Specific inhibition of spleen tyrosine kinase suppresses leukocyte immune function and inflammation in animal models of rheumatoid arthritis

Journal of Pharmacology and Experimental Therapeutics

Volumn 340, Issue 2, 2012, Pages 350-359

  Coffey, Greg ^a   DeGuzman, Francis ^a   Inagaki, Mayuko ^a   Pak, Yvonne ^a   Delaney, Suzanne M ^a   Ives, Dan ^a   Betz, Andreas ^a   Jia, Zhaozhong J ^a   Pandey, Anjali ^a   Baker, Dale ^a   Hollenbach, Stanley J ^a   Phillips, David R ^a   Sinha, Uma ^a  

^a Portola Pharmaceuticals   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

[4 [3 (2H 1,2,3 TRIAZOL 2 YL)PHENYLAMINO] 2 (2 AMINOCYCLOHEXYLAMINO)PYRIMIDINE 5 CARBOXAMIDE ACETATE]; B LYMPHOCYTE ANTIGEN RECEPTOR; FC EPSILON RECEPTOR 1; FC RECEPTOR; LYMPHOCYTE ANTIGEN RECEPTOR; P 505 15; PREDNISOLONE; PROTEIN KINASE SYK INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTIINFLAMMATORY ACTIVITY; ARTICLE; B LYMPHOCYTE ACTIVATION; BASOPHIL DEGRANULATION; CONCENTRATION RESPONSE; CONTROLLED STUDY; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG DOSE COMPARISON; DRUG EFFICACY; DRUG MEGADOSE; DRUG POTENCY; DRUG STRUCTURE; ENZYME INHIBITION; ENZYME PURIFICATION; ENZYME SPECIFICITY; EX VIVO STUDY; FEMALE; FLOW CYTOMETRY; GENETIC DISORDER; HISTOPATHOLOGY; HUMAN; HUMAN CELL; IC 50; IMMUNOMODULATION; INHIBITION KINETICS; LEUKOCYTE FUNCTION; MAXIMUM PLASMA CONCENTRATION; MOUSE; NONHUMAN; PHARMACODYNAMICS; PRIORITY JOURNAL; RAT; RHEUMATOID ARTHRITIS; SIGNAL TRANSDUCTION; SINGLE DRUG DOSE; STRUCTURE ACTIVITY RELATION;

ADAPTOR PROTEINS, SIGNAL TRANSDUCING; ANIMALS; ARTHRITIS, EXPERIMENTAL; B-LYMPHOCYTES; BASOPHILS; BIOCATALYSIS; BLOOD; CELL DEGRANULATION; CELL LINE; CELL LINE, TUMOR; CELL PROLIFERATION; CYCLOHEXYLAMINES; DISEASE MODELS, ANIMAL; EDEMA; EXTRACELLULAR SIGNAL-REGULATED MAP KINASES; FEMALE; FOOT; HUMANS; INHIBITORY CONCENTRATION 50; INTRACELLULAR SIGNALING PEPTIDES AND PROTEINS; LEUKOCYTES; LYMPHOCYTE ACTIVATION; MICE; MICE, INBRED BALB C; MOLECULAR STRUCTURE; PHOSPHORYLATION; PRECURSOR CELLS, B-LYMPHOID; PROTEIN KINASE INHIBITORS; PROTEIN-TYROSINE KINASES; PYRIMIDINES; RATS; RATS, INBRED LEW; RECEPTORS, ANTIGEN, B-CELL; SIGNAL TRANSDUCTION; SYNOVITIS;

EID: 84856023801     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.111.188441     Document Type: Article

References (35)

