Development of Activity-Based Proteomic Probes for Protein Citrullination

  • Venkatesh V. Nemmara
  • Paul R. ThompsonEmail author
Part of the Current Topics in Microbiology and Immunology book series (CT MICROBIOLOGY, volume 420)


Protein arginine deiminases (PADs) catalyze the post-translational deimination of peptidyl arginine to form peptidyl citrulline. This modification is increased in multiple inflammatory diseases and in certain cancers. PADs regulate a variety of signaling pathways including apoptosis, terminal differentiation, and transcriptional regulation. Activity-based protein profiling (ABPP) probes have been developed to understand the role of the PADs in vivo and to investigate the effect of protein citrullination in various pathological conditions. Furthermore, these ABPPs have been utilized as a platform for high-throughput inhibitor discovery. This review will showcase the development of ABPPs targeting the PADs. In addition, it provides a brief overview of PAD structure and function along with recent advances in PAD inhibitor development.


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© Springer Nature Switzerland AG 2018

Authors and Affiliations

  1. 1.Department of Biochemistry and Molecular PharmacologyUniversity of Massachusetts Medical SchoolWorcesterUSA
  2. 2.Program in Chemical BiologyUniversity of Massachusetts Medical SchoolWorcesterUSA

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