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Volumn 9, Issue 6, 2015, Pages 1194-1206

Hitting the right spot: Mechanism of action of OPB-31121, a novel and potent inhibitor of the Signal Transducer and Activator of Transcription 3 (STAT3)

Author keywords

Anticancer drugs; Cancer therapy; Computational modeling; Mechanism of action; Molecular dynamic simulation; Site directed mutagenesis; Small molecule inhibitors; STAT3; Transcription factors

Indexed keywords

ANTINEOPLASTIC AGENT; OPB 31121; STAT3 PROTEIN; UNCLASSIFIED DRUG; STAT3 PROTEIN, HUMAN; TUMOR PROTEIN;

EID: 84929514550     PISSN: 15747891     EISSN: 18780261     Source Type: Journal    
DOI: 10.1016/j.molonc.2015.02.012     Document Type: Article
Times cited : (81)

References (54)
  • 1
    • 0032499801 scopus 로고    scopus 로고
    • Three-dimensional structure of the Stat3beta homodimer bound to DNA
    • Becker S., Groner B., Muller C.W. Three-dimensional structure of the Stat3beta homodimer bound to DNA. Nature 1998, 394:145-151.
    • (1998) Nature , vol.394 , pp. 145-151
    • Becker, S.1    Groner, B.2    Muller, C.W.3
  • 3
    • 70349323403 scopus 로고    scopus 로고
    • Targeting signal transducer and activator of transcription signaling pathway in leukemias
    • Benekli M., Baumann H., Wetzler M. Targeting signal transducer and activator of transcription signaling pathway in leukemias. J. Clin. Oncol. 2009, 27:4422-4432.
    • (2009) J. Clin. Oncol. , vol.27 , pp. 4422-4432
    • Benekli, M.1    Baumann, H.2    Wetzler, M.3
  • 4
    • 4944239032 scopus 로고    scopus 로고
    • Disruption of Stat3 reveals a critical role in both the initiation and the promotion stages of epithelial carcinogenesis
    • Chan K.S., Sano S., Kiguchi K., Anders J., Komazawa N., Takeda J., DiGiovanni J. Disruption of Stat3 reveals a critical role in both the initiation and the promotion stages of epithelial carcinogenesis. J. Clin. Invest. 2004, 114:720-728.
    • (2004) J. Clin. Invest. , vol.114 , pp. 720-728
    • Chan, K.S.1    Sano, S.2    Kiguchi, K.3    Anders, J.4    Komazawa, N.5    Takeda, J.6    DiGiovanni, J.7
  • 5
    • 23944441266 scopus 로고    scopus 로고
    • Interleukin-6 regulation of prostate cancer cell growth
    • Culig Z., Steiner H., Bartsch G., Hobisch A. Interleukin-6 regulation of prostate cancer cell growth. J. Cell Biochem. 2005, 95:497-505.
    • (2005) J. Cell Biochem. , vol.95 , pp. 497-505
    • Culig, Z.1    Steiner, H.2    Bartsch, G.3    Hobisch, A.4
  • 6
    • 84864917825 scopus 로고    scopus 로고
    • Small molecule inhibitors of signal transducer and activator of transcription 3 (Stat3) protein
    • Debnath B., Xu S., Neamati N. Small molecule inhibitors of signal transducer and activator of transcription 3 (Stat3) protein. J. Med. Chem. 2012, 55:6645-6668.
    • (2012) J. Med. Chem. , vol.55 , pp. 6645-6668
    • Debnath, B.1    Xu, S.2    Neamati, N.3
  • 8
    • 54349127051 scopus 로고    scopus 로고
    • Molecular approaches towards the inhibition of the signal transducer and activator of transcription 3 (Stat3) protein
    • Fletcher S., Turkson J., Gunning P.T. Molecular approaches towards the inhibition of the signal transducer and activator of transcription 3 (Stat3) protein. ChemMedChem 2008, 3:1159-1168.
    • (2008) ChemMedChem , vol.3 , pp. 1159-1168
    • Fletcher, S.1    Turkson, J.2    Gunning, P.T.3
  • 9
    • 84866641956 scopus 로고    scopus 로고
    • Transcriptional and non-transcriptional functions of PPARbeta/delta in non-small cell lung cancer
    • Genini D., Garcia-Escudero R., Carbone G.M., Catapano C.V. Transcriptional and non-transcriptional functions of PPARbeta/delta in non-small cell lung cancer. PLoS One 2012, 7:e46009.
    • (2012) PLoS One , vol.7 , pp. e46009
    • Genini, D.1    Garcia-Escudero, R.2    Carbone, G.M.3    Catapano, C.V.4
  • 10
    • 77955473941 scopus 로고    scopus 로고
    • Synergistic experimental/computational studies on arylazoenamine derivatives that target the bovine viral diarrhea virus RNA-dependent RNA polymerase
    • Giliberti G., Ibba C., Marongiu E., Loddo R., Tonelli M., Boido V., Laurini E., Posocco P., Fermeglia M., Pricl S. Synergistic experimental/computational studies on arylazoenamine derivatives that target the bovine viral diarrhea virus RNA-dependent RNA polymerase. Bioorg. Med. Chem. 2010, 18:6055-6068.
    • (2010) Bioorg. Med. Chem. , vol.18 , pp. 6055-6068
