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Volumn 10, Issue 4, 2010, Pages 467-473

Pharmacological profile of AW-814141, a novel, potent, selective and orally active inhibitor of p38 MAP kinase

Author keywords

Arthritis; Collagen induced arthritis; Inflammation; Interleukin; Kinases; MAP kinases; p38; Tumor necrosis factor

Indexed keywords

5 (2,6 DICHLOROPHENYL) 2 (2,4 DIFLUOROPHENYLTHIO)PYRIMIDO[1,6 B]PYRIDAZIN 6 ONE; [2 (HEXAHYDRO CYCLOPENTA[C]PYRROL 2 YLAMINO) 8 METHYL 6 2 TOLYL 8H PYRIDO[2,3 D]PYRIMIDINE 7 ONE]; AW 814141; CARRAGEENAN; DEXAMETHASONE; DORAMAPIMOD; INDOMETACIN; LIPOPOLYSACCHARIDE; MITOGEN ACTIVATED PROTEIN KINASE P38 INHIBITOR; SYNAPTOPHYSIN; TUMOR NECROSIS FACTOR ALPHA; UNCLASSIFIED DRUG;

EID: 77949489123     PISSN: 15675769     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.intimp.2010.01.007     Document Type: Article
Times cited : (12)

References (35)
  • 1
    • 0034254536 scopus 로고    scopus 로고
    • Cytokines in rheumatoid arthritis: trials and tribulations
    • Carteron N.L. Cytokines in rheumatoid arthritis: trials and tribulations. Mol Med Today 6 (2000) 315-323
    • (2000) Mol Med Today , vol.6 , pp. 315-323
    • Carteron, N.L.1
  • 2
    • 14244268696 scopus 로고    scopus 로고
    • Psoriatic arthritis treatment: biological response modifiers
    • Mease P.J., and Antoni C.E. Psoriatic arthritis treatment: biological response modifiers. Ann Rheum Dis 64 (2005) 78-82
    • (2005) Ann Rheum Dis , vol.64 , pp. 78-82
    • Mease, P.J.1    Antoni, C.E.2
  • 3
    • 0035986898 scopus 로고    scopus 로고
    • TNF inhibition as therapy for rheumatoid arthritis
    • Wollheim F.A. TNF inhibition as therapy for rheumatoid arthritis. Expert Opin Investig Drugs 11 (2002) 947-953
    • (2002) Expert Opin Investig Drugs , vol.11 , pp. 947-953
    • Wollheim, F.A.1
  • 4
    • 4544347621 scopus 로고    scopus 로고
    • Considerations with the use of biological therapy in the treatment of rheumatoid arthritis
    • Fleischmann R.M., Iqbal I., and Stern R.L. Considerations with the use of biological therapy in the treatment of rheumatoid arthritis. Expert Opin Drug Saf 3 (2004) 391-403
    • (2004) Expert Opin Drug Saf , vol.3 , pp. 391-403
    • Fleischmann, R.M.1    Iqbal, I.2    Stern, R.L.3
  • 5
    • 0034997845 scopus 로고    scopus 로고
    • Mitogen-activated protein (MAP) kinase pathways: regulation and physiological functions
    • Pearson G., Robinson F., Beers G.T., Xu B.E., Karandikar M., Berman K., et al. Mitogen-activated protein (MAP) kinase pathways: regulation and physiological functions. Endocr Rev 22 (2001) 153-183
    • (2001) Endocr Rev , vol.22 , pp. 153-183
    • Pearson, G.1    Robinson, F.2    Beers, G.T.3    Xu, B.E.4    Karandikar, M.5    Berman, K.6
  • 6
    • 0028605318 scopus 로고
    • A protein kinase involved in the regulation of inflammatory cytokine biosynthesis
    • Lee J.C., Laydon J.T., Mcdonnell P.C., Gallagher T.F., Kumar S., Green D., et al. A protein kinase involved in the regulation of inflammatory cytokine biosynthesis. Nature 372 (1994) 739-746
    • (1994) Nature , vol.372 , pp. 739-746
    • Lee, J.C.1    Laydon, J.T.2    Mcdonnell, P.C.3    Gallagher, T.F.4    Kumar, S.5    Green, D.6
  • 7
    • 0029982565 scopus 로고    scopus 로고
    • Characterization of the structure and function of a new mitogen-activated protein kinase (p38beta)
