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Bromodomain-containing protein BRPF1 is a therapeutic target for liver cancer
Carol Lai-Hung Cheng1,2, Felice Hoi-Ching Tsang1,2, Lai Wei1,2
1State Key Laboratory of Liver Research, The University of Hong Kong, Pok Fu Lam, Hong Kong.
Abstract:
Epigenetic deregulation plays an essential role in hepatocellular carcinoma (HCC) progression. Bromodomains are epigenetic "readers" of histone acetylation. Recently, bromodomain inhibitors have exhibited promising therapeutic potential for cancer treatment. Using transcriptome sequencing, we identified BRPF1 (bromodomain and PHD finger containing 1) as the most significantly upregulated gene among the 43 bromodomain-containing genes in human HCC. BRPF1 upregulation was significantly associated with poor patient survival. Gene ablation or pharmacological inactivation of BRPF1 significantly attenuated HCC cell growth in vitro and in vivo. BRPF1 was involved in cell cycle progression, senescence and cancer stemness. Transcriptome sequencing revealed that BRPF1 is a master regulator controlling the expression of multiple key oncogenes, including E2F2 and EZH2. We demonstrated that BRPF1 activated E2F2 and EZH2 expression by facilitating promoter H3K14 acetylation through MOZ/MORF complex. In conclusion, BRPF1 is frequently upregulated in human HCCs. Targeting BRPF1 may be an approach for HCC treatment.
Insights
Bromodomain and PHD finger containing 1 (BRPF1) is upregulated in hepatocellular carcinoma (HCC), driving cancer progression. Targeting BRPF1 shows therapeutic potential for treating HCC by inhibiting cell growth and oncogene expression.
Area of Science:
- Oncology
- Epigenetics
- Molecular Biology
Background:
- Epigenetic alterations are crucial in hepatocellular carcinoma (HCC) development.
- Bromodomains, as epigenetic readers of histone acetylation, are emerging therapeutic targets in cancer.
- BRPF1 is identified as a significantly upregulated bromodomain-containing gene in HCC.
Purpose of the Study:
- To investigate the role of BRPF1 in hepatocellular carcinoma (HCC) progression.
- To explore the therapeutic potential of targeting BRPF1 in HCC treatment.
Main Methods:
- Transcriptome sequencing to identify differentially expressed bromodomain genes in HCC.
- Gene ablation and pharmacological inhibition of BRPF1.
- Analysis of BRPF1's role in cell cycle, senescence, and cancer stemness.
- Investigating BRPF1's regulatory mechanism on oncogenes E2F2 and EZH2 via histone acetylation.
Main Results:
- BRPF1 was the most significantly upregulated bromodomain gene in HCC and associated with poor patient survival.
- BRPF1 inhibition attenuated HCC cell growth in vitro and in vivo.
- BRPF1 regulates cell cycle, senescence, and cancer stemness.
- BRPF1 acts as a master regulator, activating oncogenes E2F2 and EZH2 expression through MOZ/MORF-mediated H3K14 acetylation.
Conclusions:
- BRPF1 is frequently overexpressed in human HCC and plays a critical role in its progression.
- Targeting BRPF1 presents a promising therapeutic strategy for hepatocellular carcinoma treatment.
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