Article

Cyclin A/B RxL Macrocyclic Inhibitors to Treat Cancers with High E2F Activity

2024-08-01

Abstract excerpt

Cancer cell proliferation requires precise control of E2F1 activity; excess activity promotes apoptosis. Here, we developed cell-permeable and bioavailable macrocycles that selectively kill small cell lung cancer (SCLC) cells with inherent high E2F1 activity by blocking RxL-mediated interactions of cyclin A and cyclin B with select substrates. Genome-wide CRISPR/Cas9 knockout and random mutagenesis screens found t...

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Literature Corpus work: ebee179a-710d-59f8-bfe5-4de7df2e4b5d
DOI: 10.1101/2024.08.01.605889

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