Breast anticancer drug tamoxifen and its metabolites bind DNA and RNA at multiple sites - Tajmir-Riahi, Heidar-Ali
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Tamoxifen is a breast anticancer drug that has been in worldwide use for the treatment of estrogen receptor (ER)-positive breast cancer for over 30 years. We compare the binding sites of the tamoxifen and its metabolites 4-hydroxytamoxifen and endoxifen with DNA and tRNA. Structural models showed that tamoxifen and its metabolites bind DNA and tRNA at multiple sites via hydrophobic, hydrophilic and H-bonding contacts with tRNA forming more stable drug conjugates than DNA. Drug conjugation did not alter DNA and tRNA conformations, while major biopolymer aggregation occurred at high drug…mehr

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Produktbeschreibung
Tamoxifen is a breast anticancer drug that has been in worldwide use for the treatment of estrogen receptor (ER)-positive breast cancer for over 30 years. We compare the binding sites of the tamoxifen and its metabolites 4-hydroxytamoxifen and endoxifen with DNA and tRNA. Structural models showed that tamoxifen and its metabolites bind DNA and tRNA at multiple sites via hydrophobic, hydrophilic and H-bonding contacts with tRNA forming more stable drug conjugates than DNA. Drug conjugation did not alter DNA and tRNA conformations, while major biopolymer aggregation occurred at high drug contents. The drug loading efficacy is correlated with the mechanism of action of antitumor activity of tamoxifen and its metabolites.
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Autorenporträt
Tajmir-Riahi H.A. Research Professor at University of Quebec in Trois-Rivieres (UQTR) Canada. Research interest 1. Drug interactions with DNA, RNA and proteins. 2. Drug delivery by natural and synthetic polymers, using microscopic and spectroscopic analysis. I have 300 publications in international journals with 3 books and 10 book chapters.