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AZD7762 induces CRBN dependent BAG3 degradation through ubiquitin-proteasome pathway.


ABSTRACT: Protein degraders are currently under rapid development as a promising modality for drug discovery. They are compounds that orchestrate interactions between a target protein and an E3 ubiquitin ligase, prompting intracellular protein degradation through proteasomal pathway. More protein degraders identification will greatly promote the development of this field. BAG3 is widely recognized as an excellent therapeutic target in cancer treatments. Exploring protein degraders that target BAG3 degradation has profound implications. Herein, molecular docking was applied to assess binding energy between 81 clinical phase I kinase inhibitors and BAG3. BAG3 protein and mRNA level were detected by western blot and quantitative real-time PCR. CCK8 assay and colony formation assay were applied to detec

SUBMITTER: Liao Y 

PROVIDER: S-EPMC10720835 | biostudies-literature | 2023 Jul

REPOSITORIES: biostudies-literature