Histone methyltransferase and drug resistance in cancers

Cheng Yang1,2, Jiayu Zhang1,2, Yukui Ma3

  • 1Department of Pharmacology, Shenyang Pharmaceutical University, Shenyang, People's Republic of China.

Insights

Novel anticancer drugs face challenges from emerging drug resistance. Targeting histone methyltransferases offers a promising strategy to overcome this resistance and improve cancer treatment outcomes.

Area of Science:

  • Oncology
  • Epigenetics
  • Pharmacology

Background:

  • Despite advances in novel anticancer drugs, cancer patient mortality remains high due to acquired drug resistance.
  • Drug resistance mechanisms can involve epigenetic modifications, such as changes in gene expression without altering DNA sequence.
  • Histone methyltransferases (HMTs) play a role in these epigenetic changes and have been implicated in cancer drug resistance.

Purpose of the Study:

  • To review the current understanding of how histone methyltransferases contribute to cancer drug resistance.
  • To explore therapeutic strategies targeting histone methyltransferases to reverse or overcome drug resistance.

Main Methods:

  • Literature review of studies investigating histone methyltransferases and cancer drug resistance.
  • Analysis of mechanisms by which HMTs influence drug resistance.
  • Summary of therapeutic approaches targeting HMTs for cancer treatment.

Main Results:

  • Histone methyltransferases are involved in regulating gene expression patterns that lead to drug resistance in various cancers.
  • Targeting HMTs, through inhibition or other strategies, has shown potential in preclinical models to restore sensitivity to anticancer drugs.
  • Specific HMTs have been identified as key players in resistance to different classes of chemotherapeutics.

Conclusions:

  • Histone methyltransferases represent a critical target for overcoming cancer drug resistance.
  • Inhibitors of histone methyltransferases offer a viable therapeutic avenue for enhancing the efficacy of existing anticancer treatments.
  • Further research into HMTs and their role in drug resistance is crucial for developing next-generation cancer therapies.

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