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Research Paper

MLS-2384, a new 6-bromoindirubin derivative with dual JAK/Src kinase inhibitory activity, suppresses growth of diverse cancer cells

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Pages 178-184 | Received 15 Jul 2013, Accepted 06 Oct 2013, Published online: 01 Nov 2013

References

  • Frame MC. Newest findings on the oldest oncogene; how activated src does it. J Cell Sci 2004; 117:989 - 98; http://dx.doi.org/10.1242/jcs.01111; PMID: 14996930
  • Niu G, Bowman T, Huang M, Shivers S, Reintgen D, Daud A, Chang A, Kraker A, Jove R, Yu H. Roles of activated Src and Stat3 signaling in melanoma tumor cell growth. Oncogene 2002; 21:7001 - 10; http://dx.doi.org/10.1038/sj.onc.1205859; PMID: 12370822
  • Sinibaldi D, Wharton W, Turkson J, Bowman T, Pledger WJ, Jove R. Induction of p21WAF1/CIP1 and cyclin D1 expression by the Src oncoprotein in mouse fibroblasts: role of activated STAT3 signaling. Oncogene 2000; 19:5419 - 27; http://dx.doi.org/10.1038/sj.onc.1203947; PMID: 11114718
  • Darnell JE Jr., Kerr IM, Stark GR. Jak-STAT pathways and transcriptional activation in response to IFNs and other extracellular signaling proteins. Science 1994; 264:1415 - 21; http://dx.doi.org/10.1126/science.8197455; PMID: 8197455
  • Wojcik EJ, Sharifpoor S, Miller NA, Wright TG, Watering R, Tremblay EA, Swan K, Mueller CR, Elliott BE. A novel activating function of c-Src and Stat3 on HGF transcription in mammary carcinoma cells. Oncogene 2006; 25:2773 - 84; http://dx.doi.org/10.1038/sj.onc.1209306; PMID: 16407846
  • Sam MR, Elliott BE, Mueller CR. A novel activating role of SRC and STAT3 on HGF transcription in human breast cancer cells. Mol Cancer 2007; 6:69; http://dx.doi.org/10.1186/1476-4598-6-69; PMID: 17967179
  • Hbibi AT, Lagorce C, Wind P, Spano JP, Des Guetz G, Milano G, Benamouzig R, Rixe O, Morere JF, Breau JL, et al. Identification of a functional EGF-R/p60c-src/STAT3 pathway in colorectal carcinoma: analysis of its long-term prognostic value. Cancer Biomark 2008; 4:83 - 91; PMID: 18503159
  • Yu H, Jove R. The STATs of cancer--new molecular targets come of age. Nat Rev Cancer 2004; 4:97 - 105; http://dx.doi.org/10.1038/nrc1275; PMID: 14964307
  • Gao SP, Bromberg JF. Touched and moved by STAT3. Sci STKE 2006; 2006:pe30; PMID: 16835434
  • Yu H, Pardoll D, Jove R. STATs in cancer inflammation and immunity: a leading role for STAT3. Nat Rev Cancer 2009; 9:798 - 809; http://dx.doi.org/10.1038/nrc2734; PMID: 19851315
  • Kortylewski M, Jove R, Yu H. Targeting STAT3 affects melanoma on multiple fronts. Cancer Metastasis Rev 2005; 24:315 - 27; http://dx.doi.org/10.1007/s10555-005-1580-1; PMID: 15986140
  • Zhang S, Yu D. Targeting Src family kinases in anti-cancer therapies: turning promise into triumph. Trends Pharmacol Sci 2012; 33:122 - 8; http://dx.doi.org/10.1016/j.tips.2011.11.002; PMID: 22153719
  • Creedon H, Brunton VG. Src kinase inhibitors: promising cancer therapeutics?. Crit Rev Oncog 2012; 17:145 - 59; http://dx.doi.org/10.1615/CritRevOncog.v17.i2.20; PMID: 22471705
  • Chatzizacharias NA, Kouraklis GP, Giaginis CT, Theocharis SE. Clinical significance of Src expression and activity in human neoplasia. Histol Histopathol 2012; 27:677 - 92; PMID: 22473690
  • Levine RL, Pardanani A, Tefferi A, Gilliland DG. Role of JAK2 in the pathogenesis and therapy of myeloproliferative disorders. Nat Rev Cancer 2007; 7:673 - 83; http://dx.doi.org/10.1038/nrc2210; PMID: 17721432
  • Pesu M, Laurence A, Kishore N, Zwillich SH, Chan G, O’Shea JJ. Therapeutic targeting of Janus kinases. Immunol Rev 2008; 223:132 - 42; http://dx.doi.org/10.1111/j.1600-065X.2008.00644.x; PMID: 18613833
  • Wernig G, Kharas MG, Okabe R, Moore SA, Leeman DS, Cullen DE, Gozo M, McDowell EP, Levine RL, Doukas J, et al. Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia vera. Cancer Cell 2008; 13:311 - 20; http://dx.doi.org/10.1016/j.ccr.2008.02.009; PMID: 18394554
