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Items: 1 to 20 of 99

1.

Development of a Selective Inhibitor of Protein Arginine Deiminase 2.

Muth A, Subramanian V, Beaumont E, Nagar M, Kerry P, McEwan P, Srinath H, Clancy K, Parelkar S, Thompson PR.

J Med Chem. 2017 Apr 13;60(7):3198-3211. doi: 10.1021/acs.jmedchem.7b00274. Epub 2017 Mar 31.

2.

Protein arginine deiminase 2 binds calcium in an ordered fashion: implications for inhibitor design.

Slade DJ, Fang P, Dreyton CJ, Zhang Y, Fuhrmann J, Rempel D, Bax BD, Coonrod SA, Lewis HD, Guo M, Gross ML, Thompson PR.

ACS Chem Biol. 2015 Apr 17;10(4):1043-53. doi: 10.1021/cb500933j. Epub 2015 Jan 26.

3.

Design, synthesis, and biological evaluation of tetrazole analogs of Cl-amidine as protein arginine deiminase inhibitors.

Subramanian V, Knight JS, Parelkar S, Anguish L, Coonrod SA, Kaplan MJ, Thompson PR.

J Med Chem. 2015 Feb 12;58(3):1337-44. doi: 10.1021/jm501636x. Epub 2015 Jan 16.

4.

A fluoroacetamidine-based inactivator of protein arginine deiminase 4: design, synthesis, and in vitro and in vivo evaluation.

Luo Y, Knuckley B, Lee YH, Stallcup MR, Thompson PR.

J Am Chem Soc. 2006 Feb 1;128(4):1092-3.

5.

Substrate specificity and kinetic studies of PADs 1, 3, and 4 identify potent and selective inhibitors of protein arginine deiminase 3.

Knuckley B, Causey CP, Jones JE, Bhatia M, Dreyton CJ, Osborne TC, Takahara H, Thompson PR.

Biochemistry. 2010 Jun 15;49(23):4852-63. doi: 10.1021/bi100363t.

6.

D-amino acid based protein arginine deiminase inhibitors: Synthesis, pharmacokinetics, and in cellulo efficacy.

Bicker KL, Anguish L, Chumanevich AA, Cameron MD, Cui X, Witalison E, Subramanian V, Zhang X, Chumanevich AP, Hofseth LJ, Coonrod SA, Thompson PR.

ACS Med Chem Lett. 2012 Oct 26;3(12):1081-1085.

7.

Increased levels of peptidylarginine deiminase 2 in synovial fluid from anti-CCP-positive rheumatoid arthritis patients: Association with disease activity and inflammatory markers.

Damgaard D, Senolt L, Nielsen CH.

Rheumatology (Oxford). 2016 May;55(5):918-27. doi: 10.1093/rheumatology/kev440. Epub 2016 Feb 15.

8.

Peptidomimetics as protein arginine deiminase 4 (PAD4) inhibitors.

Trabocchi A, Pala N, Krimmelbein I, Menchi G, Guarna A, Sechi M, Dreker T, Scozzafava A, Supuran CT, Carta F.

J Enzyme Inhib Med Chem. 2015 Jun;30(3):466-71. doi: 10.3109/14756366.2014.947976. Epub 2014 Sep 8.

PMID:
25198885
9.

Inhibitors and inactivators of protein arginine deiminase 4: functional and structural characterization.

Luo Y, Arita K, Bhatia M, Knuckley B, Lee YH, Stallcup MR, Sato M, Thompson PR.

Biochemistry. 2006 Oct 3;45(39):11727-36.

10.

Inhibitors of protein arginine deiminases and their efficacy in animal models of multiple sclerosis.

Sarswat A, Wasilewski E, Chakka SK, Bello AM, Caprariello AV, Muthuramu CM, Stys PK, Dunn SE, Kotra LP.

Bioorg Med Chem. 2017 May 1;25(9):2643-2656. doi: 10.1016/j.bmc.2017.03.006. Epub 2017 Mar 6.

PMID:
28341402
11.

Protein arginine deiminase 4 (PAD4): Current understanding and future therapeutic potential.

Jones JE, Causey CP, Knuckley B, Slack-Noyes JL, Thompson PR.

Curr Opin Drug Discov Devel. 2009 Sep;12(5):616-27. Review.

12.

A FluoPol-ABPP PAD2 high-throughput screen identifies the first calcium site inhibitor targeting the PADs.

Lewallen DM, Bicker KL, Madoux F, Chase P, Anguish L, Coonrod S, Hodder P, Thompson PR.

ACS Chem Biol. 2014 Apr 18;9(4):913-21. doi: 10.1021/cb400841k. Epub 2014 Jan 27.

13.

GnRH Stimulates Peptidylarginine Deiminase Catalyzed Histone Citrullination in Gonadotrope Cells.

Khan SA, Edwards BS, Muth A, Thompson PR, Cherrington BD, Navratil AM.

Mol Endocrinol. 2016 Oct;30(10):1081-1091. Epub 2016 Sep 7.

14.

Photochemical Control of Protein Arginine Deiminase (PAD) Activity.

Mondal S, Parelkar SS, Nagar M, Thompson PR.

ACS Chem Biol. 2018 Apr 20;13(4):1057-1065. doi: 10.1021/acschembio.8b00053. Epub 2018 Mar 16.

PMID:
29517899
15.

PAD2 Activity Monitored via a Fluorescent Substrate Analog.

Sabulski MJ, Wang Y, Pires MM.

Chem Biol Drug Des. 2015 Oct;86(4):599-605. doi: 10.1111/cbdd.12526. Epub 2015 Feb 16.

PMID:
25643806
16.

N-α-benzoyl-N5-(2-chloro-1-iminoethyl)-L-ornithine amide, a protein arginine deiminase inhibitor, reduces the severity of murine collagen-induced arthritis.

Willis VC, Gizinski AM, Banda NK, Causey CP, Knuckley B, Cordova KN, Luo Y, Levitt B, Glogowska M, Chandra P, Kulik L, Robinson WH, Arend WP, Thompson PR, Holers VM.

J Immunol. 2011 Apr 1;186(7):4396-404. doi: 10.4049/jimmunol.1001620. Epub 2011 Feb 23.

17.

Mechanistic studies of protein arginine deiminase 2: evidence for a substrate-assisted mechanism.

Dreyton CJ, Knuckley B, Jones JE, Lewallen DM, Thompson PR.

Biochemistry. 2014 Jul 15;53(27):4426-33. doi: 10.1021/bi500554b. Epub 2014 Jul 3.

18.

Reactive oxygen species inhibit catalytic activity of peptidylarginine deiminase.

Damgaard D, Bjørn ME, Jensen PØ, Nielsen CH.

J Enzyme Inhib Med Chem. 2017 Dec;32(1):1203-1208. doi: 10.1080/14756366.2017.1368505.

19.

Noncovalent Protein Arginine Deiminase (PAD) Inhibitors Are Efficacious in Animal Models of Multiple Sclerosis.

Tejeda EJC, Bello AM, Wasilewski E, Koebel A, Dunn S, Kotra LP.

J Med Chem. 2017 Nov 9;60(21):8876-8887. doi: 10.1021/acs.jmedchem.7b01102. Epub 2017 Oct 30.

PMID:
29045782
20.

A fluopol-ABPP HTS assay to identify PAD inhibitors.

Knuckley B, Jones JE, Bachovchin DA, Slack J, Causey CP, Brown SJ, Rosen H, Cravatt BF, Thompson PR.

Chem Commun (Camb). 2010 Oct 14;46(38):7175-7. doi: 10.1039/c0cc02634d. Epub 2010 Aug 25.

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