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Updated: Aug 11, 2026

Peptide-based Identification of Functional Motifs and their Binding Partners
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TET protein inhibitors: Potential and limitations

Robert Kaplánek1, Zdeněk Kejík1, Jan Hajduch1

  • 1BIOCEV, First Faculty of Medicine, Charles University, Průmyslová 595, 252 50 Vestec, Czech Republic; Department of Paediatrics and Inherited Metabolic Disorders, First Faculty of Medicine, Charles University and General University Hospital in Prague, Ke Karlovu 455/2, 128 08 Prague, Czech Republic.

Biomedicine & Pharmacotherapy = Biomedecine & Pharmacotherapie
|August 20, 2023
PubMed

Insights

This review explores Ten-Eleven Translocation (TET) protein inhibitors for cancer therapy. It details their mechanisms, applications, and limitations, offering insights into novel therapeutic strategies for oncological diseases.

Area of Science:

  • Biochemistry and Molecular Biology
  • Epigenetics
  • Oncology

Background:

  • Ten-Eleven Translocation (TET) proteins are crucial regulators of gene expression through DNA demethylation.
  • Aberrant TET protein activity is implicated in the pathogenesis of various cancers.
  • Targeting TET proteins with inhibitors presents a potential therapeutic avenue for oncological diseases.

Purpose of the Study:

  • To review and categorize different types of TET protein inhibitors.
  • To analyze the inhibitory mechanisms and potential applications of these compounds.
  • To evaluate the therapeutic strategies and limitations of TET inhibition in cancer treatment.

Main Methods:

  • Literature review of existing studies on TET protein inhibitors.
  • Analysis of inhibitory mechanisms, including competitive and allosteric inhibition.
  • Evaluation of preclinical and clinical data regarding TET inhibitor efficacy and safety.

Main Results:

  • Various classes of TET inhibitors have been identified, differing in their molecular targets and modes of action.
  • Inhibitors show promise in preclinical cancer models by modulating epigenetic landscapes.
  • Challenges include achieving specificity, managing off-target effects, and understanding complex in vivo functionality.

Conclusions:

  • TET protein inhibitors offer a promising, albeit complex, strategy for cancer therapy.
  • Further research is needed to optimize inhibitor design and fully elucidate their therapeutic potential and limitations.
  • Targeted inhibition of TET proteins could lead to novel epigenetic therapies for various cancers.
Keywords:
CancerInhibitorMitochondriaTET proteinTherapy

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