    • Giliberti, G.1    Ibba, C.2    Marongiu, E.3    Loddo, R.4    Tonelli, M.5    Boido, V.6    Laurini, E.7    Posocco, P.8    Fermeglia, M.9    Pricl, S.10
  • 12
    • 37349098725 scopus 로고    scopus 로고
    • Autocrine IL-6 signaling: a key event in tumorigenesis?
    • Grivennikov S., Karin M. Autocrine IL-6 signaling: a key event in tumorigenesis?. Cancer Cell 2008, 13:7-9.
    • (2008) Cancer Cell , vol.13 , pp. 7-9
    • Grivennikov, S.1    Karin, M.2
  • 13
    • 84861229091 scopus 로고    scopus 로고
    • The molecular basis of IGF-II/IGF2R recognition: a combined molecular dynamics simulation, free-energy calculation and computational alanine scanning study
    • Guo J., Wang X., Sun H., Liu H., Yao X. The molecular basis of IGF-II/IGF2R recognition: a combined molecular dynamics simulation, free-energy calculation and computational alanine scanning study. J. Mol. Model. 2012, 18:1421-1430.
    • (2012) J. Mol. Model. , vol.18 , pp. 1421-1430
    • Guo, J.1    Wang, X.2    Sun, H.3    Liu, H.4    Yao, X.5
  • 14
    • 84888424589 scopus 로고    scopus 로고
    • A novel STAT inhibitor, OPB-31121, has a significant antitumor effect on leukemia with STAT-addictive oncokinases
    • Hayakawa F., Sugimoto K., Harada Y., Hashimoto N., Ohi N., Kurahashi S., Naoe T. A novel STAT inhibitor, OPB-31121, has a significant antitumor effect on leukemia with STAT-addictive oncokinases. Blood Cancer J. 2013, 3:e166.
    • (2013) Blood Cancer J. , vol.3 , pp. e166
    • Hayakawa, F.1    Sugimoto, K.2    Harada, Y.3    Hashimoto, N.4    Ohi, N.5    Kurahashi, S.6    Naoe, T.7
  • 17
    • 84878432714 scopus 로고    scopus 로고
    • OPB-31121, a novel small molecular inhibitor, disrupts the JAK2/STAT3 pathway and exhibits an antitumor activity in gastric cancer cells
    • Kim M.J., Nam H.J., Kim H.P., Han S.W., Im S.A., Kim T.Y., Oh D.Y., Bang Y.J. OPB-31121, a novel small molecular inhibitor, disrupts the JAK2/STAT3 pathway and exhibits an antitumor activity in gastric cancer cells. Cancer Lett. 2013, 335:145-152.
    • (2013) Cancer Lett. , vol.335 , pp. 145-152
    • Kim, M.J.1    Nam, H.J.2    Kim, H.P.3    Han, S.W.4    Im, S.A.5    Kim, T.Y.6    Oh, D.Y.7    Bang, Y.J.8
  • 21
    • 84868585563 scopus 로고    scopus 로고
    • Another brick in the wall. Validation of the sigma1 receptor 3D model by computer-assisted design, synthesis, and activity of new sigma1 ligands
    • Laurini E., Marson D., Dal Col V., Fermeglia M., Mamolo M.G., Zampieri D., Vio L., Pricl S. Another brick in the wall. Validation of the sigma1 receptor 3D model by computer-assisted design, synthesis, and activity of new sigma1 ligands. Mol. Pharm. 2012, 9:3107-3126.
    • (2012) Mol. Pharm. , vol.9 , pp. 3107-3126
    • Laurini, E.1    Marson, D.2    Dal Col, V.3    Fermeglia, M.4    Mamolo, M.G.5    Zampieri, D.6    Vio, L.7    Pricl, S.8
  • 23
    • 84905726946 scopus 로고    scopus 로고
    • Drug resistance via feedback activation of Stat3 in oncogene-addicted cancer cells
    • Lee H.J., Zhuang G., Cao Y., Du P., Kim H.J., Settleman J. Drug resistance via feedback activation of Stat3 in oncogene-addicted cancer cells. Cancer Cell 2014, 26:207-221.
    • (2014) Cancer Cell , vol.26 , pp. 207-221
    • Lee, H.J.1    Zhuang, G.2    Cao, Y.3    Du, P.4    Kim, H.J.5    Settleman, J.6
  • 24
    • 0036731485 scopus 로고    scopus 로고
    • Stats: transcriptional control and biological impact
    • Levy D.E., Darnell J.E. Stats: transcriptional control and biological impact. Nat. Rev. Mol. Cell Biol. 2002, 3:651-662.
    • (2002) Nat. Rev. Mol. Cell Biol. , vol.3 , pp. 651-662
    • Levy, D.E.1    Darnell, J.E.2
  • 25
    • 33750040230 scopus 로고    scopus 로고
    • Structure, function, and regulation of STAT proteins
    • Lim C.P., Cao X. Structure, function, and regulation of STAT proteins. Mol. Biosyst. 2006, 2:536-550.
    • (2006) Mol. Biosyst. , vol.2 , pp. 536-550
    • Lim, C.P.1    Cao, X.2
  • 26
    • 20444400857 scopus 로고    scopus 로고
    • STAT3 nuclear import is independent of tyrosine phosphorylation and mediated by importin-alpha3
    • Liu L., McBride K.M., Reich N.C. STAT3 nuclear import is independent of tyrosine phosphorylation and mediated by importin-alpha3. Proc. Natl. Acad. Sci. U. S. A. 2005, 102:8150-8155.
    • (2005) Proc. Natl. Acad. Sci. U. S. A. , vol.102 , pp. 8150-8155
    • Liu, L.1    McBride, K.M.2    Reich, N.C.3
  • 28
    • 84896490633 scopus 로고    scopus 로고
    • