Molecular Mechanisms of Epigenetic Regulators as Activatable Targets in Cancer Theranostics

Yinglu Li1,2, Zhiming Li1,2, Wei-Guo Zhu1,2

  • 1Shenzhen University School of Medicine, Shenzhen 518060, China.

Current Medicinal Chemistry
|September 22, 2017
PubMed

Insights

Epigenetics, inheritable changes without DNA alteration, is crucial in cancer. Understanding epigenetic modifications, especially histone modifications, offers new diagnostic and therapeutic strategies for cancer.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Epigenetics involves heritable changes in gene expression without altering DNA sequence, including DNA methylation and histone modifications.
  • Aberrant epigenetic alterations are key drivers in cancer development, influencing malignant transformation, metastasis, and drug resistance.

Purpose of the Study:

  • To summarize the critical roles of epigenetics, particularly histone modifications, in cancer diagnostics and therapeutics.
  • To discuss the implications of activatable epigenetic targets for cancer theranostics.

Main Methods:

  • Review of current literature on epigenetics and histone modifications in cancer.
  • Analysis of the role of histone modification enzymes and their inhibitors in tumorigenesis and treatment.

Main Results:

  • Abnormal epigenetic changes are integral to cancer progression and recurrence.
  • Histone modifications and associated enzymes are linked to cancer incidence and patient prognosis.
  • Several histone modification inhibitors are in clinical use or under investigation.

Conclusions:

  • Epigenetic insights, especially regarding histone modifications, provide valuable targets for cancer diagnosis and therapy.
  • Activatable epigenetic targets hold promise for advancing cancer theranostics.

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