TNF α signaling beholds thalidomide saga: A review of mechanistic role of TNF-α signaling under thalidomide

Current Topics in Medicinal Chemistry

Volumn 12, Issue 13, 2012, Pages 1456-1467

  Majumder, Syamantak ^a   Sreedhara, Sree Rama Chaitanya ^a   Banerjee, Santanu ^a   Chatterjee, Suvro ^a  

^a ANNA UNIVERSITY   (India)

Author keywords

Cytokines; Inflammation; Myeloid differentiation factor 88; Nuclear factor kappa B; Thalidomide; Tumor necrosis factor a

Indexed keywords

ADALIMUMAB; APREMILAST; DEXAMETHASONE; ETANERCEPT; IMMUNOGLOBULIN ENHANCER BINDING PROTEIN; INFLIXIMAB; INTERLEUKIN 1; INTERLEUKIN 12; INTERLEUKIN 18; INTERLEUKIN 1BETA; INTERLEUKIN 8; LENALIDOMIDE; MESSENGER RNA; MYELOID DIFFERENTIATION FACTOR 88; OROSOMUCOID; PENTOXIFYLLINE; POMALIDOMIDE; REACTIVE OXYGEN METABOLITE; THALIDOMIDE; TUMOR NECROSIS FACTOR ALPHA;

ALLERGIC PNEUMONITIS; ANTIINFLAMMATORY ACTIVITY; B LYMPHOCYTE; B LYMPHOCYTE ACTIVATION; CYTOKINE PRODUCTION; DOWN REGULATION; HUMAN; IMMUNITY; LUNG FIBROSIS; NONHUMAN; PROTEIN EXPRESSION; REVIEW; SARCOIDOSIS; SIGNAL TRANSDUCTION;

ANIMALS; ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL; HUMANS; REACTIVE OXYGEN SPECIES; RNA, MESSENGER; SIGNAL TRANSDUCTION; THALIDOMIDE; TUMOR NECROSIS FACTOR-ALPHA;

EID: 84864543115     PISSN: 15680266     EISSN: 18734294     Source Type: Journal    
DOI: 10.2174/156802612801784443     Document Type: Review

References (149)

1. Tang, X.; Metzger, D.; Leeman, S.; Amar, S. LPS-induced TNF-[factor (LITAF)-deficient mice express reduced LPS-induced cytokine: Evidence for LITAF-dependent LPS signaling pathways. Proc. Natl. Acad. Sci. USA., 2006, 103, 13777-13782.
2. Kim, Y.; So, H.S.; Moon, B.S.; Youn, M.J.; Kim, H.J.; Shin, Y.I.; Moon, S.K.; Song, M.S.; Choi, K.Y.; Song, J.; Park, R. Sasim attenuates LPS-induced TNF-LLproduction through the induction of HO-1 in THP-1 differentiated macrophage-like cells. J. Ethnopharmacol., 2008, 119, 122-128.
3. Nakae, S.; Komiyama, Y.; Narumi, S.; Sudo, K.; Horai, R.; Tagawa, Y.; Sekikawa, K.; Matsushima, K.; Asano, M.; Iwakura, Y. IL-1-induced tumor necrosis factor-alpha elicits inflammatory cell infiltration in the skin by inducing IFN-gamma-inducible protein 10 in the elicitation phase of the contact hypersensitivity response. Int. Immunol., 2003, 15, 251-260.
4. Deshpande, S.S.; Angkeow, P.; Huang, J.; Ozaki, M.; Irani, K. Rac1 inhibits TNF-alpha-induced endothelial cell apoptosis: dual regulation by reactive oxygen. FASEB J., 2000, 14, 1705-1714.
5. Van Antwerp, D.J.; Martin, S.J.; Kafri, T.; Green, D.R.; Verma, I.M. Suppression of TNF-alpha-induced apoptosis by NF-kappaB. Science, 1996, 274, 787-789.
6. Hernandez-Pando, R.; Rook, G.A. The role of TNF-alpha in T-cellmediated inflammation depends on the Th1/Th2 cytokine balance. Immunology. 1994, 82, 591-595.
7. Lane, B.R.; Markovitz, D.M.; Woodford, N.L.; Rochford, R.; Strieter, R.M.; Coffey, M.J. NF-alpha inhibits HIV-1 replication in peripheral blood monocytes and alveolar macrophages by inducing the production of RANTES and decreasing C-C chemokine receptor 5 (CCR5) expression. J. Immunol., 1999, 63, 3653-3661.
8. Locksley, R.M.; Killeen, N.; Lenardo, M.J. The TNF and TNF receptor superfamilies: integrating mammalian biology. Cell. 2001. 104, 487-501.
9. Korzenik, JR. Crohn's disease: future anti-tumor necrosis factor therapies beyond infliximab. Gastroenterol Clin North Am., 2004, 33, 285-301.
10. Rutgeerts, P.; Van Assche, G.; Vermeire, S. Optimizing anti-TNF treatment in inflammatory bowel disease. Gastroenterology., 2004, 126, 1593-1610.
11. Pearson, J.M.; Vedagiri, M. Treatment of moderately severe erythema nodosum leprosum with thalidomide--a double-blind controlled trial. Lepr Rev., 40, 111-116.
12. Wilhelm, S.M.; Taylor, J.D.; Osiecki. L.L.; Kale-Pradhan, P.B. Novel therapies for Crohn's disease: focus on immunomodulators and antibiotics. Ann Pharmacother., 2006, 40, 1804-1813.
