Targeting DUBs to degrade oncogenic proteins

Br J Cancer. 2020 Apr;122(8):1121-1123. doi: 10.1038/s41416-020-0728-7. Epub 2020 Feb 4.

Abstract

Targeted protein degradation has emerged as a strategy in cancer therapy. Yang et al. discovered that HBX19818, an inhibitor of the deubiquitinase (DUB) USP10, leads to the dual degradation of spleen tyrosine kinase (SYK) and FLT3, resulting in death of AML cells.

Publication types

  • Editorial
  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Humans
  • Leukemia, Myeloid, Acute / drug therapy*
  • Leukemia, Myeloid, Acute / pathology
  • Syk Kinase / metabolism*
  • Ubiquitin Thiolesterase / antagonists & inhibitors*
  • fms-Like Tyrosine Kinase 3 / metabolism*

Substances

  • USP10 protein, human
  • FLT3 protein, human
  • fms-Like Tyrosine Kinase 3
  • SYK protein, human
  • Syk Kinase
  • Ubiquitin Thiolesterase