Nobiletin targets CHEK1-H3K27ac-CENPM axis and suppresses the malignancy of colorectal cancer
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ABSTRACT: Pharmacological intervention targeting super-enhancer activity represents a promising therapeutic approach to suppress the expression of oncogenes. The challenges remain in unveiling the key factors accounting for the hyperactive super-enhancers in cancers and small molecules for the functional inhibition. In this study, we identified CHEK1 as a critical factor for sustaining the high level H3K27ac enrichment in the super-enhancer regions of oncogenes. Nobiletin was found as an inhibitor of CHEK1. We made these findings in the efforts to decipher the molecular mechanism underlying a modified Traditional Chinese Medicine formula Liujunzi Decoctiom (mLJZD). We experimentally confirmed the anti-cancer function of mLJZD both in vitro and in vivo. Through an interactive analysis of RNA profiling data, we identified oncogenic CENPM as a critical effector gene that is downregulated by mLJZD
ORGANISM(S): Mus musculus
PROVIDER: GSE298436 | GEO | 2026/05/31
REPOSITORIES: GEO
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