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Current and potential anticancer drugs targeting members of the UHRF1 complex including epigenetic modifiers

Motoko Unoki1

  • 1Laboratory for Biomarker Development, The Institute of Physical and Chemical Research, Center for Genomic Medicine, RIKEN, Tokyo 108-8639, Japan. unokim@ims.u-tokyo.ac.jp

Recent Patents on Anti-Cancer Drug Discovery
|November 30, 2010
PubMed

Insights

Epigenetic modulators like UHRF1 are crucial in cancer development. This review discusses patents on developing safer anticancer drugs targeting the UHRF1 complex to mitigate adverse effects.

Area of Science:

  • Oncology
  • Epigenetics
  • Drug Discovery

Background:

  • Epigenetic modulators, including DNA methylation and histone modifications, are key drivers of carcinogenesis.
  • Many epigenetic enzymes and DNA methyltransferases (DNMTs) are overexpressed in cancer cells, promoting malignant transformation.
  • Current cancer drugs often target oncogenic proteins, but epigenetic alterations also contribute to cancer via aberrant modulator expression.

Purpose of the Study:

  • To review patents on strategies for developing safer anticancer drugs.
  • To focus on targeting epigenetic modulators, particularly the UHRF1 complex and its associated proteins.
  • To explore novel therapeutic approaches for cancer treatment by modulating epigenetic machinery.

Main Methods:

  • Literature review of patents related to epigenetic modulators and cancer therapy.
  • Analysis of the role of UHRF1 in linking DNA methylation and histone modifications.
  • Identification of UHRF1 complex members (e.g., HDAC1, G9a, DNMTs) and their involvement in cancer.

Main Results:

  • UHRF1, upregulated in various cancers, bridges DNA methylation and histone modifications.
  • The UHRF1 complex comprises enzymes like HDAC1, G9a, and DNMTs, many implicated in carcinogenesis.
  • Existing epigenetic drugs (HDAC and DNMT inhibitors) show efficacy but have adverse reactions.

Conclusions:

  • Developing safer anticancer drugs targeting epigenetic modulators, especially the UHRF1 complex, is a critical area of research.
  • Patent strategies are emerging to overcome the limitations of current epigenetic therapies.
  • Targeting UHRF1 and its modifiers offers a promising avenue for novel cancer treatments with potentially reduced side effects.

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