Phosphinic acid-based inhibitors of tubulin polyglycylation

Chem Commun (Camb). 2022 Jun 1;58(45):6530-6533. doi: 10.1039/d2cc01783k.

Abstract

Tubulin polyglycylation is a posttranslational modification that occurs primarily on the axonemes of flagella and cilia and has been shown to be essential for proper sperm motility. Inhibitors of both the initiase and elongase ligases (TTLL8 and TTLL10) are shown to inhibit tubulin glycylation in the low micromolar range.

MeSH terms

  • Cilia / metabolism
  • Humans
  • Male
  • Microtubules / metabolism
  • Phosphinic Acids*
  • Protein Processing, Post-Translational
  • Sperm Motility
  • Tubulin* / metabolism

Substances

  • Phosphinic Acids
  • Tubulin