13. Randall, T. Thalidomide has 37-year history. JAMA. 1990, 263, 1474.
14. Melchert, M.; List, A. The thalidomide saga. Int J Biochem Cell Biol., 2007, 39, 1489-1499.
15. Noman, A.S.; Koide, N.; Hassan, F.; I-E-Khuda, I.; Dagvadorj, J.; Tumurkhuu, G.; Islam, S.; Naiki, Y.; Yoshida, T.; Yokochi, T. Thalidomide inhibits lipopolysaccharide-induced tumor necrosis factor-alpha production via down-regulation of MyD88 expression. Innate Immun. 2009, 15, 33-41.
16. Yagyu, T.; Kobayashi, H.; Matsuzaki, H.; Wakahara, K.; Kondo, T.; Kurita, N.; Sekino, H.; Inagaki, K.; Suzuki, M.; Kanayama, N.; Terao, T. Thalidomide inhibits tumor necrosis factor-alpha-induced interleukin-8 expression in endometriotic stromal cells, possibly through suppression of nuclear factor-kappaB activation. J Clin Endocrinol Metab., 2005, 90, 3017-3021.
17. Walker, S.L.; Waters, M.F.; Lockwood, DN. The role of thalidomide in the management of erythema nodosum leprosum. Lepr Rev., 2007, 78, 197-215.
18. Yagyu, T.; Kobayashi, H.; Matsuzaki, H.; Wakahara, K.; Kondo, T.; Kurita, N.; Sekino, H.; Inagaki, K.; Suzuki, M.; Kanayama, N.; Terao, T. Thalidomide inhibits tumor necrosis factor-alpha-induced interleukin-8 expression in endometriotic stromal cells, possibly through suppression of nuclear factor-kappaB activation. J Clin Endocrinol Metab., 2005, 90, 3017-3021.
19. Kim, Y.S.; Kim, J.S.; Jung, H.C.; Song, IS. The effects of thalidomide on the stimulation of NF-kappaB activity and TNF-alpha production. Mol Cells., 2004, 17, 210-6.
20. Noman, A.S.; Koide, N.; Hassan, F.; I-E-Khuda, I.; Dagvadorj, J.; Tumurkhuu, G.; Islam, S.; Naiki, Y.; Yoshida, T.; Yokochi, T. Thalidomide inhibits lipopolysaccharide-induced tumor necrosis factor-alpha production via down-regulation of MyD88 expression. Innate Immun. 2009, 15, 33-41.
21. Moreira, A.L.; Sampaio, E.P.; Zmuidzinas, A.; Frindt, P.; Smith, K.A.; Kaplan, G. Thalidomide exerts its inhibitory action on tumor necrosis factor alpha by enhancing mRNA degradation. J. Exp. Med., 1993, 177, 1675-1680.
22. Sampaio, E.P.; Sarno, E.N.; Galilly, R.; Cohn, Z.A.; Kaplan, G. Thalidomide selectively inhibits tumor necrosis factor alpha production by stimulated human monocytes. J. Exp. Med., 1991, 173, 699-703.
23. Rowland, T.L.; McHugh, S.M.; Deighton, J.; Ewan, P.W.; Dearman, R.J.; Kimber, I. Selective down-regulation of T cell-and non-T cell-derived tumour necrosis factor alpha by thalidomide: comparisons with dexamethasone. Immunol Lett., 1999, 68, 325-332.
24. Carswell, E.; Old, L.; Kassel, R.; Green, N.; Fiore, N.; Williamson, B. An Endotoxin-Induced Serum Factor that Causes Necrosis of Tumors. Proceedings of the National Academy of Science. 1975, 72, 3666-3670.
25. Janeway, C.; Travers, P.; Walport, M.; Capra, J. Immunobiology: The Immune System in Health and Disease. New York, N.Y. Garland Publishers. 1999.
26. Rink, L.; Kirchner, H. Recent Progress in the Tumor Necrosis Factor-Alpha Field. International Archives of Allergy and Immunology. 1996, 111, 199-209.
27. Strieter, R.; Kunkel, S.; Bone, R. Role of Tumor Necrosis Factor-Alpha in Disease States and Inflammation. Critical Care Medicine. 1993, 21, S447-S463.
28. Tracey, K.; Cerami, A. Metabolic Response to Cachectin/TNF. Annals of the New York Academy of Sciences. 1990, 587.
29. Tracey, K.; Cerami, A. Tumor Necrosis Factor: A Pleiotropic Cytokine and Therapeutic Target. Annual Review of Medicine. 1994, 45, 491-503.
30. Beutler, B.; Greenwald, D.; Hulmes, J.; Chang, M.; Pan, Y.; Mathison, J.; Ulevitch, R.; Cerami, A. Identity of Tumour Necrosis Factor and the Macrophage-Secreted Factor Cachectin. Nature. 1985, 316, 552-554.
31. Haitian, L.U.; Ouyang, W.; Huang, C. Inflammation, a Key Event in Cancer Development. Mol Cancer Res., 2006, 4, 221-233.
32. Ye, Q.; Chen, B.; Tong, Z.; Nakamura, S.; Sarria, R.; Costabel, U.; Guzman, J. Thalidomide reduces IL-18, IL-8 and TNF-a release from alveolar macrophages in interstitial lung disease. Eur Respir J., 2006, 28, 824-831.
33. Park, S.J.; Kim, H.S.; Yang, H.O.; Park, K.W.; Youn, S.W.; Jeon, S.I.; Kim, D.H.; Koo, B.K.; Chae, I.H.; Choi, D.J.; Oh, B.H.; Lee, M.M.; Park, Y.B. Thalidomide as a Potent Inhibitor of Neointimal Hyperplasia After Balloon Injury in Rat Carotid Artery. Arterioscler. Thromb. Vasc. Biol., 2004, 24, 885-891.
34. Kumar, V.; Harjai, K.; Chhibber, S. A combination of thalidomide and augmentin protects BALB/c mice suffering from Klebsiella pneumoniae B5055-induced sepsis. J Chemother., 2009, 21, 159-164.
35. Kumar, V.; Chhibber, S. Anti-inflammatory effect of thalidomide alone or in combination with augmentin in Klebsiella pneumoniae B5055 induced acute lung infection in BALB/c mice. Eur. J. Pharmacol., 2008, 592:146-150.
36. Rodrigues, G.B.; Passos, G.F.; Di Giunta, G.; Figueiredo, C.P.; Rodrigues, E.B.; Grumman, A. Jr,; Medeiros, R.; Calixto, J.B. Pre ventive and therapeutic anti-inflammatory effects of systemic and topical thalidomide on endotoxin-induced uveitis in rats. Exp. Eye. Res., 2007, 84, 553-560.
37. Chen, X.; El Gazzar, M.; Yoza, B.K.; McCall, C.E. The NFkappaB factor RelB and histone H3 lysine methyltransferase G9a directly interact to generate epigenetic silencing in endotoxin tolerance. J. Biol. Chem., 2009.
38. Tweedie, D.; Sambamurti, K.; Greig, N.H. TNF-alpha inhibition as a treatment strategy for neurodegenerative disorders: new drug candidates and targets. Curr. Alzheimer Res., 2007, 4, 378-385.
39. Eski, M.; Sahin, I.; Sengezer, M.; Serdar, M.; Ifran, A. Thalidomide decreases the plasma levels of IL-1 and TNF following burn injury: is it a new drug for modulation of systemic inflammatory response. Burns., 2008, 34, 104-108.
40. Deng, L.; Ding, W.; Granstein, R.D. Thalidomide inhibits tumor necrosis factor-alpha production and antigen presentation by Langerhans cells. J. Invest. Dermatol., 2003, 121, 1060-1065.
41. Lin, J.H.; Yang, X.; Bostrom, M.P. Thalidomide blocking of particle-induced TNFalpha release in vitro. J. Orthop. Sci., 2003, 8, 79-83.
42. Ye, Q.; Chen, B.; Tong, Z.; Nakamura, S.; Sarria, R.; Costabel, U.; Guzman, J. Thalidomide reduces IL-18, IL-8 and TNF-alpha release from alveolar macrophages in interstitial lung disease. Eur. Respir J., 2006, 28, 824-831.
43. Giamarellos-Bourboulis, E.J.; Poulaki, H.; Kostomitsopoulos, N.; Dontas, I.; Perrea, D.; Karayannacos, P.E.; Giamarellou, H. Effective immunomodulatory treatment of Escherichia coli experimental sepsis with thalidomide. Antimicrob. Agents Chemother., 2003, 47, 2445-2449.
44. Giamarellos-Bourboulis, E.J.; Bolanos, N.; Laoutaris, G.; Papadakis, V.; Koussoulas, V.; Perrea, D.; Karayannacos, P.E.; Giamarellou, H. Immunomodulatory intervention in sepsis by multidrugresistant Pseudomonas aeruginosa with thalidomide: an experimental study. BMC Infect. Dis., 2005, 26, 51.
45. Barnes, P.F.; Chatterjee, D.; Brennan, P.J.; Rea, T.H.; Modlin, R.L. Tumor necrosis factor production in patients with leprosy. Infect Immun., 1992, 60, 1441-1446
46. Tadesse, A.; Shannon, E.J. Effects of thalidomide on intracellular Mycobacterium leprae in normal and activated macrophages. Clin Diagn Lab Immunol., 2005, 12, 130-134.
47. Scollard, D.M.; Adams, L.B.; Gillis, T.P.; Krahenbuhl, J.L.; Truman, R.W.; Williams, D.L. The continuing challenges of leprosy. Clin Microbiol Rev., 2006, 19, 338-381.
48. Teo, S.K.; Resztak, K.E.; Scheffler, M.A.; Kook, K.A.; Zeldis, J.B.; Stirling, D.I.; Thomas, S.D. Thalidomide in the treatment of leprosy. Microbes Infect., 2002, 4, 1193-1202.
49. Melo, M.L.; Brito, G.A.; Soares, R.C.; Carvalho, S.B.; Silva, J.V.; Soares, P.M.; Vale, M.L.; Souza, M.H.; Cunha, F.Q.; Ribeiro, R.A. Role of cytokines (TNF-alpha, IL-1beta and KC) in the pathogenesis of CPT-11-induced intestinal mucositis in mice: effect of pentoxifylline and thalidomide. Cancer Chemother Pharmacol., 2008, 61, 775-784.
50. Ye, Q.; Chen, B.; Tong, Z.; Nakamura, S.; Sarria, R.; Costabel, U.; Guzman, J. Thalidomide reduces IL-18, IL-8 and TNF-alpha release from alveolar macrophages in interstitial lung disease. Eur Respir J. 2006, 28, 824-831.
