Two additive mechanisms impair the differentiation of 'substrate-selective' p38 inhibitors from classical p38 inhibitors in vitro

BMC Systems Biology

Volumn 4, Issue , 2010, Pages

  Hendriks, Bart S ^a   Seidl, Kelly M ^a   Chabot, Jeffrey R ^a  

^a PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ACTIVATING TRANSCRIPTION FACTOR 2; ATF2 PROTEIN, HUMAN; MAP KINASE ACTIVATED KINASE 2; MAP-KINASE-ACTIVATED KINASE 2; MITOGEN ACTIVATED PROTEIN KINASE P38; PROTEIN KINASE INHIBITOR; PROTEIN SERINE THREONINE KINASE; SIGNAL PEPTIDE;

ARTICLE; BIOLOGICAL MODEL; CHEMICAL MODEL; CHEMISTRY; COMPUTER SIMULATION; DRUG ANTAGONISM; ENZYME SPECIFICITY; KINETICS; METABOLISM;

ACTIVATING TRANSCRIPTION FACTOR 2; COMPUTER SIMULATION; INTRACELLULAR SIGNALING PEPTIDES AND PROTEINS; KINETICS; MODELS, BIOLOGICAL; MODELS, CHEMICAL; P38 MITOGEN-ACTIVATED PROTEIN KINASES; PROTEIN KINASE INHIBITORS; PROTEIN-SERINE-THREONINE KINASES; SUBSTRATE SPECIFICITY;

EID: 77949464598     PISSN: None     EISSN: 17520509     Source Type: Journal    
DOI: 10.1186/1752-0509-4-23     Document Type: Article

References (31)

