Synthesis and use of novel inhibitors and inactivators of...

Details Synthesis and use of novel inhibitors and inactivators of... Synthesis and use of novel inhibitors and inactivators of...

2011-06-21

2011-06-21

Henley, III, Raymond J (Department: 1614)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

Reexamination Certificate

active

07964636

ABSTRACT:
In one embodiment of the present disclosure, an inactivator of protein arginine deiminase 4 is disclosed. The inactivator includes: (I) and x includes F; Cl, and H, y includes OH and NH2, R includes H, an alkyl group, an alkenyl group, an alknyl group, and n is greater than 0.

REFERENCES:
Kearney et al., “Kinetic Characterization of Protein Arginine Deiminase 4: A Transcriptional Corepressor Implicated in the Onset and Progression of Rheumatoid Arthritis”, Biochemistry, vol. 44, No. 31, pp. 10570-10582, (2005).
Luo, Y. et al., “A Fluoroacetamidine-Based Inactivator of Protein Arginine Deiminase 4: Design, Synthesis, and in Vitro and in Vivo Evaluation”, J. Am. Chem. Soc., vol. 128, No. 4, pp. 1092-1093, (2006).
Luo, Y. et al., “Inhibitors and Inactivators of Protein Arginine Deiminase 4: Functional and Structural Characterization”, Biochemistry, vol. 45, No. 39, pp. 11727-11736, (2006).
Luo, Y. et al., “Activity-Basted Protein Profiling Reagents for Protein Arginine Deiminase 4 (PAD4): Synthesis and in vitro Evaluation of a Fluorescently Labeled Probe”, J. Am. Chem. Soc., vol. 128, No. 45, pp. 14468-14469, (2006).
Thompson et al., “Histone Citrullination by Protein Arginine Deiminase: Is Arginine Methylation a Green Light or a Roadblock?”, ACS Chemical Biology, vol. 1, No. 7, pp. 433-441, (2006).

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