51. Klausner, J.D.; Makonkawkeyoon, S.; Akarasewi, P. et al. The effect of thalidomide on the pathogenesis of human immunodeficiency virus type 1 and M. tuberculosis infection. J Acquir Immune Defic Syndr Hum Retrovirol., 1996, 11, 247-257.
52. Schuler, U., Ehninger, G. Thalidomide: rationale for renewed use in immunological disorders. Drug Saf., 1995, 12, 364-369.
53. Jacobson, J.M.; Greenspan, J.S.; Spritzler, J., et al. Thalidomide for the treatment of oral aphthous ulcers in patients with human immunodeficiency virus infection. N. Engl. J. Med., 1997, 336, 1487-1493.
54. Vogelsang, G.B.; Farmer, E.R.; Hess, A.D., et al. Thalidomide for the treatment of chronic graft-versus-host disease. N. Engl. J. Med., 1992, 326, 1055-1058.
55. Yaccoby, S.; Johnson, C.L.; Mahaffey, S.C.; Wezeman, M.J.; Barlogie, B.; Epstein, J. Antimyeloma efficacy of thalidomide in the SCID-hu model. Blood. 2002, 100, 4162-4168.
56. Castilla, E.E.; Ashton-Prolla, P.; Barreda-Mejia, E.; et al. Thalidomide, a current teratogen in South America. Tera-tology. 1996, 54, 273-277.
57. Tseng, S.; Pak, G.; Washenik, K.; Pomeranz, M.K.; Shupack, J.L. Rediscovering thalidomide: a review of its mechanism of action, side effects, and potential uses. J. Am. Acad. Dermatol., 1996, 35, 969-979.
58. Majumder, S.; Rajaram, M.; Muley, A.; Reddy, H.S.; Tamilarasan, K.; Kolluru, G.K.; Sinha, S.; Siamwala, J.H.; Gupta, R.; Ilavarasan, R.; Venkataraman, S.; Sivakumar, K.; Anishetty, S.; Kumar, P.G.; Chatterjee, S. Thalidomide attenuates nitric oxide-driven angiogenesis by interacting with soluble guanylyl cyclase. Br J Pharmacol. 2009 [Epub ahead of print].
59. Fernandes, D.; Sordi, R.; Pacheco, L.K.; Nardi, G.M.; Heckert, B.T.; Villela, C.G.; Lobo, A.R.; Barja-Fidalgo, C.; Assreuy, J. Late, but not early, inhibition of soluble guanylate cyclase decreases mortality in a rat sepsis model. J Pharmacol Exp Ther. 2009, 328, 991-999.
60. Tamilarasan, K.P.; Kolluru, G.K.; Rajaram, M.; Indhumathy, M.; Saranya, R.; Chatterjee, S. Thalidomide attenuates nitric oxide mediated angiogenesis by blocking migration of endothelial cells. BMC Cell Biol. 2006, 4, 7-17.
61. Gunzler, V. Thalidomide in human immunodeficiency virus (HIV) patients. A review of safety considerations. Drug Saf. 1992, 7, 116-134.
62. Muller, G.W.; Corral, L.G.; Shire, M.G.; et al. Structural modifications of thalidomide produce analogs with enhanced tumor necrosis factor inhibitory activity. J Med Chem. 1996, 39, 3238-3240.
63. Muller, G.W.; Shire, M.G.; Wong, L.M.; et al. Thalidomide analogs and PDE4 inhibition. Bioorg Med Chem Lett. 1998, 8, 2669-2674.
64. Muller, G.W.; Chen, R.; Huang, S.Y.; et al. Amino-substituted thalidomide analogs: potent inhibitors of TNF-alpha production. Bioorg Med Chem Lett. 1999, 9, 1625-1630.
65. Nakamura, T.; Noguchi, T.; Kobayashi, H.; Miyachi, H.; Hashimoto, Y. Mono-and dihydroxylated metabolites of thalidomide: synthesis and TNF-alpha production-inhibitory activity. Chem Pharm Bull (Tokyo). 2006, 54, 1709-1714.
66. de Almeida, M.V.; Teixeira, F.M.; de Souza, M.V.; Amarante, G.W.; Alves, C.C.; Cardoso, S.H.; Mattos, A.M.; Ferreira, A.P.; Teixeira, H.C. Thalidomide analogs from diamines: Synthesis and evaluation as inhibitors of TNF-alpha production. Chem Pharm Bull (Tokyo). 2007, 55, 223-226.
67. Greig, N.H.; Giordano, T.; Zhu, X.; Yu, Q.S.; Perry, T.A.; Holloway, H.W.; Brossi, A.; Rogers, J.T.; Sambamurti, K.; Lahiri, D.K. Thalidomide-based TNF-alpha inhibitors for neurodegenerative diseases. Acta Neurobiol Exp (Wars). 2004, 64, 1-9.
68. Luzzio, F.A.; Mayorov, A.V.; Ng, S.S.; Kruger, E.A.; Figg, W.D. Thalidomide metabolites and analogues. 3. Synthesis and antiangiogenic activity of the teratogenic and TNFalpha-modulatory thalidomide analogue 2-(2,6-dioxopiperidine-3-yl)phthalimidine. J Med Chem. 2003, 46, 3793-3799.
69. Thiele, A.; Bang, R.; Gütschow, M.; Rossol, M.; Loos, S.; Eger, K.; Tiegs, G.; Hauschildt, S. Cytokine modulation and suppression of liver injury by a novel analogue of thalidomide. Eur J Pharmacol. 2002, 453, 325-334.
