Highly Efficient Cell-Penetrating Probes of Protein Arginine Deiminases for Functional Proteomics

Chembiochem. 2018 Sep 4;19(17):1806-1809. doi: 10.1002/cbic.201800257. Epub 2018 Jul 23.

Abstract

Protein arginine deiminases (PADs) have recently emerged at the forefront of drug-discovery programs for several human disorders. Despite this, a precise understanding of their functional roles in human biology remains to be fully elucidated. This report highlights a recent development of next-generation activity-based PAD probes that are highly efficient, cell active, and metabolically stable. This discovery should rapidly expedite functional assignments of PAD biology in both normal and diseased cells, thereby leading to the development of PAD-targeted therapeutics in the near future.

Keywords: activity-based probes; autoimmune diseases; post-translational modifications; protein arginine deiminase; protein citrullination.

Publication types

  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Catalytic Domain
  • Click Chemistry
  • Humans
  • Molecular Probes / chemistry*
  • Protein-Arginine Deiminases / chemistry*
  • Protein-Arginine Deiminases / metabolism*
  • Proteomics / methods

Substances

  • Molecular Probes
  • Protein-Arginine Deiminases