1. Aringer M, Cheng A, Nelson JW, Chen M, Sudarshan C, Zhou YJ, and O'Shea JJ (1999) Janus kinases and their role in growth and disease. Life Sci 64:2173-2186. (Pubitemid 29254037)
2. Atwell S, Adams JM, Badger J, Buchanan MD, Feil IK, Froning KJ, Gao X, Hendle J, Keegan K, Leon BC, et al. (2004) A novel mode of Gleevec binding is revealed by the structure of spleen tyrosine kinase. J Biol Chem 279:55827-55832. (Pubitemid 40066590)
3. Au-Yeung BB, Levin SE, Zhang C, Hsu LY, Cheng DA, Killeen N, Shokat KM, and Weiss A (2010) A genetically selective inhibitor demonstrates a function for the kinase Zap70 in regulatory T cells independent of its catalytic activity. Nat Immunol 11:1085-1092.
4. Biazzo-Ashnault DE, Park YW, Cummings RT, Ding V, Moller DE, Zhang BB, and Qureshi SA (2001) Detection of insulin receptor tyrosine kinase activity using time-resolved fluorescence energy transfer technology. Anal Biochem 291:155-158. (Pubitemid 32324537)
5. Boilard E, Nigrovic PA, Larabee K, Watts GF, Coblyn JS, Weinblatt ME, Massarotti EM, Remold-O'Donnell E, Farndale RW, Ware J, et al. (2010) Platelets amplify inflammation in arthritis via collagen-dependent microparticle production. Science 327:580-583.
6. Braselmann S, Taylor V, Zhao H, Wang S, Sylvain C, Baluom M, Qu K, Herlaar E, Lau A, Young C, et al. (2006) R406, an orally available spleen tyrosine kinase inhibitor blocks Fc receptor signaling and reduces immune complex-mediated inflammation. J Pharmacol Exp Ther 319:998-1008.
7. Buchner M, Baer C, Prinz G, Dierks C, Burger M, Zenz T, Stilgenbauer S, Jumaa H, Veelken H, and Zirlik K (2010) Spleen tyrosine kinase inhibition prevents chemokine- and integrin-mediated stromal protective effects in chronic lymphocytic leukemia. Blood 115:4497-4506.
8. Cheng AM, Rowley B, Pao W, Hayday A, Bolen JB, and Pawson T (1995) Syk tyrosine kinase required for mouse viability and B-cell development. Nature 378:303-306.
9. Chiorazzi N, Hatzi K, and Albesiano E (2005) B-cell chronic lymphocytic leukemia, a clonal disease of B lymphocytes with receptors that vary in specificity for (auto)antigens. Ann NY Acad Sci 1062:1-12.
10. Coffey G, DeGuzman F, Inagaki M, Pak Y, Delaney S, Betz A, Jia Z, Xu Q, Bauer S, Song Y, et al. (2010) Specific inhibition of Syk suppresses leukocyte immune function and alleviates inflammation in rodent models of rheumatoid arthritis. Blood 116:Abstract 1727.
11. Davis RE, Brown KD, Siebenlist U, and Staudt LM (2001) Constitutive nuclear factor κB activity is required for survival of activated B cell-like diffuse large B cell lymphoma cells. J Exp Med 194:1861-1874. (Pubitemid 34028664)
12. Davis RE, Ngo VN, Lenz G, Tolar P, Young RM, Romesser PB, Kohlhammer H, Lamy L, Zhao H, Yang Y, et al. (2010) Chronic active B-cell-receptor signalling in diffuse large B-cell lymphoma. Nature 463:88-92.
13. Fodor S, Jakus Z, and Mócsai A (2006) ITAM-based signaling beyond the adaptive immune response. Immunol Lett 104:29-37. (Pubitemid 43330706)
14. Frommhold D, Mannigel I, Schymeinsky J, Mocsai A, Poeschl J, Walzog B, and Sperandio M (2007) Spleen tyrosine kinase Syk is critical for sustained leukocyte adhesion during inflammation in vivo. BMC Immunol 8:31.
15. Holmdahl R, Lorentzen JC, Lu S, Olofsson P, Wester L, Holmberg J, and Pettersson U (2001) Arthritis induced in rats with nonimmunogenic adjuvants as models for rheumatoid arthritis. Immunol Rev 184:184-202. (Pubitemid 34123775)
16. Hutamekalin P, Saito T, Yamaki K, Mizutani N, Brand DD, Waritani T, Terato K, and Yoshino S (2009) Collagen antibody-induced arthritis in mice: development of a new arthritogenic 5-clone cocktail of monoclonal anti-type II collagen antibodies. J Immunol Methods 343:49-55.
17. Jakus Z, Simon E, Balázs B, and Mócsai A (2010) Genetic deficiency of Syk protects mice from autoantibody-induced arthritis. Arthritis Rheum 62:1899-1910.
