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Items: 1 to 20 of 193

1.

Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050.

Fridman JS, Scherle PA, Collins R, Burn TC, Li Y, Li J, Covington MB, Thomas B, Collier P, Favata MF, Wen X, Shi J, McGee R, Haley PJ, Shepard S, Rodgers JD, Yeleswaram S, Hollis G, Newton RC, Metcalf B, Friedman SM, Vaddi K.

J Immunol. 2010 May 1;184(9):5298-307. doi: 10.4049/jimmunol.0902819. Epub 2010 Apr 2.

2.

VX-509 (decernotinib) is a potent and selective janus kinase 3 inhibitor that attenuates inflammation in animal models of autoimmune disease.

Mahajan S, Hogan JK, Shlyakhter D, Oh L, Salituro FG, Farmer L, Hoock TC.

J Pharmacol Exp Ther. 2015 May;353(2):405-14. doi: 10.1124/jpet.114.221176. Epub 2015 Mar 11.

3.

INCB16562, a JAK1/2 selective inhibitor, is efficacious against multiple myeloma cells and reverses the protective effects of cytokine and stromal cell support.

Li J, Favata M, Kelley JA, Caulder E, Thomas B, Wen X, Sparks RB, Arvanitis A, Rogers JD, Combs AP, Vaddi K, Solomon KA, Scherle PA, Newton R, Fridman JS.

Neoplasia. 2010 Jan;12(1):28-38.

4.

Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases.

Van Rompaey L, Galien R, van der Aar EM, Clement-Lacroix P, Nelles L, Smets B, Lepescheux L, Christophe T, Conrath K, Vandeghinste N, Vayssiere B, De Vos S, Fletcher S, Brys R, van 't Klooster G, Feyen JH, Menet C.

J Immunol. 2013 Oct 1;191(7):3568-77. doi: 10.4049/jimmunol.1201348. Epub 2013 Sep 4.

5.

Anti-inflammatory properties of a novel N-phenyl pyridinone inhibitor of p38 mitogen-activated protein kinase: preclinical-to-clinical translation.

Hope HR, Anderson GD, Burnette BL, Compton RP, Devraj RV, Hirsch JL, Keith RH, Li X, Mbalaviele G, Messing DM, Saabye MJ, Schindler JF, Selness SR, Stillwell LI, Webb EG, Zhang J, Monahan JB.

J Pharmacol Exp Ther. 2009 Dec;331(3):882-95. doi: 10.1124/jpet.109.158329. Epub 2009 Aug 31.

6.

Periodic, partial inhibition of IkappaB Kinase beta-mediated signaling yields therapeutic benefit in preclinical models of rheumatoid arthritis.

Gillooly KM, Pattoli MA, Taylor TL, Chen L, Cheng L, Gregor KR, Whitney GS, Susulic V, Watterson SH, Kempson J, Pitts WJ, Booth-Lute H, Yang G, Davies P, Kukral DW, Strnad J, McIntyre KW, Darienzo CJ, Salter-Cid L, Yang Z, Wang-Iverson DB, Burke JR.

J Pharmacol Exp Ther. 2009 Nov;331(2):349-60. doi: 10.1124/jpet.109.156018. Epub 2009 Aug 3.

7.

Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition.

Telliez JB, Dowty ME, Wang L, Jussif J, Lin T, Li L, Moy E, Balbo P, Li W, Zhao Y, Crouse K, Dickinson C, Symanowicz P, Hegen M, Banker ME, Vincent F, Unwalla R, Liang S, Gilbert AM, Brown MF, Hayward M, Montgomery J, Yang X, Bauman J, Trujillo JI, Casimiro-Garcia A, Vajdos FF, Leung L, Geoghegan KF, Quazi A, Xuan D, Jones L, Hett E, Wright K, Clark JD, Thorarensen A.

ACS Chem Biol. 2016 Dec 16;11(12):3442-3451. Epub 2016 Nov 10.

PMID:
27791347
8.

Selective functional inhibition of JAK-3 is sufficient for efficacy in collagen-induced arthritis in mice.

Lin TH, Hegen M, Quadros E, Nickerson-Nutter CL, Appell KC, Cole AG, Shao Y, Tam S, Ohlmeyer M, Wang B, Goodwin DG, Kimble EF, Quintero J, Gao M, Symanowicz P, Wrocklage C, Lussier J, Schelling SH, Hewet AG, Xuan D, Krykbaev R, Togias J, Xu X, Harrison R, Mansour T, Collins M, Clark JD, Webb ML, Seidl KJ.

Arthritis Rheum. 2010 Aug;62(8):2283-93. doi: 10.1002/art.27536.

9.

The novel kinase inhibitor PRT062070 (Cerdulatinib) demonstrates efficacy in models of autoimmunity and B-cell cancer.

Coffey G, Betz A, DeGuzman F, Pak Y, Inagaki M, Baker DC, Hollenbach SJ, Pandey A, Sinha U.

J Pharmacol Exp Ther. 2014 Dec;351(3):538-48. doi: 10.1124/jpet.114.218164. Epub 2014 Sep 24.

10.

Preclinical evaluation of local JAK1 and JAK2 inhibition in cutaneous inflammation.