    • Jiang Y., Chen C., Li Z., Guo W., Gegner J.A., Lin S., et al. Characterization of the structure and function of a new mitogen-activated protein kinase (p38beta). J Biol Chem 271 (1996) 17920-17926
    • (1996) J Biol Chem , vol.271 , pp. 17920-17926
    • Jiang, Y.1    Chen, C.2    Li, Z.3    Guo, W.4    Gegner, J.A.5    Lin, S.6
  • 8
    • 0030581626 scopus 로고    scopus 로고
    • The primary structure of p38γ: a new member of p38 group of map kinases
    • Li Z., Jiang Y., Ulevitch R.J., and Han J. The primary structure of p38γ: a new member of p38 group of map kinases. Biochem Biophys Res Commun 228 (1996) 334-340
    • (1996) Biochem Biophys Res Commun , vol.228 , pp. 334-340
    • Li, Z.1    Jiang, Y.2    Ulevitch, R.J.3    Han, J.4
  • 9
    • 0142026209 scopus 로고    scopus 로고
    • p38 map kinases: key signalling molecules as therapeutic targets for inflammatory diseases
    • Kumar S., Boehm J., and Lee J.C. p38 map kinases: key signalling molecules as therapeutic targets for inflammatory diseases. Nat Rev Drug Discov 2 (2003) 717-726
    • (2003) Nat Rev Drug Discov , vol.2 , pp. 717-726
    • Kumar, S.1    Boehm, J.2    Lee, J.C.3
  • 10
    • 0034887261 scopus 로고    scopus 로고
    • Vx-745 Vertex pharmaceuticals.
    • Haddad J.J. Vx-745 Vertex pharmaceuticals. Curr Opin Investig Drugs 2 (2001) 1070-1076
    • (2001) Curr Opin Investig Drugs , vol.2 , pp. 1070-1076
    • Haddad, J.J.1
  • 12
    • 0031934170 scopus 로고    scopus 로고
    • Pharmacological effects of SB-220025, a selective inhibitor of p38 mitogen-activated protein kinase, in angiogenesis and chronic inflammatory disease models
    • Jackson J.R., Bolognese B., Hillegass L., Kassis S., Adams J., Griswold D.E., et al. Pharmacological effects of SB-220025, a selective inhibitor of p38 mitogen-activated protein kinase, in angiogenesis and chronic inflammatory disease models. J Pharmacol Exp Ther 284 (1998) 687-692
    • (1998) J Pharmacol Exp Ther , vol.284 , pp. 687-692
    • Jackson, J.R.1    Bolognese, B.2    Hillegass, L.3    Kassis, S.4    Adams, J.5    Griswold, D.E.6
  • 14
    • 0037090078 scopus 로고    scopus 로고
    • Anti- inflammatory effects of a p38 mitogen-activated protein kinase inhibitor during human endotoxemia
    • Branger J., Van den blink B., Weijer S., Madwed J., Bos C.L., Gupta A., et al. Anti- inflammatory effects of a p38 mitogen-activated protein kinase inhibitor during human endotoxemia. J Immunol 168 (2002) 4070-4077
    • (2002) J Immunol , vol.168 , pp. 4070-4077
    • Branger, J.1    Van den blink, B.2    Weijer, S.3    Madwed, J.4    Bos, C.L.5    Gupta, A.6
  • 15
    • 3342903327 scopus 로고    scopus 로고
    • An improved synthesis of 5-(2, 6- dichlorophenyl)-2-(phenyl-thio)- 6 h-pyrimidol [1, 6-blpyridazin-6-one (Vx-745)]
    • Treu M., Jordis U., and Lee V.J. An improved synthesis of 5-(2, 6- dichlorophenyl)-2-(phenyl-thio)- 6 h-pyrimidol [1, 6-blpyridazin-6-one (Vx-745)]. Molecules 6 (2001) 959-963
    • (2001) Molecules , vol.6 , pp. 959-963
    • Treu, M.1    Jordis, U.2    Lee, V.J.3
  • 16
    • 0037019275 scopus 로고    scopus 로고
    • Pyrazole urea-based inhibitors of p38 map kinase: from lead compound to clinical candidate
    • Regan J., Breitfelder S., Cirillo P., Gilmore T., Graham A.G., Hickey E., et al. Pyrazole urea-based inhibitors of p38 map kinase: from lead compound to clinical candidate. J Med Chem 45 (2002) 2994-3008