18. Kremer JM, Bloom BJ, Breedveld FC, Coombs JH, Fletcher MP, Gruben D, Krishnaswami S, Burgos-Vargas R, Wilkinson B, Zerbini CA, et al. (2009) The safety and efficacy of a JAK inhibitor in patients with active rheumatoid arthritis: Results of a double-blind, placebo-controlled phase IIa trial of three dosage levels of CP-690,550 versus placebo. Arthritis Rheum 60:1895-1905.
19. Mankin HJ (1971) Biochemical and metabolic aspects of osteoarthritis. Orthop Clin North Am 2:19-31.
20. Mócsai A, Ruland J, and Tybulewicz VL (2010) The SYK tyrosine kinase: a crucial player in diverse biological functions. Nat Rev Immunol 10:387-402.
21. Mócsai A, Zhou M, Meng F, Tybulewicz VL, and Lowell CA (2002) Syk is required for integrin signaling in neutrophils. Immunity 16:547-558. (Pubitemid 34442579)
22. Monti S, Savage KJ, Kutok JL, Feuerhake F, Kurtin P, Mihm M, Wu B, Pasqualucci L, Neuberg D, Aguiar RC, et al. (2005) Molecular profiling of diffuse large B-cell lymphoma identifies robust subtypes including one characterized by host inflammatory response. Blood 105:1851-1861. (Pubitemid 40731764)
23. Ngo VN, Young RM, Schmitz R, Jhavar S, Xiao W, Lim KH, Kohlhammer H, Xu W, Yang Y, Zhao H, et al. (2011) Oncogenically active MYD88 mutations in human lymphoma. Nature 470:115-119.
24. Pine PR, Chang B, Schoettler N, Banquerigo ML, Wang S, Lau A, Zhao F, Grossbard EB, Payan DG, and Brahn E (2007) Inflammation and bone erosion are suppressed in models of rheumatoid arthritis following treatment with a novel Syk inhibitor. Clin Immunol 124:244-257. (Pubitemid 47247604)
25. Poole A, Gibbins JM, Turner M, van Vugt MJ, van de Winkel JG, Saito T, Tybulewicz VL, and Watson SP (1997) The Fc receptor γ-chain and the tyrosine kinase Syk are essential for activation of mouse platelets by collagen. EMBO J 16:2333-2341. (Pubitemid 27258634)
26. Quiroga MP, Balakrishnan K, Kurtova AV, Sivina M, Keating MJ, Wierda WG, Gandhi V, and Burger JA (2009) B-cell antigen receptor signaling enhances chronic lymphocytic leukemia cell migration and survival: specific targeting with a novel spleen tyrosine kinase inhibitor, R406. Blood 114:1029-1037.
27. Ritz CSJ and Streibig J (2005) Bioassay analysis using R. J Stat Software 12:1-22.
28. Rogers NC, Slack EC, Edwards AD, Nolte MA, Schulz O, Schweighoffer E, Williams DL, Gordon S, Tybulewicz VL, Brown GD, et al. (2005) Syk-dependent cytokine induction by Dectin-1 reveals a novel pattern recognition pathway for C type lectins. Immunity 22:507-517. (Pubitemid 40545115)
29. Terato K, Hasty KA, Reife RA, Cremer MA, Kang AH, and Stuart JM (1992) Induction of arthritis with monoclonal antibodies to collagen. J Immunol 148:2103-2108.
30. Trentham DE, Townes AS, and Kang AH (1977) Autoimmunity to type II collagen an experimental model of arthritis. J Exp Med 146:857-868. (Pubitemid 8175993)
31. Turner M, Mee PJ, Costello PS, Williams O, Price AA, Duddy LP, Furlong MT, Geahlen RL, and Tybulewicz VL (1995) Perinatal lethality and blocked B-cell development in mice lacking the tyrosine kinase Syk. Nature 378:298-302.
32. Turner M, Schweighoffer E, Colucci F, Di Santo JP, and Tybulewicz VL (2000) Tyrosine kinase SYK: essential functions for immunoreceptor signalling. Immunol Today 21:148-154. (Pubitemid 30122705)
33. Warmuth M, Kim S, Gu XJ, Xia G, and Adrián F (2007) Ba/F3 cells and their use in kinase drug discovery. Curr Opin Oncol 19:55-60. (Pubitemid 44885601)
34. Weinblatt ME, Kavanaugh A, Burgos-Vargas R, Dikranian AH, Medrano-Ramirez G, Morales-Torres JL, Murphy FT, Musser TK, Straniero N, Vicente-Gonzales AV, et al. (2008) Treatment of rheumatoid arthritis with a Syk kinase inhibitor: a twelve-week, randomized, placebo-controlled trial. Arthritis Rheum 58:3309-3318.
35. Zarbock A, Abram CL, Hundt M, Altman A, Lowell CA, and Ley K (2008) PSGL-1 engagement by E-selectin signals through Src kinase Fgr and ITAM adapters DAP12 and FcRγ to induce slow leukocyte rolling. J Exp Med 205:2339-2347.