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- W4234108782 abstract "<div>The small molecule gibberellin JRA-003 (1) was identified as an inhibitor of the NF-kB (nuclear kappa-light-chain enhancer of activated B cells) pathway. Here we find that JRA-003 binds to and significantly inhibits the nuclear translocation of pathway-activating kinases IKKalpha (IkB kinase alpha) and IKKbeta (IkB kinase beta). Analogs were synthesized and NF-kB-inhibiting gibberellins were found to be cytotoxic in cancer-derived cell lines (HS 578T, HCC 1599, RC-K8, Sud-HL4, CA 46, and NCIH 4466). Not only was JRA-003 (1) identified as the most potent synthetic gibberellin against cancer-derived cell lines, it displayed no cytotoxicity in cells derived from non-cancerous sources (HEK 293T, HS 578BST, HS 888Lu, HS 895Sk, HUVEC). This selectivity suggests a promising approach for the development of new therapeutics.</div>" @default.
- W4234108782 created "2022-05-12" @default.
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- W4234108782 date "2019-12-20" @default.
- W4234108782 modified "2023-09-24" @default.
- W4234108782 title "Gibberellin JRA-003: A Selective Inhibitor of Nuclear Translocation of IKKalpha" @default.
- W4234108782 doi "https://doi.org/10.26434/chemrxiv.11374338" @default.
- W4234108782 hasPublicationYear "2019" @default.
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