    • (2002) J Med Chem , vol.45 , pp. 2994-3008
    • Regan, J.1    Breitfelder, S.2    Cirillo, P.3    Gilmore, T.4    Graham, A.G.5    Hickey, E.6
  • 17
    • 0348133551 scopus 로고    scopus 로고
    • Iq™ technology: development of a universal, homogeneous method for high-throughput screening of kinase and phosphatase activity
    • Mccauley T.J., Stanaitis M.L., Savage M.D., Onken J., and Millis S.Z. Iq™ technology: development of a universal, homogeneous method for high-throughput screening of kinase and phosphatase activity. J Assoc Lab Autom 8 (2003) 36-40
    • (2003) J Assoc Lab Autom , vol.8 , pp. 36-40
    • Mccauley, T.J.1    Stanaitis, M.L.2    Savage, M.D.3    Onken, J.4    Millis, S.Z.5
  • 19
    • 0026501878 scopus 로고
    • Different effects of staurosporine, an inhibitor of protein kinases, on the cell cycle and chromatin structure of normal and leukemic lymphocytes
    • Bruno S., Ardelt B., Skierski J.S., Traganos F., and Darzynkiewicz Z. Different effects of staurosporine, an inhibitor of protein kinases, on the cell cycle and chromatin structure of normal and leukemic lymphocytes. Cancer Res 52 (1992) 470-473
    • (1992) Cancer Res , vol.52 , pp. 470-473
    • Bruno, S.1    Ardelt, B.2    Skierski, J.S.3    Traganos, F.4    Darzynkiewicz, Z.5
  • 20
    • 2542428509 scopus 로고    scopus 로고
    • Anti-inflammatory effects of moxifloxacin on activated human monocytic cells: inhibition of NF-kappaB and mitogen-activated protein kinase activation and of synthesis of proinflammatory cytokines
    • Weiss T., Shalit I., Blau H., Werber S., Halperin D., Levitov A., et al. Anti-inflammatory effects of moxifloxacin on activated human monocytic cells: inhibition of NF-kappaB and mitogen-activated protein kinase activation and of synthesis of proinflammatory cytokines. Antimicrob Agents Chemother 48 (2004) 1974-1982
    • (2004) Antimicrob Agents Chemother , vol.48 , pp. 1974-1982
    • Weiss, T.1    Shalit, I.2    Blau, H.3    Werber, S.4    Halperin, D.5    Levitov, A.6
  • 21
    • 18544406054 scopus 로고    scopus 로고
    • SB239063, a potent p38 map kinase inhibitor, reduces inflammatory cytokine production, airways eosinophil Infiltration, and persistence
    • Underwood D.C., Osborn R.R., Kotzer C.J., Adams J.L., Lee J.C., Webb E.F., et al. SB239063, a potent p38 map kinase inhibitor, reduces inflammatory cytokine production, airways eosinophil Infiltration, and persistence. J Pharmacol Exp Ther 293 (2000) 281-288
    • (2000) J Pharmacol Exp Ther , vol.293 , pp. 281-288
    • Underwood, D.C.1    Osborn, R.R.2    Kotzer, C.J.3    Adams, J.L.4    Lee, J.C.5    Webb, E.F.6
  • 22
    • 43049159562 scopus 로고    scopus 로고
    • Development of a cell death-based method for the screening of nuclear factor-kappaB inhibitors
    • Chopra P., Bajpai M., Dastidar S.G., and Ray A. Development of a cell death-based method for the screening of nuclear factor-kappaB inhibitors. J Immunol Methods 335 (2008) 126-131
    • (2008) J Immunol Methods , vol.335 , pp. 126-131
    • Chopra, P.1    Bajpai, M.2    Dastidar, S.G.3    Ray, A.4
  • 23
    • 77949486497 scopus 로고    scopus 로고
    • Phyllis EW, Stacie AD. Models of inflammation: carrageenan-induced paw edema in the rat. in: Current protocols in pharmacology. pp 5.4.1-5.4.3, John Willie & Sons, inc.
