2018
DOI: 10.1007/82_2018_132
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Development of Activity-Based Proteomic Probes for Protein Citrullination

Abstract: 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 var… Show more

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Cited by 8 publications
(8 citation statements)
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References 78 publications
(130 reference statements)
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“…Reversible PAD4 inhibitors are chemically more diverse, and rely on different mechanisms of PAD4 inhibition, such as guanidine‐containing compounds that interact with PAD4 active site residues (Figure 4C) and compounds that occupy both the “front door” and “back door” of the U‐shaped tunnel. This topic is extensively covered in a recent article by Nemmara and Thompson 99 . The different modes of action of irreversible and reversible PAD4 inhibitors are described in Figure 4.…”
Section: Pad4 Inhibitionmentioning
confidence: 99%
See 1 more Smart Citation
“…Reversible PAD4 inhibitors are chemically more diverse, and rely on different mechanisms of PAD4 inhibition, such as guanidine‐containing compounds that interact with PAD4 active site residues (Figure 4C) and compounds that occupy both the “front door” and “back door” of the U‐shaped tunnel. This topic is extensively covered in a recent article by Nemmara and Thompson 99 . The different modes of action of irreversible and reversible PAD4 inhibitors are described in Figure 4.…”
Section: Pad4 Inhibitionmentioning
confidence: 99%
“…This topic is extensively covered in a recent article by Nemmara and Thompson. 99 The different modes of action of irreversible and reversible PAD4 inhibitors are described in Figure 4 . In conclusion, it appears very difficult to design PAD inhibitors to have a high selectivity for the PAD4 isotype in combination with achieving high potency.…”
Section: Pad4 Inhibitionmentioning
confidence: 99%
“…More recent efforts also include the development of specific PAD inhibitors, targeting for instance PAD2 or PAD4, as well as non-covalent reversible inhibitors. For a detailed overview of all developed PAD inhibitors we refer to a recent review specifically focusing on these developments (197).…”
Section: Targeting Citrullination: Types Of Pad Inhibitors and Their Potential As Therapeutic Agent In Preclinical Models Of Autoimmunitymentioning
confidence: 99%
“…68 Furthermore, PAD isoform-selective inhibitors have been developed. 69,70 For example, D-Cl-amidine demonstrates decent selectivity for PAD1. 71 A benzimidazole-based derivative of Cl-amidine shows excellent selectivity for and inhibition of PAD2.…”
Section: Pad-mediated Citrullination Of Histones In Cancermentioning
confidence: 99%
“…Additional pan‐PAD inhibitors have also been reported and developed, such as the Cl‐amidine derivative YW3‐56 67 and furan‐containing peptide‐based inhibitors 68 . Furthermore, PAD isoform‐selective inhibitors have been developed 69,70 . For example, D‐Cl‐amidine demonstrates decent selectivity for PAD1 71 .…”
Section: Therapeutic Potential Of Pad Inhibitorsmentioning
confidence: 99%