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Yeast Chemogenomic Profiling Reveals Iron Chelation to Be the Principle Cell Inhibitory Mode of Action of Gossypol

Prescott, Thomas A.K. and Jaeg, Tiphaine and Hoepfner, Dominic (2018) Yeast Chemogenomic Profiling Reveals Iron Chelation to Be the Principle Cell Inhibitory Mode of Action of Gossypol. Journal of Medicinal Chemistry, 61 (16). pp. 7381-7386. ISSN 15204804

Abstract

Gossypol is an inhibitor of eukaryotic cells with an undetermined mode of action. Here we show that the chemogenomic profile of gossypol is strikingly similar to that of the iron chelators deferasirox and desferricoprogen. Iron import channels Fet1 and Fet3 are prominent in all three profiles. Furthermore, yeast inhibited by gossypol and deferasirox is rescued by the addition of Fe2+. We propose that Fe2+ chelation is in fact the principle mode of action of gossypol.

Item Type: Article
Date Deposited: 02 Oct 2018 00:45
Last Modified: 02 Oct 2018 00:45
URI: https://oak.novartis.com/id/eprint/35560

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