DNA methylation inhibitors in cancer: recent and future approaches

Christina Gros1, Jacques Fahy, Ludovic Halby

  • 1USR CNRS-Pierre Fabre n° 3388-ETaC Epigenetic Targeting of Cancer, CRDPF 3 avenue Hubert Curien, 31035 Toulouse Cedex 01, France.

Biochimie
|September 13, 2012
PubMed

Insights

This review covers human DNA methyltransferases (DNMTs) and their role in cancer. It details DNMT inhibitors (DNMTi), their clinical trials, and future directions for cancer therapy.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • DNA methyltransferases (DNMTs) are crucial enzymes involved in epigenetic regulation.
  • Aberrant DNA methylation is a hallmark of various cancers.
  • Understanding DNMTs is key to developing targeted cancer therapies.

Purpose of the Study:

  • To review human DNA methyltransferases (DNMTs), their functions, and their involvement in cancer.
  • To describe assays for identifying DNMT inhibitors (DNMTi).
  • To summarize current DNMTi, their clinical applications, and future prospects.

Main Methods:

  • Literature review of DNMTs, their roles in cancer, and DNMT inhibitors.
  • Analysis of existing assays for DNMT inhibitor screening.
  • Compilation of data on DNMTi clinical trials and their outcomes.

Main Results:

  • Detailed overview of human DNMTs, including their biological functions and mechanisms.
  • Description of various assays used to detect DNMT inhibitors.
  • Summary of known DNMT inhibitors, highlighting their pros, cons, and clinical trial status.

Conclusions:

  • DNMTs play a significant role in cancer development and progression.
  • DNMT inhibitors represent a promising therapeutic strategy for cancer treatment.
  • Further research into novel DNMT inhibitors is warranted for improved cancer therapies.

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