Open Access

Targeting complexes of super‑enhancers is a promising strategy for cancer therapy (Review)

  • Authors:
    • Chuqian Zheng
    • Min Liu
    • Hong Fan
  • View Affiliations

  • Published online on: July 10, 2020     https://doi.org/10.3892/ol.2020.11855
  • Pages: 2557-2566
  • Copyright: © Zheng et al. This is an open access article distributed under the terms of Creative Commons Attribution License.

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Abstract

The hyperactivation and overexpression of critical oncogenes is a common occurrence in multiple types of malignant tumors. Recently, the abnormal activation mechanism of an oncogene by a super‑enhancer (SE) has attracted significant attention. A series of changes (insertion, deletion, translocation and rearrangement) in the genome occurring in cancer cells may generate new SEs, leading to the overexpression of SE‑driven oncogenes. SEs are composed of typical enhancers densely loaded with mediator complexes, transcription factors, and chromatin regulators, and drive the overexpression of oncogenes associated with cellular identity and disease. Cyclin‑dependent kinase 7 (CDK7) and bromodomain protein 4 (BRD4) are critical mediator complexes associated with SE‑mediated transcription. Clinical trials have shown that emerging small‑molecule inhibitors (CDK7 and BRD4 inhibitor), targeting the SE exert a notable effect on cancer treatment. Increasing evidences has illustrated that the SE and its associated complexes play a critical role in the development of various types of cancer. The present review discusses the composition, function and regulation of SEs and their contribution to oncogenic transcription. In addition, creative therapeutic approaches that target SE, their advantages and disadvantages, as well as the problems with their clinical application are discussed. It was found that targeting SE may be used in conventional treatment and establish more access for patients with cancer.

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September-2020
Volume 20 Issue 3

Print ISSN: 1792-1074
Online ISSN:1792-1082

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Spandidos Publications style
Zheng C, Liu M and Fan H: Targeting complexes of super‑enhancers is a promising strategy for cancer therapy (Review). Oncol Lett 20: 2557-2566, 2020
APA
Zheng, C., Liu, M., & Fan, H. (2020). Targeting complexes of super‑enhancers is a promising strategy for cancer therapy (Review). Oncology Letters, 20, 2557-2566. https://doi.org/10.3892/ol.2020.11855
MLA
Zheng, C., Liu, M., Fan, H."Targeting complexes of super‑enhancers is a promising strategy for cancer therapy (Review)". Oncology Letters 20.3 (2020): 2557-2566.
Chicago
Zheng, C., Liu, M., Fan, H."Targeting complexes of super‑enhancers is a promising strategy for cancer therapy (Review)". Oncology Letters 20, no. 3 (2020): 2557-2566. https://doi.org/10.3892/ol.2020.11855