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1
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33745088052
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Small molecular weight inhibitors of stress- activated and mitogen-activated protein kinases
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This review chronicled the development, structure, mechanism of action and biological activities of SMIs of SAP/MAPKs.
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Malemud C.J. Small molecular weight inhibitors of stress- activated and mitogen-activated protein kinases. Mini Rev Med Chem 6 (2006) 689-698. This review chronicled the development, structure, mechanism of action and biological activities of SMIs of SAP/MAPKs.
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Mini Rev Med Chem
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Malemud, C.J.1
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34248353740
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Malemud CJ: MAP kinases. In OA, Inflammation and Degradation: A Continuum. Edited by Buckwalter J, Lotz M, Stoltz J-F. IOS Press; 2007, in press.
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3
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33746101818
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Functional in vivo interactions between JNK1 and JNK2 isoforms in obesity and insulin resistance
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-/- mice, this study showed that the JNK2 isoform is highly involved in metabolic syndrome, but JNK2 function is not as critical when JNK1 is fully expressed because of cross-talk between JNK isoforms.
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-/- mice, this study showed that the JNK2 isoform is highly involved in metabolic syndrome, but JNK2 function is not as critical when JNK1 is fully expressed because of cross-talk between JNK isoforms.
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(2006)
Proc Natl Acad Sci USA
, vol.103
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Tuncman, G.1
Hirosumi, J.2
Solinas, G.3
Chang, L.4
Karin, M.5
Hotamisligil, G.S.6
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4
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Dialogue between ERKs and JNKs: friendly or antagonistic?
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Dong Z., and Bode A.M. Dialogue between ERKs and JNKs: friendly or antagonistic?. Mol Interv 3 (2003) 306-308
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Mol Interv
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Dong, Z.1
Bode, A.M.2
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5
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0037040883
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Ras participates in the activation of p38 MAPK by interleukin-1 by associating with IRAK, IRAK2, TRAF6 and TAK-1
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McDermott E.P., and O'Neill L.A.J. Ras participates in the activation of p38 MAPK by interleukin-1 by associating with IRAK, IRAK2, TRAF6 and TAK-1. J Biol Chem 277 (2002) 7808-7815
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McDermott, E.P.1
O'Neill, L.A.J.2
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6
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25144492764
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MAPK signalling in rheumatoid arthritis destruction: can we unravel the puzzle?
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This review focused on recent data indicating that, in addition to JNK and ERK, stable activation of p38 kinase contributes to destructive arthritis in human TNF-α transgenic mice.
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Meyer L.H., and Pap T. MAPK signalling in rheumatoid arthritis destruction: can we unravel the puzzle?. Arthritis Res Ther 7 (2005) 177-178. This review focused on recent data indicating that, in addition to JNK and ERK, stable activation of p38 kinase contributes to destructive arthritis in human TNF-α transgenic mice.
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Arthritis Res Ther
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Meyer, L.H.1
Pap, T.2
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7
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33744831517
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Resveratrol inhibits proliferation of human epidermoid carcinoma A431 cells by modulating MEK1 and AP-1 signalling pathways
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Kim A.L., Zhu Y., Zhu H., Han L., Kopelovich L., Bickers D.R., and Athar M. Resveratrol inhibits proliferation of human epidermoid carcinoma A431 cells by modulating MEK1 and AP-1 signalling pathways. Exp Dermatol 15 (2006) 538-546
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Exp Dermatol
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Kim, A.L.1
Zhu, Y.2
Zhu, H.3
Han, L.4
Kopelovich, L.5
Bickers, D.R.6
Athar, M.7
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8
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33845225077
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Tangeretin suppresses IL-1β-induced cyclooxygenase (COX)-2 expression through inhibition of p38 MAPK, JNK and AKT activation in human lung carcinoma cells
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Chen K.H., Weng M.S., and Lin J.K. Tangeretin suppresses IL-1β-induced cyclooxygenase (COX)-2 expression through inhibition of p38 MAPK, JNK and AKT activation in human lung carcinoma cells. Biochem Pharmacol 73 (2007) 215-227
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Biochem Pharmacol
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Chen, K.H.1
Weng, M.S.2
Lin, J.K.3
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9
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Tangeretin inhibits extracellular-signal-regulated-kinase (ERK) phosphorylation
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Van Slambrouck S., Parmar V.S., Sharma S.K., De Bondt B., Fore F., Coopman P., Vanhoecke B.W., Boterberg T., Depypere H.T., Leclercq G., et al. Tangeretin inhibits extracellular-signal-regulated-kinase (ERK) phosphorylation. FEBS Lett 579 (2005) 1665-1669
