Biomedicine & Pharmacotherapy (Oct 2023)

TET protein inhibitors: Potential and limitations

  • Robert Kaplánek,
  • Zdeněk Kejík,
  • Jan Hajduch,
  • Kateřina Veselá,
  • Kateřina Kučnirová,
  • Markéta Skaličková,
  • Anna Venhauerová,
  • Božena Hosnedlová,
  • Róbert Hromádka,
  • Petr Dytrych,
  • Petr Novotný,
  • Nikita Abramenko,
  • Veronika Antonyová,
  • David Hoskovec,
  • Petr Babula,
  • Michal Masařík,
  • Pavel Martásek,
  • Milan Jakubek

Journal volume & issue
Vol. 166
p. 115324

Abstract

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TET proteins (methylcytosine dioxygenases) play an important role in the regulation of gene expression. Dysregulation of their activity is associated with many serious pathogenic states such as oncological diseases. Regulation of their activity by specific inhibitors could represent a promising therapeutic strategy. Therefore, this review describes various types of TET protein inhibitors in terms of their inhibitory mechanism and possible applicability. The potential and possible limitations of this approach are thoroughly discussed in the context of TET protein functionality in living systems. Furthermore, possible therapeutic strategies based on the inhibition of TET proteins are presented and evaluated, especially in the field of oncological diseases.

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