70. Zhu, X.; Giordano, T.; Yu, Q.S.; Holloway, H.W.; Perry, T.A.; Lahiri, D.K.; Brossi, A.; Greig, N.H. Thiothalidomides: novel isosteric analogues of thalidomide with enhanced TNF-alpha inhibitory activity. J Med Chem. 2003, 46, 5222-5229.
71. Corral, L.G.; Kaplan, G. Immunomodulation by thalidomide and thalidomide analogues. Ann Rheum Dis. 1999, 1, 107-113.
72. Corral, L.G.; Muller, G.W.; Moreira, A.L.; et al. Selection of novel analogs of thalidomide with enhanced tumor necrosis factor alpha inhibitory activity. Mol Med. 1996, 2, 506-515.
73. Oliver, S.J.; Freeman, S.L.; Corral, L.G.; Ocampo, C.J.; Kaplan, G. Thalidomide analogue CC1069 inhibits development of rat adjuvant arthritis. Clin Exp Immunol. 1999, 118, 315-321.
74. Marriott, J.B.; Westby, M.; Cookson, S.; Guckian, M.; Goodbourn, S.; Muller, G.; Shire, M.G.; Stirling, D.; Dalgleish, A, G. CC-3052: a water-soluble analog of thalidomide and potent inhibitor of activation-induced TNF-alpha production. J Immunol. 1998, 161, 4236-4243.
75. Shannon, E.; Noveck, R.; Sandoval, F.; Kamath, B.; Kearney, M. Thalidomide suppressed interleukin-6 but not tumor necrosis factor-alpha in volunteers with experimental endotoxemia. Transl Res. 2007, 150, 275-280.
76. Shannon, E.; Noveck, R.; Sandoval, F.; Kamath, B. Thalidomide suppressed IL-1beta while enhancing TNF-alpha and IL-10, when cells in whole blood were stimulated with lipopolysaccharide. Immunopharmacol Immunotoxicol. 2008, 30, 447-457.
77. Moreira, A.L.; Kaplan, G.; Villahermosa, L.G.; Fajardo, T.J.; Abalos, R.M.; Cellona, R.V.; Balagon, M.V.; Tan, E.V.; Walsh, G.P. Comparison of pentoxifylline, thalidomide and prednisone in the treatment of ENL. Int J Lepr Other Mycobact Dis 1998, 66: 61-65.
78. Villahermosa, L.G.; Fajardo, T.T.; Abalos, R.M.; Balagon, M.V.; Tan, E.V.; Cellona, R.V.; Palmer, J.P.; Wittes, J.; Thomas, S.D.; Kook, K.A.; Walsh, G.P.; Walsh, D.S. A randomized, doubleblind, double-dummy, controlled dose comparison of thalidomide for treatment of erythema nodosum leprosum. Am J Trop Med Hyg. 2005, 72, 518-526.
79. Fujimoto, H., Noguchi, T., Kobayashi, H., Miyachi, H., Hashimoto, Y. Effects of immunomodulatory derivatives of thalidomide (IMiDs) and their analogs on cell-differentiation, cyclooxygenase activity and angiogenesis. Chem Pharm Bull (Tokyo). 2006, 54, 855-860.
80. Aragon-Ching, J.B.; Li, H.; Gardner, E.R.; Figg, W.D. Thalidomide analogues as anticancer drugs. Recent Pat Aniticancer Drug Discov. 2007, 2, 167-174.
81. Schafer, P.H.; Parton, A.; Gandhi, A.K.; Capone, L.; Adams, M.; Wu, L.; Bartlett, J.B.; Loveland, M.A.; Gilhar, A.; Cheung, Y.F.; Baillie, G.S.; Houslay, M.D.; Man, H.W.; Muller, G.W.; Stirling, D.I. Apremilast, a cAMP phosphodiesterase-4 inhibitor, demonstrates anti-inflammatory activity in vitro and in a model of psoriasis. Br J Pharmacol. 2010, 159, 842-855.
82. Lentzsch, S.; LeBlanc, R.; Podar, K.; Davies, F.; Lin, B.; Hideshima, T.; Catley, L.; Stirling, D.I.; Anderson, K.C. Immunomodulatory analogs of thalidomide inhibit growth of Hs Sultan cells and angiogenesis in vivo. Leukemia. 2003, 17, 41-44.
83. Schey, S.A.; Fields, P.; Bartlett, J.B.; Clarke, I.A.; Ashan, G.; Knight, R.D.; Streetly, M.; Dalgleish, A.G. Phase I study of an immunomodulatory thalidomide analog, CC-4047, in relapsed or refractory multiple myeloma. J Clin Oncol. 2004, 22, 3269-3276.
84. Guckian, M.; Dransfield, I.; Hay, P.; Dalgleish, A.G. Thalidomide analogue CC-3052 reduces HIV+ neutrophil apoptosis in vitro. Clin Exp Immunol. 2000, 121, 472-479.
85. Dredge, K.; Marriott, J.B.; Todryk, S.M.; Muller, G.W.; Chen, R.; Stirling, D.I.; Dalgleish, A.G. Protective antitumor immunity induced by a costimulatory thalidomide analog in conjunction with whole tumor cell vaccination is mediated by increased Th1-type immunity. J Immunol. 2002, 168, 4914-4919.
86. Hideshima, T.; Chauhan, D.; Shima, Y.; Raje, N.; Davies, F.E.; Tai, Y.T.; Treon, S.P.; Lin, B.; Schlossman, R.L.; Richardson, P.; Muller, G.; Stirling, D.I.; Anderson, K.C. Thalidomide and its analogs overcome drug resistance of human multiple myeloma cells to conventional therapy. Blood. 2000, 96, 2943-2950.
