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Targeting bromodomain and extra-terminal proteins to inhibit neuroblastoma tumorigenesis through regulating MYCN

Xiyao Shi1,2, Ying Wang3, Longhui Zhang1,2

  • 1Key Laboratory of Organ Regeneration and Transplantation of Ministry of Education, First Hospital, Jilin University, Changchun, China.

Frontiers in Cell and Developmental Biology
|October 3, 2022
PubMed

Insights

Bromodomain and extra-terminal domain (BET) proteins regulate genes driving cancer. BET inhibitors show promise for treating MYCN-amplified neuroblastoma, with research exploring resistance mechanisms and combination therapies.

Area of Science:

  • Oncology
  • Epigenetics
  • Molecular Biology

Background:

  • Bromodomain and extra-terminal domain (BET) proteins are epigenetic readers involved in gene expression.
  • Dysregulation of BET proteins contributes to proto-oncogene activation, promoting cancer progression.
  • BET proteins are validated therapeutic targets in various cancers, including neuroblastoma.

Purpose of the Study:

  • To review the critical function of BET proteins in tumorigenesis.
  • To summarize the therapeutic potential of BET/BRD4 inhibitors in MYCN-amplified neuroblastoma.
  • To discuss combined therapeutic strategies for overcoming BET inhibitor resistance.

Main Methods:

  • Literature review of recent research on BET proteins and neuroblastoma.
  • Analysis of the role of BET proteins as epigenetic readers in cancer.
  • Evaluation of therapeutic strategies targeting BET/BRD4 in MYCN-amplified neuroblastoma.

Main Results:

  • BET proteins critically regulate gene expression, impacting tumor cell proliferation, survival, metastasis, and immune escape.
  • BET/BRD4 inhibitors are a key therapeutic strategy for MYCN-amplified neuroblastoma.
  • Understanding BET protein function is crucial for developing effective cancer treatments.

Conclusions:

  • BET proteins are essential epigenetic regulators in cancer development.
  • BET/BRD4 inhibitors represent a promising therapeutic avenue for MYCN-amplified neuroblastoma.
  • Future research should focus on combination therapies to address treatment resistance.
Keywords:
BET family proteinsBRD4 inhibitorsMYCNepigenetic regulationneuroblastoma

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