Cell permeable degrader of splicing factor 3B1 (SF3B1)
SF3B1 Protein degrader (reported as "PROTAC-O4I2" in Gama-Brambila et al.) is a cell permeable degrader of splicing factor 3B1 (SF3B1) containing an SF3B1 activator O4I2 connected to the ligand of the cereblon ubiquitin ligase thalidomide. PROTAC-O4I2 selectively degrades SF3B1 in cells. It induces apoptosis of tumor cells and extends survival in Drosophila intestinal tumor model.
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PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license
Cell chemical biology, 28(11), 1616-1627 (2021-05-29)
The proteolysis-targeting chimeras (PROTACs) are a new technology to degrade target proteins. However, their clinical application is limited currently by lack of chemical binders to target proteins. For instance, it is still unknown whether splicing factor 3B subunit 1 (SF3B1)
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