Advances in inhibitor development targeting the PWWP domain

Trends Pharmacol Sci. 2024 Mar;45(3):193-196. doi: 10.1016/j.tips.2024.01.007. Epub 2024 Feb 9.

Abstract

The PWWP domain binds to both histone and DNA of a nucleosome in a bivalent way. PWWP domain-containing proteins are involved in different biological processes, and their aberrant expression is implicated in various human diseases. Here, we discuss the recent developments and challenges in targeting the PWWP domain for therapeutic intervention.

Keywords: PROTAC; PWWP domain; aromatic cage; nucleosome-binding.

MeSH terms

  • DNA* / metabolism
  • Histones* / metabolism
  • Humans
  • Protein Binding
  • Protein Domains

Substances

  • Histones
  • DNA