87. Marriott, J.B.; Clarke, I.A.; Czajka, A.; Dredge, K.; Childs, K.; Man, H.W.; Schafer, P.; Govinda, S.; Muller, G.W.; Stirling, D.I., Dalgleish, A.G. A novel subclass of thalidomide analogue with anti-solid tumor activity in which caspase-dependent apoptosis is associated with altered expression of bcl-2 family proteins. Cancer Res. 2003, 63, 593-599.
88. Therapontos, C.; Erskine, L.; Gardner, E.R.; Figg, W.D.; Vargesson, N. Thalidomide induces limb defects by preventing angiogenic outgrowth during early limb formation. Proc Natl Acad Sci U S A. 2009, 106, 8573-8578.
89. Kumar, S.; Raje, N.; Hideshima, T.; Ishitsuka, K.; Roccaro, A.; Shiraishi, N.; Hamasaki, M.; Yasui, H.; Munshi, N.C.; Richardson, P.; Figg, W.D.; Anderson, K.C. Antimyeloma activity of two novel N-substituted and tetraflourinated thalidomide analogs. Leukemia. 2005, 19, 1253-1261.
90. Ng, S.S., Gütschow, M., Weiss, M., Hauschildt, S., Teubert, U., Hecker, T.K., Luzzio, F.A., Kruger, E.A., Eger, K., Figg, W.D. Antiangiogenic activity of N-substituted and tetrafluorinated thalidomide analogues. Cancer Res. 2003, 6, 3189-3194.
91. Lentzsch, S.; Rogers, M.S.; LeBlanc, R.; Birsner, A.E.; Shah, J.H.; Treston, A.M.; Anderson, K.C.; D'Amato, R.J. S-3-Aminophthalimido-glutarimide inhibits angiogenesis and growth of B-cell neoplasias in mice. Cancer Res. 2002, 62, 2300-2305.
92. Fernández-Martínez, E.; Morales-Ríos, M.S.; Pérez-Alvarez, V.; Muriel, P. Immunomodulatory effects of thalidomide analogs on LPS-induced plasma and hepatic cytokines in the rat. Biochem Pharmacol. 2004, 68, 1321-1329.
93. Shibata, N.; Yamamoto, T.; Toru, T. Synthesis of Thalidomide, Bioactive Heterocycles II. Top Heterocycl Chem. 2007, 8, 73-97.
94. Bartlett, J.B.; Dredge, K.; Dalgleish, A.G. The evolution of thalidomide and its IMiD derivatives as anticancer agents. Nat Rev Cancer. 2004, 4, 314-322
95. Sharma, R.; Sharma, C.L. TNF-alpha inhibitors: Current indications. Indian J Crit Care Med. 2007, 11, 139-148.
96. Stephens, T.D.; Bundea, C.J.W.; Fillmore, B.J. Mechanism of action in thalidomide teratogenesis. Biochemical Pharmacology. 2000, 59, 1489-1499.
97. Balleza, E.; López-Bojorquez, L.N.; Martínez-Antonio, A.; Resendis-Antonio, O.; Lozada-Chávez, I.; Balderas-Martínez, Y.I.; Encarnación, S.; Collado-Vides, J. Regulation by transcription factors in bacteria: beyond description. FEMS Microbiol Rev. 2009, 33, 133-151.
98. Rayet, B.; Gélinas, C. Aberrant rel/NF-kB genes and activity in human cancer. Oncogene. 1999, 18, 6938-6947.
99. Liebermann, D.A.; Hoffman, B. Myeloid differentiation (MyD)/growth arrest DNA damage (GADD) genes in tumor suppression, immunity and inflammation. Leukemia. 2002, 16, 527-541.
100. Royds, J.A.; Dower, S.K.; Qwarnstrom, E.E.; Lewis, C.W. Response of tumour cells to hypoxia: role of p53 and NF-kB. Mol Pathol. 1998, 51, 55-61.
101. Majumdar, S.; Lamothe, B.; Aggarwal, B.B. Thalidomide suppresses NF-kappa B activation induced by TNF and HO, but not that activated by ceramide, lipopolysaccharides, or phorbol ester. J Immunol. 2002, 168, 2644-2651.
102. Karin, M.; Ben-Neriah, Y. Phosphorylation meets ubiquitination: the control of NF-[kappa]B activity. Annu Rev Immunol. 2000, 18, 621-663.
103. Vallabhapurapu, S.; Karin, M. Regulation and function of NFkappaB transcription factors in the immune system. Annu Rev Immunol. 2009, 27, 693-733.
104. Keifer, J.A.; Guttridge, D.C.; Ashburner, B.P.; Baldwin, A.S. Jr;. Inhibition of NF-kappa B activity by thalidomide through suppression of IkappaB kinase activity. J Biol Chem. 2001, 276, 22382-22387.
105. Villalona-Calero, M.; Schaaf, L.; Phillips, G.; Otterson, G.; Panico, K.; Duan, W.; Kleiber, B.; Shah, M.; Young, D.; Wu, W.H.; Kuhn, J. Thalidomide and celecoxib as potential modulators of irinotecan's activity in cancer patients. Cancer Chemother Pharmacol. 2007, 59, 23-33.