    • Phyllis EW, Stacie AD. Models of inflammation: carrageenan-induced paw edema in the rat. in: Current protocols in pharmacology. pp 5.4.1-5.4.3, John Willie & Sons, inc.
  • 24
    • 0042121489 scopus 로고    scopus 로고
    • Efficacy of treatment with glycosaminoglycans on experimental collagen-induced arthritis in rats
    • Campo G.M., Avenoso A., Campo S., Ferlazzo A.M., Altavilla D., and Calatroni A. Efficacy of treatment with glycosaminoglycans on experimental collagen-induced arthritis in rats. Arth Res Ther 5 (2003) 122-131
    • (2003) Arth Res Ther , vol.5 , pp. 122-131
    • Campo, G.M.1    Avenoso, A.2    Campo, S.3    Ferlazzo, A.M.4    Altavilla, D.5    Calatroni, A.6
  • 25
    • 0033120590 scopus 로고    scopus 로고
    • Differential expression and activation of p38 mitogen-activated protein kinase alpha, beta, gamma, and delta in inflammatory cell lineages
    • Hale K.K., Trollinger D., Rihanek M., and Manthey C.L. Differential expression and activation of p38 mitogen-activated protein kinase alpha, beta, gamma, and delta in inflammatory cell lineages. J Immunol 162 (1999) 4246-4252
    • (1999) J Immunol , vol.162 , pp. 4246-4252
    • Hale, K.K.1    Trollinger, D.2    Rihanek, M.3    Manthey, C.L.4
  • 26
    • 0032928614 scopus 로고    scopus 로고
    • Mitogen-activated protein kinase: conservation of a three-kinase module from yeast to human
    • Widmann C., Gibson S., Jarpe M.B., and Johnson G.L. Mitogen-activated protein kinase: conservation of a three-kinase module from yeast to human. Physiol Rev 79 (1999) 143-180
    • (1999) Physiol Rev , vol.79 , pp. 143-180
    • Widmann, C.1    Gibson, S.2    Jarpe, M.B.3    Johnson, G.L.4
  • 27
    • 0035932519 scopus 로고    scopus 로고
    • Cytokine pathways and joint inflammation in rheumatoid arthritis
    • Choy E.H., and Panayi G.S. Cytokine pathways and joint inflammation in rheumatoid arthritis. N Engl. J Med 344 (2001) 907-916
    • (2001) N Engl. J Med , vol.344 , pp. 907-916
    • Choy, E.H.1    Panayi, G.S.2
  • 28
    • 0036781052 scopus 로고    scopus 로고
    • NF-kappa B regulation in the immune system
    • Li Q., and Verma I.M. NF-kappa B regulation in the immune system. Nat Rev Immunol 2 (2002) 725
    • (2002) Nat Rev Immunol , vol.2 , pp. 725
    • Li, Q.1    Verma, I.M.2
  • 29
    • 0028675681 scopus 로고
    • Evaluation of the significance of elevated levels of systemic and localized tumor necrosis factor in different animal models of inflammation
    • Sekut L., Menius Jr. J.A., Brackeen M.F., and Connolly K.M. Evaluation of the significance of elevated levels of systemic and localized tumor necrosis factor in different animal models of inflammation. J Lab Clin Med 124 (1994) 813-820
    • (1994) J Lab Clin Med , vol.124 , pp. 813-820
    • Sekut, L.1    Menius Jr., J.A.2    Brackeen, M.F.3    Connolly, K.M.4
  • 30
    • 0037144228 scopus 로고    scopus 로고