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FEBS Lett
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Van Slambrouck, S.1
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Coopman, P.6
Vanhoecke, B.W.7
Boterberg, T.8
Depypere, H.T.9
Leclercq, G.10
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10
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23944478448
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Preparative isolation and purification of polymethoxylated flavones from Tangerine peel using high-speed counter-current chromatography
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Wang X., Li F., Zhang H., Geng Y., Yuan J., and Jiang T. Preparative isolation and purification of polymethoxylated flavones from Tangerine peel using high-speed counter-current chromatography. J Chromatogr A 1090 (2005) 188-192
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J Chromatogr A
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Wang, X.1
Li, F.2
Zhang, H.3
Geng, Y.4
Yuan, J.5
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11
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33746000417
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Ligustilide inhibits vascular smooth muscle cells proliferation
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Lu Q., Qiu T.-Q., and Yang H. Ligustilide inhibits vascular smooth muscle cells proliferation. Eur J Pharmacol 542 (2006) 136-140
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Eur J Pharmacol
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Lu, Q.1
Qiu, T.-Q.2
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20844450752
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Targeting the JNK signaling pathway for stroke and Parkinson's diseases therapy
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Kuan C.-Y., and Burke R.E. Targeting the JNK signaling pathway for stroke and Parkinson's diseases therapy. Curr Drug Targets CNS Neurol Disord 4 (2005) 63-67
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Curr Drug Targets CNS Neurol Disord
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Kuan, C.-Y.1
Burke, R.E.2
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13
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1342344813
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Mixed lineage kinases: a target for the prevention of neurodegeneration
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Wang L.H., Besirli C.G., and Johnson Jr. E.M. Mixed lineage kinases: a target for the prevention of neurodegeneration. Annu Rev Pharmacol Toxicol 44 (2004) 451-474
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Annu Rev Pharmacol Toxicol
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Wang, L.H.1
Besirli, C.G.2
Johnson Jr., E.M.3
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14
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20344365580
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CEP-11004, an inhibitor of the SAPK/JNK pathway, reduces TNF-α release from lipopolysaccharide-treated cells and mice
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Ciallella J.R., Saporito M., Lund S., Leist M., Hasseldam H., McGann N., Smith C.S., Bozyczko-Coyne D., and Flood D.G. CEP-11004, an inhibitor of the SAPK/JNK pathway, reduces TNF-α release from lipopolysaccharide-treated cells and mice. Eur J Pharmacol 515 (2005) 179-187
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Eur J Pharmacol
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Ciallella, J.R.1
Saporito, M.2
Lund, S.3
Leist, M.4
Hasseldam, H.5
McGann, N.6
Smith, C.S.7
Bozyczko-Coyne, D.8
Flood, D.G.9
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16
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27944503331
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MAP kinase p38 inhibitors: clinical results and an intimate look at their interactions with p38α protein
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Lee M.R., and Dominguez C. MAP kinase p38 inhibitors: clinical results and an intimate look at their interactions with p38α protein. Curr Med Chem 12 (2005) 2979-2994
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Curr Med Chem
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Lee, M.R.1
Dominguez, C.2
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17
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20244363808
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Design and synthesis of potent pyridazine inhibitors of p38 MAP kinase
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Tamayo N., Liao L., Goldberg M., Powers D., Tudor Y.-Y., Yu V., Wong L.M., Henkle B., Middleton S., Syed R., et al. Design and synthesis of potent pyridazine inhibitors of p38 MAP kinase. Bioorg Med Chem Lett 15 (2005) 2409-2413
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Bioorg Med Chem Lett
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Tamayo, N.1
Liao, L.2
Goldberg, M.3
Powers, D.4
Tudor, Y.-Y.5
Yu, V.6
Wong, L.M.7
Henkle, B.8
Middleton, S.9
Syed, R.10
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18
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33749370145
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Differential tissue expression and activation of p38 MAPK α, β, γ, δ isoforms in rheumatoid arthritis
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Using human synovial tissue biopsies combined with immunoblotting, immunoprecipitation and immunohistochemistry techniques, the authors revealed that the most frequent p38 kinase isoforms in inflamed rheumatoid arthritis joints are p38α and p38γ.
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Korb A., Tohidast-Akrad M., Cetin E., Axmann R., Smolen J., and Schett G. Differential tissue expression and activation of p38 MAPK α, β, γ, δ isoforms in rheumatoid arthritis. Arthritis Rheum 54 (2006) 2745-2756. Using human synovial tissue biopsies combined with immunoblotting, immunoprecipitation and immunohistochemistry techniques, the authors revealed that the most frequent p38 kinase isoforms in inflamed rheumatoid arthritis joints are p38α and p38γ.