106. Li, M.; Sun, W.; Yang, Y.P.; Xu, B.; Yi, W.Y.; Ma, Y.X.; Li, Z.J.; Cui, J.R. In vitro anticancer property of a novel thalidomide analogue through inhibition of NF-kappaB activation in HL-60 cells. Acta Pharmacol Sin. 2009, 30, 134-140.
107. Paul, S.C.; Lv, P.; Xiao, Y.J.; An, P.; Liu, S.Q.; Luo, H.S. Thalidomide in rat liver cirrhosis: blockade of tumor necrosis factoralpha via inhibition of degradation of an inhibitor of nuclear factorkappaB. Pathobiology. 2006, 73, 82-92.
108. Mitsiades, N.; Mitsiades, C.S.; Poulaki, V.; Chauhan, D.; Richardson, P.G.; Hideshima, T.; Munshi, N.C.; Treon, S.P.; Anderson, K.C. Apoptotic signaling induced by immunomodulatory thalidomide analogs in human multiple myeloma cells: therapeutic implications. Blood. 2002, 99, 4525-4530.
109. Ohnishi, H.; Tochio, H.; Kato, Z.; Orii, K.E.; Li, A.; Kimura, T.; Hiroaki, H.; Kondo, N.; Shirakawa, M. Structural basis for the multiple interactions of the MyD88 TIR domain in TLR4 signaling. Proc Natl Acad Sci U S A. 2009, 106, 10260-10265.
110. Liebermann, D.A.; Hoffman, B. Myeloid Differentiation (MyD)/Growth Arrest DNA Damage (GADD) genes in tumorsuppression, immunity and inflammation. Leukemia. 2002, 16, 527-541.
111. Kawai, T.; Akira, S. Toll-like receptor downstream signaling. Arthritis Res Ther. 2005, 7,12-19.
112. Nandi, D.; Tahiliani, P.; Kumar, A.; Chandu, D. The ubiquitinproteasome system. J Biosci. 2006, 31, 137-155.
113. Shaw, G.; Kamen, R. 1986. A conserved AU sequence from the 3' untranslated region of GM-CSF mRNA mediates selective mRNA degradation. Cell. 46, 659.
114. Beulter, B.; Krochin, N.; Mitsark, I.W.; Luedke, C.; Cerami, A. Control of cachectin (tumor necrosis factor) synthesis: Mechanisms of endotoxin resistance. Science. 1986, 232:977.
115. Han, J.; Huez, G.; Beutler, B. Interactive effects of the tumor necrosis factor promoter and Y-untranslated region. J Immunol. 1990, 146, 1843.
116. Sung, S.S.; Waiters, J.A. Increased cyclic AMP levels enhance IL-1 alpha and IL-1 beta mRNA expression and protein production in human myelomonocytic cell lines and monocytes. J. Clin. Invest. 1991, 88, 1915.
117. Thorens, B.; Mermod, J.J.; Vassali, P. Phagocytosis and inflammatory stimuli induce GM-CSF mRNA in macrophages through posttranscriptional regulation. Cell. 1987, 48, 671.
118. Doherty, G.M.; Jensen, J.C.; Alexander, H.R.; Buresh, C.M.; Norton, J.A. Pentoxifylline suppression of tumor necrosis factor gene transcription. Surgery (St. Louis). 1990, 110, 192.
119. Han, J.; Thompson, P.; Beutler, B. Dexamethasone and Pentoxifylline inhibit endotoxin induced cachectin/tumor necrosis factor synthesis at separate points in the signaling pathway. J. Exp Med. 1990, 172, 391.
120. Victor, J. Thannickal and Barry L. Fanburg. Reactive oxygen species in cell signaling. Am J Physiol Lung Cell Mol Physiol. 2000, 279:1005-1028.
121. Forman, H.J.; Fukuto, J.M.; Torres, M. Redox signaling: thiol chemistry defines which reactive oxygen and nitrogen species can act as second messengers. Am J Physiol Cell Physiol. 2004, 287: 246-256.
122. Addabbo, F.; Montagnani, M.; Goligorsky, M.S. Mitochondria and reactive oxygen species. Hypertension. 2009, 53, 885-892.
123. Halliwell, B.; Gutteridge, J.M.C. Free Radicals in Biology and Medicine Third Edition. Page-246.1999.
124. Yakes, F.M.; VanHouten, B. Mitochondrial DNA damage is more extensive and persists longer than nuclear DNA damage in human cells following oxidative stress. PNAS. 1997, 94, 514-519.
125. Berlett, B.S.; Stadtman, ER. Protein Oxidation in Aging, Disease, and Oxidative Stress. 1997 272, 20313-20316.
126. Butterfielda, D.A.; Lauderback, C.M. Lipid peroxidation and protein oxidation in Alzheimer's disease brain: potential causes and consequences involving amyloid α-peptide-associated free radical oxidative stress. Free Radical Biology and Medicine. 2002, 32, 1050-1060.
127. Liu, C.Y.; Lee, C.F.; Wei, Y.H. Role of Reactive Oxygen Specieselicited Apoptosis in the Pathophysiology of Mitochondrial and Neurodegenerative Diseases Associated With Mitochondrial DNA Mutations. J Formos Med Assoc. 2009, 108, 599-611.
128. Cerutti, P.A.; Trump, B.F. Inflammation and oxidative stress in carcinogenesis. Cancer Cells. 1991, 3, 1-7.
129. Sauer, H.; Günther, J.; Hescheler, J.; Wartenberg, M. Thalidomide Inhibits Angiogenesis in Embryoid Bodies by the Generation of Hydroxyl Radicals. American Journal of Pathology. 2000, 156, 151-158.
