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A PROTAC Targets Splicing Factor 3B1

ABSTRACT: The proteolysis-targeting chimera (PROTAC) is a new technology to degrade a target protein. However, its clinical application is limited currently by lack of chemical binders to target protein. For instance, it is still unknown, whether splicing factor 3B subunit 1 (SF3B1) is targetable by PROTACs. We recently identified a 2-aminothiazole derivative (herein O4I2) to promote the generation of human pluripotent stem cells. In the present work, proteomic analysis on the biotinylated O4I2 revealed that O4I2 targeted SF3B1 and positively regulated RNA splicing.

INSTRUMENT(S): Orbitrap Fusion Lumos

ORGANISM(S): Homo Sapiens (human)

TISSUE(S): Epithelial Cell

SUBMITTER: Georg Tascher

LAB HEAD: Xinlai Cheng

PROVIDER: PXD024661 | Pride | 2022-08-08

REPOSITORIES: Pride

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A PROTAC targets splicing factor 3B1.

Gama-Brambila Rodrigo A RA Chen Jie J Zhou Jun J Tascher Georg G Münch Christian C Cheng Xinlai X

Cell chemical biology 20210527 11

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) is targetable by PROTACs. We recently identified a 2-aminothiazole derivative (herein O4I2) as a promoter in the generation of human pluripotent stem cells. In this work, proteomic analysis on the biotinylated O4I2 reveale ...[more]

PMID: 34048672

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