    • Anti-inflammatory potency of FR167653, a p38 mitogen-activated protein kinase inhibitor, in mouse models of acute inflammation
    • Nishikori T., Irie K., Suganuma T., Ozaki M., and Yoshioka T. Anti-inflammatory potency of FR167653, a p38 mitogen-activated protein kinase inhibitor, in mouse models of acute inflammation. Eur J Pharmacol 451 (2002) 327-333
    • (2002) Eur J Pharmacol , vol.451 , pp. 327-333
    • Nishikori, T.1    Irie, K.2    Suganuma, T.3    Ozaki, M.4    Yoshioka, T.5
  • 31
    • 0035158436 scopus 로고    scopus 로고
    • The effects of newly synthesized pyrazole derivatives on formaldehyde-carrageenan- and dextran-induced acute paw edema in rats
    • Suleyman H., and Buyukokuroglu M.E. The effects of newly synthesized pyrazole derivatives on formaldehyde-carrageenan- and dextran-induced acute paw edema in rats. Biol Pharm Bull 24 (2001) 1133-1136
    • (2001) Biol Pharm Bull , vol.24 , pp. 1133-1136
    • Suleyman, H.1    Buyukokuroglu, M.E.2
  • 32
    • 0020082308 scopus 로고
    • Nature and specificity of the immune response to collagen in type II collagen-induced arthritis in mice
    • Stuart J.M., Townes A.S., and Kang A.H. Nature and specificity of the immune response to collagen in type II collagen-induced arthritis in mice. J Clin Invest 69 (1982) 673-683
    • (1982) J Clin Invest , vol.69 , pp. 673-683
    • Stuart, J.M.1    Townes, A.S.2    Kang, A.H.3
  • 33
    • 0032536542 scopus 로고    scopus 로고
    • Interleukin 6 is required for the development of collagen-induced arthritis
    • Alonzi T., Fattori E., Lazzaro D., Costa P., Probert L., Kollias G., et al. Interleukin 6 is required for the development of collagen-induced arthritis. J Exp Med 187 (1998) 461-468
    • (1998) J Exp Med , vol.187 , pp. 461-468
    • Alonzi, T.1    Fattori, E.2    Lazzaro, D.3    Costa, P.4    Probert, L.5    Kollias, G.6
  • 34
    • 0034967902 scopus 로고    scopus 로고
    • Severe inflammatory arthritis and lymphadenopathy in the absence of TNF
    • Campbell I.K., O'donnell K., Lawlor K.E., and Wicks I.P. Severe inflammatory arthritis and lymphadenopathy in the absence of TNF. J Clin Invest 107 (2001) 1519-1527
    • (2001) J Clin Invest , vol.107 , pp. 1519-1527
    • Campbell, I.K.1    O'donnell, K.2    Lawlor, K.E.3    Wicks, I.P.4
  • 35
    • 0034671575 scopus 로고    scopus 로고
    • Evaluation of TNF- alpha and Il-1 blockade in collagen-induced arthritis and comparison with combined anti-TNF-alpha/anti-cd4 therapy
    • Williams R.O., Marinova-mutafchieva L., Feldmann M., and Maini R.N. Evaluation of TNF- alpha and Il-1 blockade in collagen-induced arthritis and comparison with combined anti-TNF-alpha/anti-cd4 therapy. J Immunol 165 (2000) 7240-7245
    • (2000) J Immunol , vol.165 , pp. 7240-7245
    • Williams, R.O.1    Marinova-mutafchieva, L.2    Feldmann, M.3    Maini, R.N.4


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