Fridman JS, Scherle PA, Collins R, Burn T, Neilan CL, Hertel D, Contel N, Haley P, Thomas B, Shi J, Collier P, Rodgers JD, Shepard S, Metcalf B, Hollis G, Newton RC, Yeleswaram S, Friedman SM, Vaddi K.

J Invest Dermatol. 2011 Sep;131(9):1838-44. doi: 10.1038/jid.2011.140. Epub 2011 Jun 16.

11.

RN486, a selective Bruton's tyrosine kinase inhibitor, abrogates immune hypersensitivity responses and arthritis in rodents.

Xu D, Kim Y, Postelnek J, Vu MD, Hu DQ, Liao C, Bradshaw M, Hsu J, Zhang J, Pashine A, Srinivasan D, Woods J, Levin A, O'Mahony A, Owens TD, Lou Y, Hill RJ, Narula S, DeMartino J, Fine JS.

J Pharmacol Exp Ther. 2012 Apr;341(1):90-103. doi: 10.1124/jpet.111.187740. Epub 2012 Jan 6.

12.

Identification of imidazo-pyrrolopyridines as novel and potent JAK1 inhibitors.

Kulagowski JJ, Blair W, Bull RJ, Chang C, Deshmukh G, Dyke HJ, Eigenbrot C, Ghilardi N, Gibbons P, Harrison TK, Hewitt PR, Liimatta M, Hurley CA, Johnson A, Johnson T, Kenny JR, Bir Kohli P, Maxey RJ, Mendonca R, Mortara K, Murray J, Narukulla R, Shia S, Steffek M, Ubhayakar S, Ultsch M, van Abbema A, Ward SI, Waszkowycz B, Zak M.

J Med Chem. 2012 Jun 28;55(12):5901-21. doi: 10.1021/jm300438j. Epub 2012 Jun 11.

PMID:
22591402
13.

Cartilage preservation by inhibition of Janus kinase 3 in two rodent models of rheumatoid arthritis.

Milici AJ, Kudlacz EM, Audoly L, Zwillich S, Changelian P.

Arthritis Res Ther. 2008;10(1):R14. doi: 10.1186/ar2365. Epub 2008 Jan 30.

14.

A highly selective, orally active inhibitor of Janus kinase 2, CEP-33779, ablates disease in two mouse models of rheumatoid arthritis.

Stump KL, Lu LD, Dobrzanski P, Serdikoff C, Gingrich DE, Dugan BJ, Angeles TS, Albom MS, Ator MA, Dorsey BD, Ruggeri BA, Seavey MM.

Arthritis Res Ther. 2011 Apr 21;13(2):R68. doi: 10.1186/ar3329.

15.

Anti-inflammatory activity and neutrophil reductions mediated by the JAK1/JAK3 inhibitor, CP-690,550, in rat adjuvant-induced arthritis.

Meyer DM, Jesson MI, Li X, Elrick MM, Funckes-Shippy CL, Warner JD, Gross CJ, Dowty ME, Ramaiah SK, Hirsch JL, Saabye MJ, Barks JL, Kishore N, Morris DL.

J Inflamm (Lond). 2010 Aug 11;7:41. doi: 10.1186/1476-9255-7-41.

16.

Preclinical to clinical translation of tofacitinib, a Janus kinase inhibitor, in rheumatoid arthritis.

Dowty ME, Jesson MI, Ghosh S, Lee J, Meyer DM, Krishnaswami S, Kishore N.

J Pharmacol Exp Ther. 2014 Jan;348(1):165-73. doi: 10.1124/jpet.113.209304. Epub 2013 Nov 11.

17.

Diamino-1,2,4-triazole derivatives are selective inhibitors of TYK2 and JAK1 over JAK2 and JAK3.

Malerich JP, Lam JS, Hart B, Fine RM, Klebansky B, Tanga MJ, D'Andrea A.

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7454-7. doi: 10.1016/j.bmcl.2010.10.026. Epub 2010 Oct 13.

PMID:
21106455
18.

Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2.

Zak M, Mendonca R, Balazs M, Barrett K, Bergeron P, Blair WS, Chang C, Deshmukh G, Devoss J, Dragovich PS, Eigenbrot C, Ghilardi N, Gibbons P, Gradl S, Hamman C, Hanan EJ, Harstad E, Hewitt PR, Hurley CA, Jin T, Johnson A, Johnson T, Kenny JR, Koehler MF, Bir Kohli P, Kulagowski JJ, Labadie S, Liao J, Liimatta M, Lin Z, Lupardus PJ, Maxey RJ, Murray JM, Pulk R, Rodriguez M, Savage S, Shia S, Steffek M, Ubhayakar S, Ultsch M, van Abbema A, Ward SI, Xiao L, Xiao Y.

J Med Chem. 2012 Jul 12;55(13):6176-93. doi: 10.1021/jm300628c. Epub 2012 Jun 28.

PMID:
22698084
19.
20.

7-hydroxyfrullanolide, a sesquiterpene lactone, inhibits pro-inflammatory cytokine production from immune cells and is orally efficacious in animal models of inflammation.

Fonseca LC, Dadarkar SS, Lobo AS, Suthar AC, Chauhan VS, Chandrababu S, Sharma SD, Dagia NM, Padigaru M.

Eur J Pharmacol. 2010 Oct 10;644(1-3):220-9. doi: 10.1016/j.ejphar.2010.06.052. Epub 2010 Jul 13.

PMID:
20621086

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