  • Sayyah J, Sayeski PP. Jak2 inhibitors: rationale and role as therapeutic agents in hematologic malignancies. Curr Oncol Rep 2009; 11:117 - 24; http://dx.doi.org/10.1007/s11912-009-0018-2; PMID: 19216843
  • Verstovsek S. Therapeutic potential of JAK2 inhibitors. Hematology / the Education Program of the American Society of Hematology American Society of Hematology 2009:636-42.
  • Lee HJ, Daver N, Kantarjian HM, Verstovsek S, Ravandi F. The role of JAK pathway dysregulation in the pathogenesis and treatment of acute myeloid leukemia. Clin Cancer Res 2013; 19:327 - 35; http://dx.doi.org/10.1158/1078-0432.CCR-12-2087; PMID: 23209034
  • Komrokji R, Verstovsek S. Assessing efficacy in myelofibrosis treatment: a focus on JAK inhibition. Expert Rev Hematol 2012; 5:631 - 41; http://dx.doi.org/10.1586/ehm.12.50; PMID: 23216593
  • Constantinescu SN, Vainchenker W. Small-molecule inhibitors in myeloproliferative neoplasms: are we aiming for the right targets?. Hematology Am Soc Hematol Educ Program 2012; 2012:553 - 60; PMID: 23233634
  • Kontzias A, Kotlyar A, Laurence A, Changelian P, O’Shea JJ. Jakinibs: a new class of kinase inhibitors in cancer and autoimmune disease. Curr Opin Pharmacol 2012; 12:464 - 70; http://dx.doi.org/10.1016/j.coph.2012.06.008; PMID: 22819198
  • Lai SY, Johnson FM. Defining the role of the JAK-STAT pathway in head and neck and thoracic malignancies: implications for future therapeutic approaches. Drug Resist Updat 2010; 13:67 - 78; http://dx.doi.org/10.1016/j.drup.2010.04.001; PMID: 20471303
  • Blaskovich MA, Sun J, Cantor A, Turkson J, Jove R, Sebti SM. Discovery of JSI-124 (cucurbitacin I), a selective Janus kinase/signal transducer and activator of transcription 3 signaling pathway inhibitor with potent antitumor activity against human and murine cancer cells in mice. Cancer Res 2003; 63:1270 - 9; PMID: 12649187
  • Song H, Wang R, Wang S, Lin J. A low-molecular-weight compound discovered through virtual database screening inhibits Stat3 function in breast cancer cells. Proc Natl Acad Sci U S A 2005; 102:4700 - 5; http://dx.doi.org/10.1073/pnas.0409894102; PMID: 15781862
  • Sun J, Blaskovich MA, Jove R, Livingston SK, Coppola D, Sebti SM. Cucurbitacin Q: a selective STAT3 activation inhibitor with potent antitumor activity. Oncogene 2005; 24:3236 - 45; http://dx.doi.org/10.1038/sj.onc.1208470; PMID: 15735720
  • Liby K, Voong N, Williams CR, Risingsong R, Royce DB, Honda T, Gribble GW, Sporn MB, Letterio JJ. The synthetic triterpenoid CDDO-Imidazolide suppresses STAT phosphorylation and induces apoptosis in myeloma and lung cancer cells. Clin Cancer Res 2006; 12:4288 - 93; http://dx.doi.org/10.1158/1078-0432.CCR-06-0215; PMID: 16857804
  • Ahmad R, Raina D, Meyer C, Kufe D. Triterpenoid CDDO-methyl ester inhibits the Janus-activated kinase-1 (JAK1)-->signal transducer and activator of transcription-3 (STAT3) pathway by direct inhibition of JAK1 and STAT3. Cancer Res 2008; 68:2920 - 6; http://dx.doi.org/10.1158/0008-5472.CAN-07-3036; PMID: 18413761
  • Wang Y, Ma X, Yan S, Shen S, Zhu H, Gu Y, Wang H, Qin G, Yu Q. 17-hydroxy-jolkinolide B inhibits signal transducers and activators of transcription 3 signaling by covalently cross-linking Janus kinases and induces apoptosis of human cancer cells. Cancer Res 2009; 69:7302 - 10; http://dx.doi.org/10.1158/0008-5472.CAN-09-0462; PMID: 19706767
  • Hedvat M, Huszar D, Herrmann A, Gozgit JM, Schroeder A, Sheehy A, Buettner R, Proia D, Kowolik CM, Xin H, et al. The JAK2 inhibitor AZD1480 potently blocks Stat3 signaling and oncogenesis in solid tumors. Cancer Cell 2009; 16:487 - 97; http://dx.doi.org/10.1016/j.ccr.2009.10.015; PMID: 19962667
  • Liu L, Nam S, Tian Y, Yang F, Wu J, Wang Y, Scuto A, Polychronopoulos P, Magiatis P, Skaltsounis L, et al. 6-Bromoindirubin-3′-oxime inhibits JAK/STAT3 signaling and induces apoptosis of human melanoma cells. Cancer Res 2011; 71:3972 - 9; http://dx.doi.org/10.1158/0008-5472.CAN-10-3852; PMID: 21610112