1. Gartlehner G, Hansen RA, Jonas BL, Thieda P, Lohr KN. The comparative efficacy and safety of biologics for the treatment of rheumatoid arthritis: a systematic review and metaanalysis. J Rheumatol 2006, 33(12):2398-2408.
2. Paul AT, Gohil VM, Bhutani KK. Modulating TNF-alpha signaling with natural products. Drug Discov Today 2006, 11(15-16):725-732. 10.1016/j.drudis.2006.06.002, 16846800.
3. Hitti E, Iakovleva T, Brook M, Deppenmeier S, Gruber AD, Radzioch D, Clark AR, Blackshear PJ, Kotlyarov A, Gaestel M. Mitogen-activated protein kinase-activated protein kinase 2 regulates tumor necrosis factor mRNA stability and translation mainly by altering tristetraprolin expression, stability, and binding to adenine/uridine-rich element. Mol Cell Biol 2006, 26(6):2399-2407. 10.1128/MCB.26.6.2399-2407.2006, 1430282, 16508014.
4. Kotlyarov A, Yannoni Y, Fritz S, Laass K, Telliez JB, Pitman D, Lin LL, Gaestel M. Distinct cellular functions of MK2. Mol Cell Biol 2002, 22(13):4827-4835. 10.1128/MCB.22.13.4827-4835.2002, 133920, 12052889.
5. Winzen R, Kracht M, Ritter B, Wilhelm A, Chen CY, Shyu AB, Muller M, Gaestel M, Resch K, Holtmann H. The p38 MAP kinase pathway signals for cytokine-induced mRNA stabilization via MAP kinase-activated protein kinase 2 and an AU-rich region-targeted mechanism. Embo J 1999, 18(18):4969-4980. 10.1093/emboj/18.18.4969, 1171568, 10487749.
6. Wrobleski ST, Doweyko AM. Structural comparison of p38 inhibitor-protein complexes: a review of recent p38 inhibitors having unique binding interactions. Curr Top Med Chem 2005, 5(10):1005-1016. 10.2174/1568026054985894, 16178743.
7. Goldstein DM, Gabriel T. Pathway to the clinic: inhibition of P38 MAP kinase. A review of ten chemotypes selected for development. Curr Top Med Chem 2005, 5(10):1017-1029. 10.2174/1568026054985939, 16178744.
8. Lee MR, Dominguez C. MAP kinase p38 inhibitors: clinical results and an intimate look at their interactions with p38alpha protein. Curr Med Chem 2005, 12(25):2979-2994. 10.2174/092986705774462914, 16378500.
9. Dominguez C, Powers DA, Tamayo N. p38 MAP kinase inhibitors: many are made, but few are chosen. Curr Opin Drug Discov Devel 2005, 8(4):421-430.
10. Popa-Burke I, Birkos S, Blackwell L, Cheatham L, Clark J, Dickson JK, Galasinski S, Janzen WP, Mendoza J, Miller JL, et al. Discovery of highly selective inhibitors of p38alpha. Curr Top Med Chem 2005, 5(10):941-951. 10.2174/1568026054985867, 16178739.
11. Dambach DM. Potential adverse effects associated with inhibition of p38alpha/beta MAP kinases. Curr Top Med Chem 2005, 5(10):929-939. 10.2174/1568026054985911, 16178738.
12. Xu JJ, Hendriks BS, Zhao J, de Graaf D. Multiple effects of acetaminophen and p38 inhibitors: towards pathway toxicology. FEBS Lett 2008, 582(8):1276-1282. 10.1016/j.febslet.2008.01.063, 18282474.
13. Duraisamy S, Bajpai M, Bughani U, Dastidar SG, Ray A, Chopra P. MK2: a novel molecular target for anti-inflammatory therapy. Expert opinion on therapeutic targets 2008, 12(8):921-936. 10.1517/14728222.12.8.921, 18620516.
14. Anderson DR, Meyers MJ, Vernier WF, Mahoney MW, Kurumbail RG, Caspers N, Poda GI, Schindler JF, Reitz DB, Mourey RJ. Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). Journal of medicinal chemistry 2007, 50(11):2647-2654. 10.1021/jm0611004, 17480064.
15. Davidson W, Frego L, Peet GW, Kroe RR, Labadia ME, Lukas SM, Snow RJ, Jakes S, Grygon CA, Pargellis C, et al. Discovery and characterization of a substrate selective p38alpha inhibitor. Biochemistry 2004, 43(37):11658-11671. 10.1021/bi0495073, 15362850.
16. Gupta S, Campbell D, Derijard B, Davis RJ. Transcription factor ATF2 regulation by the JNK signal transduction pathway. Science 1995, 267(5196):389-393. 10.1126/science.7824938, 7824938.
17. Kawasaki H, Schiltz L, Chiu R, Itakura K, Taira K, Nakatani Y, Yokoyama KK. ATF-2 has intrinsic histone acetyltransferase activity which is modulated by phosphorylation. Nature 2000, 405(6783):195-200. 10.1038/35012097, 10821277.
18. Vlahopoulos SA, Logotheti S, Mikas D, Giarika A, Gorgoulis V, Zoumpourlis V. The role of ATF-2 in oncogenesis. Bioessays 2008, 30(4):314-327. 10.1002/bies.20734, 18348191.
19. Waas WF, Lo HH, Dalby KN. The kinetic mechanism of the dual phosphorylation of the ATF2 transcription factor by p38 mitogen-activated protein (MAP) kinase alpha. Implications for signal/response profiles of MAP kinase pathways. J Biol Chem 2001, 276(8):5676-5684. 10.1074/jbc.M008787200, 11069918.
20. Pargellis C, Tong L, Churchill L, Cirillo PF, Gilmore T, Graham AG, Grob PM, Hickey ER, Moss N, Pav S, et al. Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site. Nat Struct Biol 2002, 9(4):268-272. 10.1038/nsb770, 11896401.
21. Chen G, Porter MD, Bristol JR, Fitzgibbon MJ, Pazhanisamy S. Kinetic mechanism of the p38-alpha MAP kinase: phosphoryl transfer to synthetic peptides. Biochemistry 2000, 39(8):2079-2087. 10.1021/bi9919495, 10684658.
22. Citri A, Yarden Y. EGF-ERBB signalling: towards the systems level. Nat Rev Mol Cell Biol 2006, 7(7):505-516. 10.1038/nrm1962, 16829981.
23. Schieven GL. The biology of p38 kinase: a central role in inflammation. Curr Top Med Chem 2005, 5(10):921-928. 10.2174/1568026054985902, 16178737.
24. ten Hove W, Houben LA, Raaijmakers JA, Bracke M, Koenderman L. Differential regulation of TNFalpha and GM-CSF induced activation of P38 MAPK in neutrophils and eosinophils. Mol Immunol 2007, 44(9):2492-2496. 10.1016/j.molimm.2006.10.009, 17126905.
25. Mihara K, Almansa C, Smeets RL, Loomans EE, Dulos J, Vink PM, Rooseboom M, Kreutzer H, Cavalcanti F, Boots AM, et al. A potent and selective p38 inhibitor protects against bone damage in murine collagen-induced arthritis: a comparison with neutralization of mouse TNFalpha. Br J Pharmacol 2008, 154(1):153-164. 10.1038/bjp.2008.53, 2438984, 18297096.
26. Gallin EK, Mason TM, Moran A. Characterization of regulatory volume decrease in the THP-1 and HL-60 human myelocytic cell lines. Journal of cellular physiology 1994, 159(3):573-581. 10.1002/jcp.1041590321, 7514614.
27. Oehler R, Zellner M, Hefel B, Weingartmann G, Spittler A, Struse HM, Roth E. Influence of heat shock on cell volume regulation: protection from hypertonic challenge in a human monocyte cell line. Faseb J 1998, 12(7):553-560.
28. Yasaka T, Mantich NM, Boxer LA, Baehner RL. Functions of human monocyte and lymphocyte subsets obtained by countercurrent centrifugal elutriation: differing functional capacities of human monocyte subsets. J Immunol 1981, 127(4):1515-1518.
29. Morton S, Davis RJ, Cohen P. Signalling pathways involved in multisite phosphorylation of the transcription factor ATF-2. FEBS Lett 2004, 572(1-3):177-183. 10.1016/j.febslet.2004.07.031, 15304344.
30. Szafranska AE, Dalby KN. Kinetic mechanism for p38 MAP kinase alpha. A partial rapid-equilibrium random-order ternary-complex mechanism for the phosphorylation of a protein substrate. Febs J 2005, 272(18):4631-4645. 10.1111/j.1742-4658.2005.04827.x, 16156785.
31. Lukas SM, Kroe RR, Wildeson J, Peet GW, Frego L, Davidson W, Ingraham RH, Pargellis CA, Labadia ME, Werneburg BG. Catalysis and function of the p38 alpha. MK2a signaling complex. Biochemistry 2004, 43(31):9950-9960. 10.1021/bi049508v, 15287722.