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Arthritis Rheum
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Korb, A.1
Tohidast-Akrad, M.2
Cetin, E.3
Axmann, R.4
Smolen, J.5
Schett, G.6
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19
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33745248460
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A selective p38α mitogen- activated protein kinase inhibitor reverses cartilage and bone destruction in mice with collagen-induced arthritis
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Medicherla S., Ma J.Y., Mangadu R., Jiang Y., Zhao J.J., Almirez R., Kerr I., Stebbins E.G., O'Young G., Kapoun A.M., et al. A selective p38α mitogen- activated protein kinase inhibitor reverses cartilage and bone destruction in mice with collagen-induced arthritis. J Pharmacol Exp Ther 318 (2006) 132-141
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J Pharmacol Exp Ther
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Medicherla, S.1
Ma, J.Y.2
Mangadu, R.3
Jiang, Y.4
Zhao, J.J.5
Almirez, R.6
Kerr, I.7
Stebbins, E.G.8
O'Young, G.9
Kapoun, A.M.10
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20
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33845874434
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A p38α selective mitogen-activated protein kinase inhibitor prevents periodontal bone loss
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This study showed that the p38α-selective SMI SD-282 blocked arthritis progression in murine collagen-induced arthritis, even in those arthritic mice with existing bone and cartilage degeneration.
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Kirkwood K.L., Li F., Rogers J.E., Otremba J., Coatney D.D., Kreider J.M., D'Silva N.J., Chakravarty S., Dugar S., Linda H.S., et al. A p38α selective mitogen-activated protein kinase inhibitor prevents periodontal bone loss. J Pharmacol Exp Ther 320 (2007) 56-63. This study showed that the p38α-selective SMI SD-282 blocked arthritis progression in murine collagen-induced arthritis, even in those arthritic mice with existing bone and cartilage degeneration.
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J Pharmacol Exp Ther
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Kirkwood, K.L.1
Li, F.2
Rogers, J.E.3
Otremba, J.4
Coatney, D.D.5
Kreider, J.M.6
D'Silva, N.J.7
Chakravarty, S.8
Dugar, S.9
Linda, H.S.10
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21
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33750086376
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Inhibitory effect of p38 mitogen-activated protein kinase inhibitors on cytokine release from human macrophages
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Smith S.J., Fenwick P.S., Nicholson A.G., Kirschenbaum F., Finney-Haywood T.K., Higgins L.S., Giembycz M.A., Barnes P.J., and Donnelly L.E. Inhibitory effect of p38 mitogen-activated protein kinase inhibitors on cytokine release from human macrophages. Br J Pharmacol 149 (2006) 393-404
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Br J Pharmacol
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Smith, S.J.1
Fenwick, P.S.2
Nicholson, A.G.3
Kirschenbaum, F.4
Finney-Haywood, T.K.5
Higgins, L.S.6
Giembycz, M.A.7
Barnes, P.J.8
Donnelly, L.E.9
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22
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33747879777
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Selective inhibition of p38α MAPK improves cardiac function and reduces myocardial apoptosis in rat model of myocardial injury
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Li Z., Ma J.Y., Kerr I., Chakravarty S., Dugar S., Schreiner G., and Protter A.A. Selective inhibition of p38α MAPK improves cardiac function and reduces myocardial apoptosis in rat model of myocardial injury. Am J Physiol Heart Circ Physiol 291 (2006) H1972-H1977
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Am J Physiol Heart Circ Physiol
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Li, Z.1
Ma, J.Y.2
Kerr, I.3
Chakravarty, S.4
Dugar, S.5
Schreiner, G.6
Protter, A.A.7
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23
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33745945655
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Discovery and characterization of triaminotriazine aniline amides as highly selective p38 kinase inhibitors
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Lin T.H., Metzger A., Diller D.J., Desai M., Henderson I., Ahmed G., Kimble E.F., Quadros E., and Webb M.L. Discovery and characterization of triaminotriazine aniline amides as highly selective p38 kinase inhibitors. J Pharmacol Exp Ther 318 (2006) 495-502
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J Pharmacol Exp Ther
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Lin, T.H.1
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Ahmed, G.6
Kimble, E.F.7
Quadros, E.8
Webb, M.L.9
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24
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20244384283
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Design of potent and selective 2-aminobenzimidazole-based p38α MAP kinase inhibitors with excellent in vivo efficacy
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De Dios A., Shih C., Lopez de Uralde B., Sanchez C., del Prado M., Martin Calbrejas L.M., Pleite S., Blanco-Urgoiti J., Lorite M.J., Nevill Jr. C.R., et al. Design of potent and selective 2-aminobenzimidazole-based p38α MAP kinase inhibitors with excellent in vivo efficacy. J Med Chem 48 (2005) 2270-2273
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De Dios, A.1
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Pleite, S.7
Blanco-Urgoiti, J.8
Lorite, M.J.9
Nevill Jr., C.R.10
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25
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33644883681
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Discovery of S-[5-amino-1-(4-flurophenyl)-1H-pyrazol-4-yl]-[3-(2,3-dihydroxypropoxy) phenyl] methanone (RO3201195), an orally bioavailable and highly selective inhibitor of p38 MAP kinase
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Goldstein D.M., Alfredson T., Bertrand J., Browner M.F., Clifford K., Dalrymple S.A., Dunn J., Freire-Moar J., Harris S., Labadie S.S., et al. Discovery of S-[5-amino-1-(4-flurophenyl)-1H-pyrazol-4-yl]-[3-(2,3-dihydroxypropoxy) phenyl] methanone (RO3201195), an orally bioavailable and highly selective inhibitor of p38 MAP kinase. J Med Chem 49 (2006) 1562-1575
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J Med Chem
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Goldstein, D.M.1
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26
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14944358676
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R-130823, a novel inhibitor of p38 MAPK, ameliorates hyperalgesia and swelling in arthritis models
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50 = 22 nM), reduced hind paw swelling in rat adjuvant and murine collagen-induced arthritis. R-130823 also ameliorated hyperalgesia in adjuvant arthritis, with rapid onset and in association with COX-2 inhibition.