130. Aerbajinai, W.; Zhu, J.; Gao, Z.; Chin, K.; Rodgers, G.P. Thalidomide induces {gamma}-globin gene expression through increased reactive oxygen species-mediated p38 MAPK signaling and histone H4 acetylation in adult erythropoiesis. Blood. 2007, 110, 2864-2871.
131. Parman, T.; Wiley, M.J.; Wells, P.G. Free radical-mediated oxidative DNA damage in the mechanism of thalidomide teratogenicity. Nat Med. 1999, 5, 582-585.
132. Hansen, J.M.; Harris, C. A novel hypothesis for thalidomideinduced limb teratogenesis: redox misregulation of the NF-kappaB pathway. Antioxid Redox Signal. 2004, 6, 1-14.
133. Hansen, J.M.; Harris, K.K.; Philbert, M.A.; Harris, C. Thalidomide Modulates Nuclear Redox Status and preferentially Depletes Glutathione in rabbit limb versus rat limb. JPET. 2002, 300, 768-776.
134. Xu, D.X.; Chen, Y.; Wang, H.; Zhao, L.; Wang, J.; Wei, W. Effect of N-Acetylcysteine on Lipopolysaccharide-Induced Intra-uterine Fetal Death and Intra-uterine Growth Retardation in Mice. Toxicological Sciences. 2005, 88, 525-533.
135. Zahler, S.; Kupatt, C.; Becker, B.F. Endothelial preconditioning by transient oxidative stress reduces inflammatory responses of cultured endothelial cells to TNF-α. FASEB J. 2000, 14, 555-564.
136. Hayashi, T.; Ueno, Y.; Okamoto, T. Oxidoreductive Regulation of Nuclear Factor αB, Involvement of a cellular reducing catalyst thioredoxin. J Bio Chem. 1993, 268, 11380-11388.
137. Ho, E.; Bary, T.M. Antioxidanta, NFαB activation and diabetogenesis. PSEBM. 1999, 222.
138. Jason, H.M.; Siew-ging, S.; Martin, P.; Craig, H. Misregulation of gene expression in the redox-sensitive NF-αB-dependent limb outgrowth pathway by thalidomide. Developmental Dynamics 2002, 225, 86-194.
139. Shen, H.M.; Pervaiz, S. TNF receptor superfamily-induced cell death: redoxdependent execution. FASEB J. 2006, 20, 1589-1598.
140. Turk, B.E.; Jiang, H.; Liu, J.O. Binding of thalidomide to alpha1-acid glycoprotein may be involved in its inhibition of tumor necrosis factor alpha production. Proc. Natl. Acad. Sci. USA. 1996 93, 7552-7556
141. Pukhal'skii, A.L.; Shmarina, G.V.; Lyutov, A.G.; Novikova, L.I.; Shemyakin, I.G.; Aleshkin, V.A. Alpha1-acid glycoprotein possesses in vitro pro-and antiinflammatory activities. Bull Exp Biol Med. 2001, 131, 479-481.
142. Voisin, L.; Breuillé, D.; Ruot, B.; Rallière, C.; Rambourdin, F.; Dalle, M.; Obled, C. Cytokine modulation by PX differently affects specific acute phase proteins during sepsis in rats. Am J Physiol. 1998, 275, 1412-1419
143. Kitani, H.; Yagi, Y.; Naessens, J.; Sekikawa, K.; Iraqi, F. The secretion of acute phase proteins and inflammatory cytokines during Trypanosoma congolense infection is not affected by the absence of the TNF-alpha gene. Acta Trop. 2004, 92, 35-42.
144. Kuebler, J.F.; Toth, B.; Yokoyama, Y.; Bland, K.I.; Rue, L.W. 3rd; Chaudry, I.H. Alpha1-acid-glycoprotein protects against traumahemorrhagic shock. J Surg Res. 2004, 119, 21-28.
145. Matsumoto, K.; Nishi, K.; Kikuchi, M.; Kadowaki, D.; Tokutomi, Y.; Tokutomi, N.; Nishi, K.; Suenaga, A.; Otagiri, M. Alpha1-acid glycoprotein suppresses rat acute inflammatory paw edema through the inhibition of neutrophils activation and prostaglandin E2 generation. Biol Pharm Bull. 2007, 30, 1226-1230.
146. Oliveira, S.C.B.; Chiorcea-Paquima, A.M.; Ribeiro, S.M.; Melo, A.T.P.; Vivan, M.; Oliveira-Brett, A.M. In situ electrochemical and AFM study of thalidomide-DNA interaction. Bioelectrochemistry. 2009, 76, 201-207.
147. Drucker, L., Uziel, O., Tohami, T., Shapiro, H., Radnay, J., Yarkoni, S.; Lahav, M.; Lishner, M. Thalidomide Down-Regulates Transcript Levels of GC-Rich promoter Genes in Multiple Myeloma. Mol Pharmacol. 2003, 64, 415-420.
148. Krämer, B.; Meichle, A.; Hensel, G.; Charnay, P.; Krönke, M. Characterization of an Krox-24/Egr-1-responsive element in the human tumor necrosis factor promoter. Biochim Biophys Acta. 1994, 1219, 413-421.
149. Krämer, B.; Wiegmann, K.; Krönke, M. Regulation of the Human TNF Promoter by the Transcription Factor Ets. J Bio Chem. 1995, 270, 6577-6583.