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The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
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Treating human cancer by targeting EZH2.

Mengfei Xu1,2, Chunyan Xu1, Rui Wang1,2

  • 1The Second Clinical Medical College, Guangzhou University of Chinese Medicine, Guangzhou, Guangdong 510120, China.

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|March 3, 2025
PubMed
Summary
This summary is machine-generated.

Enhancer of zeste homolog 2 (EZH2) is an oncogene overexpressed in tumors, driving cancer progression. Targeting EZH2 is crucial for cancer therapy, though clinical applications face challenges.

Keywords:
CancerEZH2EZH2 inhibitorEpigenetic modificationH3K27me3

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Area of Science:

  • Oncology
  • Epigenetics
  • Molecular Biology

Background:

  • Enhancer of zeste homolog 2 (EZH2) is an epigenetic regulator overexpressed in various tumors.
  • EZH2 acts as an oncogene, promoting tumor occurrence, development, invasion, migration, drug resistance, and impacting anti-tumor immunity.
  • Elevated EZH2 expression in cancer is facilitated by cooperating transcription factors and RNAs.

Purpose of the Study:

  • To clarify the critical importance of targeting EZH2 in cancer treatment.
  • To summarize the current research landscape of targeted EZH2 inhibitors.
  • To offer insights into potential future applications of EZH2 inhibitors in oncology.

Main Methods:

  • This review synthesizes current research on EZH2's role in cancer.
  • Literature review focusing on EZH2's function, overexpression mechanisms, and therapeutic targeting.
  • Analysis of existing and potential EZH2 inhibitors and their clinical challenges.

Main Results:

  • EZH2 plays a multifaceted role as an oncogene in cancer progression and metastasis.
  • Several factors contribute to EZH2 overexpression in malignant tumors.
  • Targeting EZH2 holds significant therapeutic potential despite current clinical hurdles.

Conclusions:

  • Targeting EZH2 is a promising strategy for cancer therapy due to its oncogenic functions.
  • Overcoming challenges in the clinical application of EZH2 inhibitors is essential for effective cancer treatment.
  • Further research into EZH2 inhibitors may unlock new therapeutic avenues for various cancers.