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50 = 22 nM), reduced hind paw swelling in rat adjuvant and murine collagen-induced arthritis. R-130823 also ameliorated hyperalgesia in adjuvant arthritis, with rapid onset and in association with COX-2 inhibition.
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Eur J Pharmacol
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Wada, Y.1
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Aoki, K.7
Kimura, T.8
Ushiyama, S.9
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27
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Novel inhibitor of p38 MAP kinase an an anti-TNF-α drug: discovery of N-[4-[2-ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]-2-pyridyl] benzamide (TAK-715) as a potent and orally active anti-rheumatoid arthritis agent
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Miwatashi S., Arikawa Y., Kotani E., Miyamoto M., Naruo K., Kimura H., Tanaka T., Asahi S., and Ohkawa S. Novel inhibitor of p38 MAP kinase an an anti-TNF-α drug: discovery of N-[4-[2-ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]-2-pyridyl] benzamide (TAK-715) as a potent and orally active anti-rheumatoid arthritis agent. J Med Chem 48 (2005) 5966-5979
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J Med Chem
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Miwatashi, S.1
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Sharrocks A.D. Cell cycle: sustained ERK signaling represses the inhibitors. Curr Biol 16 (2006) R540-R542
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Nishimoto S., and Nishida E. MAPK signalling: ERK5 versus ERK 1/2. EMBO Rep 7 (2006) 782-786
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Targeting the ERK signaling pathway in cancer therapy
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This review focused on assessing the biological potency of BAY 43-9006, PD184352, PD325901 and ARRY-142886 as Raf and MEK-1/2 inhibitors. The paper also discussed their future use as anti-cancer agents in combination with traditional anti-cancer therapies (i.e. cytotoxic agents).
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Kohno M., and Pouyssegur J. Targeting the ERK signaling pathway in cancer therapy. Ann Med 38 (2006) 200-211. This review focused on assessing the biological potency of BAY 43-9006, PD184352, PD325901 and ARRY-142886 as Raf and MEK-1/2 inhibitors. The paper also discussed their future use as anti-cancer agents in combination with traditional anti-cancer therapies (i.e. cytotoxic agents).
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Staehler M., Rohrmann K., Haseke N., Stief C.G., and Siebels M. Targeted agents for the treatment of advanced renal cell carcinoma. Curr Drug Targets 6 (2005) 835-846
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Wilhelm S.M., Carter C., Tang L.-Y., Wilkie D., McNabola A., Rong H., Chen C., Zhang X., Vincent P., McHugh M., et al. BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis. Cancer Res 64 (2004) 7099-7109
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High prevalence of BRAF mutations in thyroid cancer. Genetic evidence for constitutive activation of the RET/PTC-RAS-BRAF signaling pathway in papillary thyroid carcinoma
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BRAF mutation predicts sensitivity to MEK inhibition
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i = 300 nM in vitro) and anti-cancer agents will be highly dependent upon the level of MEK activity in B-Raf-positive tumors, which suggested a rational approach to the therapy of genetically defined tumors.
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i = 300 nM in vitro) and anti-cancer agents will be highly dependent upon the level of MEK activity in B-Raf-positive tumors, which suggested a rational approach to the therapy of genetically defined tumors.
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Nature
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®), a dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature
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®), a dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature. Methods Enzymol 407 (2005) 597-612
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Recent progress in targeting the Raf/MEK/ERK pathway with inhibitors in cancer drug discovery
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