  • Tian Y, Nam S, Liu L, Yakushijin F, Yakushijin K, Buettner R, Liang W, Yang F, Ma Y, Horne D, et al. Spirooxindole derivative SOID-8 induces apoptosis associated with inhibition of JAK2/STAT3 signaling in melanoma cells. PLoS One 2012; 7:e49306; http://dx.doi.org/10.1371/journal.pone.0049306; PMID: 23166634
  • Hoessel R, Leclerc S, Endicott JA, Nobel ME, Lawrie A, Tunnah P, Leost M, Damiens E, Marie D, Marko D, et al. Indirubin, the active constituent of a Chinese antileukaemia medicine, inhibits cyclin-dependent kinases. Nat Cell Biol 1999; 1:60 - 7; PMID: 10559866
  • Xiao Z, Hao Y, Liu B, Qian L. Indirubin and meisoindigo in the treatment of chronic myelogenous leukemia in China. Leuk Lymphoma 2002; 43:1763 - 8; http://dx.doi.org/10.1080/1042819021000006295; PMID: 12685829
  • Leclerc S, Garnier M, Hoessel R, Marko D, Bibb JA, Snyder GL, Greengard P, Biernat J, Wu YZ, Mandelkow EM, et al. Indirubins inhibit glycogen synthase kinase-3 beta and CDK5/p25, two protein kinases involved in abnormal tau phosphorylation in Alzheimer’s disease. A property common to most cyclin-dependent kinase inhibitors?. J Biol Chem 2001; 276:251 - 60; http://dx.doi.org/10.1074/jbc.M002466200; PMID: 11013232
  • Jakobs S, Merz KH, Vatter S, Eisenbrand G. Molecular targets of indirubins. Int J Clin Pharmacol Ther 2005; 43:592 - 4; http://dx.doi.org/10.5414/CPP43592; PMID: 16372530
  • Vougogiannopoulou K, Ferandin Y, Bettayeb K, Myrianthopoulos V, Lozach O, Fan Y, Johnson CH, Magiatis P, Skaltsounis AL, Mikros E, et al. Soluble 3′,6-substituted indirubins with enhanced selectivity toward glycogen synthase kinase -3 alter circadian period. J Med Chem 2008; 51:6421 - 31; http://dx.doi.org/10.1021/jm800648y; PMID: 18816110
  • Liu L, Kritsanida M, Magiatis P, Gaboriaud N, Wang Y, Wu J, Buettner R, Yang F, Nam S, Skaltsounis L, et al. A novel 7-bromoindirubin with potent anticancer activity suppresses survival of human melanoma cells associated with inhibition of STAT3 and Akt signaling. Cancer Biol Ther 2012; 13:1255 - 61; http://dx.doi.org/10.4161/cbt.21781; PMID: 22895078
  • Ferandin Y, Bettayeb K, Kritsanida M, Lozach O, Polychronopoulos P, Magiatis P, Skaltsounis AL, Meijer L. 3′-Substituted 7-halogenoindirubins, a new class of cell death inducing agents. J Med Chem 2006; 49:4638 - 49; http://dx.doi.org/10.1021/jm060314i; PMID: 16854069
  • Ribas J, Bettayeb K, Ferandin Y, Knockaert M, Garrofé-Ochoa X, Totzke F, Schächtele C, Mester J, Polychronopoulos P, Magiatis P, et al. 7-Bromoindirubin-3′-oxime induces caspase-independent cell death. Oncogene 2006; 25:6304 - 18; http://dx.doi.org/10.1038/sj.onc.1209648; PMID: 16702956
  • Choi SJ, Lee JE, Jeong SY, Im I, Lee SD, Lee EJ, Lee SK, Kwon SM, Ahn SG, Yoon JH, et al. 5,5′-substituted indirubin-3′-oxime derivatives as potent cyclin-dependent kinase inhibitors with anticancer activity. J Med Chem 2010; 53:3696 - 706; http://dx.doi.org/10.1021/jm100080z; PMID: 20361800
  • Byers LA, Sen B, Saigal B, Diao L, Wang J, Nanjundan M, Cascone T, Mills GB, Heymach JV, Johnson FM. Reciprocal regulation of c-Src and STAT3 in non-small cell lung cancer. Clin Cancer Res 2009; 15:6852 - 61; http://dx.doi.org/10.1158/1078-0432.CCR-09-0767; PMID: 19861436
  • Sen B, Saigal B, Parikh N, Gallick G, Johnson FM. Sustained Src inhibition results in signal transducer and activator of transcription 3 (STAT3) activation and cancer cell survival via altered Janus-activated kinase-STAT3 binding. Cancer Res 2009; 69:1958 - 65; http://dx.doi.org/10.1158/0008-5472.CAN-08-2944; PMID: 19223541
  • Johnson FM, Saigal B, Tran H, Donato NJ. Abrogation of signal transducer and activator of transcription 3 reactivation after Src kinase inhibition results in synergistic antitumor effects. Clin Cancer Res 2007; 13:4233 - 44; http://dx.doi.org/10.1158/1078-0432.CCR-06-2981; PMID: 17634553

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