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Selective degradation of histone deacetylase 8 mediated by a proteolysis targeting chimera (PROTAC).

Jiranan ChotitumnaveeYasunobu YamashitaYukari TakahashiYuri TakadaTetsuya IidaMakoto ObaYukihiro ItohTakayoshi Suzuki
Published in: Chemical communications (Cambridge, England) (2022)
We developed a first-in-class proteolysis targeting chimera (PROTAC) for selective degradation of histone deacetylase 8 (HDAC8). The PROTAC induced degradation of HDAC8 without affecting the levels of other HDACs in cellular assays, and inhibited the growth of T-cell leukemia Jurkat cells more potently than a conventional HDAC8 inhibitor.
Keyphrases
  • histone deacetylase
  • induced apoptosis
  • cancer therapy
  • cell cycle arrest
  • bone marrow
  • diabetic rats
  • oxidative stress
  • drug delivery
  • signaling pathway