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Article

Electrophile Determines Cellular Phenotypes among XPO1-Targeting Small Molecules.

Journal of medicinal chemistry - 25 Jul 2024

Chen Yi Fan, Shen Yanqiu, Yan David F, Ghazala Maryam, Scemama de Gialluly Marc A, Srinivasan Ramya, Farrar Amanda N, Friedrich Ryan M, Adams Drew J

Abstract excerpt

Covalent drug discovery has experienced a renaissance, with numerous electrophilic small molecules recently gaining FDA approval. Many structurally diverse electrophilic small molecules target exportin-1 (XPO1/CRM1) at cysteine 528, including the selective inhibitor of nuclear export (SINE) selinexor, which was FDA-approved as an anticancer agent in 2019. Emerging evidence supports additional pharmacological...

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Identifiers

PMID: 39005064
DOI: 10.1021/acs.jmedchem.4c00754

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