The Indenoisoquinoline LMP517: A Novel Antitumor Agent Targeting both TOP1 and TOP2.
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SUBMITTER: Marzi L
PROVIDER: S-EPMC7415565 | biostudies-literature | 2020 Aug
REPOSITORIES: biostudies-literature
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The Indenoisoquinoline LMP517: A Novel Antitumor Agent Targeting both TOP1 and TOP2.
Marzi Laetitia L Sun Yilun Y Huang Shar-Yin N SN James Amy A Difilippantonio Simone S Pommier Yves Y
Molecular cancer therapeutics 20200519 8
The camptothecin derivatives topoisomerase I (TOP1) inhibitors, irinotecan and topotecan, are FDA approved for the treatment of colorectal, ovarian, lung and breast cancers. Because of the chemical instability of camptothecins, short plasma half-life, drug efflux by the multidrug-resistance ABC transporters, and the severe diarrhea produced by irinotecan, indenoisoquinoline TOP1 inhibitors (LMP400, LMP776, and LMP744), which overcome these limitations, have been developed and are in clinical dev ...[more]
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