PAD4 Inhibitor Screening Assay Kit

Cayman Chemical Item Number 700560

Protein Arginine Deiminase 4; Peptidylarginine Deiminase 4

Description

Protein Arginine Deiminase 4 (PAD4) is a guanidino-modifying enzyme that functions as a transcriptional coregulator catalyzing the conversion of specific arginine residues to citrulline. Substrates for PAD4 include histones H2A, H3, and H4. PAD4 autocitrullinates itself at several sites, inhibiting its enzymatic activity. PAD4 activity is increased in rheumatoid arthritis, producing an abundance of citrulline-containing proteins that generate an immune response resulting in production of autoantibodies that ultimately attack the host tissues. PAD4 has also been implicated in several other diseases including multiple sclerosis, Alzheimer’s disease, glaucoma, and cancer. Cayman’s PAD4 Inhibitor Screening Assay provides a convenient, fluorescence-based method for screening human PAD4 inhibitors.

Synonyms

Protein Arginine Deiminase 4
Peptidylarginine Deiminase 4

Stability

6 months

Storage

-80°C

Shipping

Dry ice in continental US; may vary elsewhere

Background Reading

Shirai, H., Blundell, T.L., and Mizuguchi, K. A novel superfamily of enzymes that catalyze the modification of guanidino groups. Trends Biochem Sci 26(8) 465-468 (2001).

Knuckley, B., Luo, Y., and Thompson, P.R. Profiling protein arginine deiminase 4 (PAD4): A novel screen to identify PAD4 inhibitors. Bioorg Med Chem 16(2) 739-45 (2008).

Hill, J.A., Southwood, S., Sette, A., et al. Cutting edge: The conversion of arginine to citrulline allows for a high-affinity peptide interaction with the rheumatoid arthritis-associated HLA-DRB1*0401 MHC class II molecule. J Immunol 171 538-541 (2003).

Jones, J.E., Causey, C.P., Knuckley, B., et al. Protein arginine deiminase 4 (PAD4): Current understanding and future therapeutic potential. Curr Opin Drug Discov Devel 12(5) 616-627 (2009).

Andrade, F., Darrah, E., Gucek, M., et al. Autocitrullination of human peptidylarginine deiminase 4 regulates protein citrullination during cell activation. Arthritis Rheum (2010).

Kearney, P.L., Bhatia, M., Jones, N.G., et al. Kinetic characterization of protein arginine deiminase 4: A transcriptional corepressor implicated in the onset and progression of rheumatoid arthritis. Biochemistry 44 10570-10582 (2005).

Slack, J.L., Causey, C.P., and Thompson, P.R. Protein arginine deiminase 4: A target for an epigenetic cancer therapy. Cell Mol Life Sci 68(4) 709-720 (2011).

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700560-96well

96-Well Cover Sheet