomycin analogue

    • CSV
    • RefMan
    • EndNote
    • BibTex
    • RefWorks
    Thumbnail
    View/Open
    medchemcomm_2015.pdf (609.6Kb)
    Download
    Publication date
    2015
    Author
    Vinader, Victoria
    Sadiq, Maria
    Sutherland, Mark H.
    Huang, M.Y.
    Loadman, Paul M.
    Elsalem, Lina M.I.
    Shnyder, Steven D.
    Cui, H.J.
    Afarinkia, Kamyar
    Searcey, M.
    Patterson, Laurence H.
    Pors, Klaus
    Show allShow less
    Keyword
    Antitumor antibiotics
    ; Sequence selectivity
    ; Colon-cancer
    ; cyp2w1
    ; DNA
    ; Cytotoxicity
    ; Expression
    ; Mechanism
    ; Epoxide
    ; Liver
    Rights
    (c) 2015 Royal Society of Chemistry. Full-text reproduced in accordance with the publisher's self-archiving policy.
    Peer-Reviewed
    Yes
    
    Metadata
    Show full item record
    Abstract
    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.
    URI
    http://hdl.handle.net/10454/9419
    Version
    Accepted manuscript
    Citation
    Vinader V, Sadiq M, Sutherland M et al (2015) Probing cytochrome P450-mediated activation with a truncated azinomycin analogue. MedChemComm. 6(1): 187-191.
    Link to publisher’s version
    http://dx.doi.org/10.1039/c4md00411f
    Type
    Article
    Collections
    Life Sciences Publications

    entitlement

     
    DSpace software (copyright © 2002 - 2023)  DuraSpace
    Quick Guide | Contact Us
    Open Repository is a service operated by 
    Atmire NV
     

    Export search results

    The export option will allow you to export the current search results of the entered query to a file. Different formats are available for download. To export the items, click on the button corresponding with the preferred download format.

    By default, clicking on the export buttons will result in a download of the allowed maximum amount of items.

    To select a subset of the search results, click "Selective Export" button and make a selection of the items you want to export. The amount of items that can be exported at once is similarly restricted as the full export.

    After making a selection, click one of the export format buttons. The amount of items that will be exported is indicated in the bubble next to export format.