Related Experiment Video
Updated: Dec 10, 2025

Author Spotlight: Epigenetic Modifications and Metabolic Rewiring as Targets for Cancer Therapy
Published on: October 18, 2024
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.
Abstract:
A number of novel anticancer drugs have been developed in recent years. However, the mortality of cancer patients remains high because of the emergence of drug resistance. It was reported that drug resistance might involved in changes in gene expression without changing genotypes, which is similar to epigenetic modification. Some studies indicated that targeting histone methyltransferase can reverse drug resistance. Hence, the use of histone methyltransferase inhibitors or histone demethylase inhibitors opens new therapeutic approaches for cancer treatment. While the relationship between histone methyltransferase and tumor resistance has been determined, there is a lack of updated review on the association between them. In this review, we summarized the mechanisms of histone methyltransferases in cancer drug resistance and the therapeutic strategies of targeting histone methyltransferase to reverse drug resistance.
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.
More Related Videos
08:46Implementation of In Vitro Drug Resistance Assays: Maximizing the Potential for Uncovering Clinically Relevant Resistance Mechanisms
Published on: December 9, 2015
14:51Pooled shRNA Library Screening to Identify Factors that Modulate a Drug Resistance Phenotype
Published on: June 17, 2022
Related Concept Videos
Treatment Resistant Cancers
Targeted Cancer Therapies
There are several types of targeted therapies against...
Epigenetic Regulation
X-chromosome...
Epigenetic Regulation
Drugs that Stabilize Microtubules
Cancer Stem Cells and Tumor Maintenance
Cancer stem cells are thought to originate from tissue-specific normal stem cells or progenitor cells. The normal stem cells usually reside in...