Potent SMARCA2 targeted degraders induce genetic synthetic lethality in SMARCA4 deleted cancer
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K Ito, A Agarwal, P Pitis, M Wang, J Carter…
Cancer …, 2021
aacrjournals.org
SWI/SNF complexes play an important role in controlling gene expression by remodeling chromatin. SMARCA2 (BRM) and SMARCA4 (BRG1) are the core subunits of the SWI/SNF complexes which contain ATPase domain and DNA binding bromodomain. SMARCA4 protein expression is lost in some cancers due to damaging mutations (eg nonsense, frameshift deletion, splice site mutations) and SMARCA4-deleted cancer cells are highly dependent on its paralog gene SMARCA2 for their survival. Therefore, targeting SMARCA2 …
