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Updated: May 8, 2026

Engineering Artificial Factors to Specifically Manipulate Alternative Splicing in Human Cells
Published on: April 26, 2017
Remediating cancer via splicing modulation
1Division of Chemistry and Structural Biology, Institute for Molecular Bioscience, The University of Queensland , St. Lucia, Brisbane, 4072, Australia.
Abstract:
The identification of three distinct but structurally related classes of microbial-derived spliceosome modulators has provided an exciting opportunity for the development of mechanistically new cancer treatments. A team at UC San Diego has undertaken a SAR study on the spliceosome modulator FD-895 that focused on improving compound stability, while retaining potent antiproliferative and splicing activity. This led to the identification of a more potent and stable analog, (17S)-FD-895 (1), and a less active but extremely stable cyclopropane analog 2, which is currently undergoing preclinical evaluation. These analogs will serve as templates for next generation spliceosome modulating anticancer drugs.
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