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. 2022 Oct 24;23(21):12815. doi: 10.3390/ijms232112815

Table 3.

Targeted therapies that directly target the aberrant chromatin remodelers as anticancer agents.

Directly Targets Associated Cancers Directly Targeted Agents
SMARCA4 and SMARCA2 Glioblastoma PFI-3 targets the essential bromodomain and blocks SWI/SNF’s chromatin binding [167,168].
SMARCA2 and SMARCA4 SMARCA4-deficient lung-cancer; uveal melanoma A dual allosteric small-molecule inhibitor targets ATPase activity of SMARCA2 and SMARCA4 [169].
SMARCA2 and SMARCA4 AR/FOXA1-driven prostate cancer AU-15330 is a proteolysis-targeting chimera degrader of the SMARCA2 and SMARCA4 [170].
SMARCA2 and SMARCA4 SMARCA4-mutant lung cancer SMASh degron-mediated SMARCA2 depletion [171].
SMARCA2, SMARCA4, and PBRM1 Unknown GNE-064 is a chemical probe targeting the bromodomains SMARCA2, SMARCA4, and PBRM1 [172].
PBAF complex Unknown LM146 targets the PBAF complex component by blocking the specific bromodomains within the complex [173].
BRD7/9 Unknown Compounds LP99 is selective inhibitor of the BRD7 and BRD9 bromodomains [174].
BRD7/9 Unknown VZ185 is a selective and rapid degrader of BRD9 and of its close homolog BRD7 [175].
BRD7/9 Unknown GSK6776 as a soluble and selective BRD7/9 inhibitor [176].
BRD9 AML xenograft model BI-7273 and BI-956456 are potent and selective BRD9 bromodomain inhibitors [177].
BRD9 Unknown GNE-375 is a small-molecule inhibitor of the BRD9 bromodomain [178].
BRD9 Human AML I-BRD9 is BRD9 bromodomain inhibitor [179].
BRD9 Human AML Compound dBRD9 bridges the BRD9 bromodomain and the E3 ubiquitin ligase complex for degradation [180].
BPTF Breast cancer cells Compound BZ1 targets the BPTF bromodomain [181].
BPTF Lung cancer cells Compounds Cpd8 and Cpd10 are highly potent and selective inhibitors of the BPTF bromodomain [22].