Polycomb and Trithorax Group Proteins: The Long Road from Mutations in Drosophila to Use in Medicine

Acta Naturae. 2020 Oct-Dec;12(4):66-85. doi: 10.32607/actanaturae.11090.

Abstract

Polycomb group (PcG) and Trithorax group (TrxG) proteins are evolutionarily conserved factors responsible for the repression and activation of the transcription of multiple genes in Drosophila and mammals. Disruption of the PcG/TrxG expression is associated with many pathological conditions, including cancer, which makes them suitable targets for diagnosis and therapy in medicine. In this review, we focus on the major PcG and TrxG complexes, the mechanisms of PcG/TrxG action, and their recruitment to chromatin. We discuss the alterations associated with the dysfunction of a number of factors of these groups in oncology and the current strategies used to develop drugs based on small-molecule inhibitors.

Keywords: Drosophila; EZH2 inhibitors; PRC2; PRC2 inhibitors; PRE; Polycomb; Trithorax; cancer, oncology; small-molecule inhibitors.