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Yuh Min Chook on Muck Rack

Yuh Min Chook

As seen in: Nature
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Preclinical characterization of a reversible XPO1 inhibitor for cancer therapy

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By Janne van Hauwenhuyse, Felien Reniers, Leentje Persoons, Sam Noppen, Casey E. Wing, Ashley B Niesman, Els Vanstreels, Maarten Jacquemyn, Ann Vankerckhoven, Yani Berckmans, Bert Kwanten, An Coosemans, Wim Dehaen, Dirk Daelemans, Eline Boel, Guy Van den Mooter, Yuh Min Chook
| Nature Verified
Abstract Exportin 1 (XPO1/CRM1) is a clinically validated anticancer target whose inhibition blocks nuclear export and promotes cancer cell apoptosis. Current XPO1 inhibitors rely on covalent Michael addition to Cys528 in the nuclear export signal binding groove of XPO1. Here, we describe a novel XPO1 inhibitor, FR-027, that targets Cys528 through nucleophilic aromatic substitution.
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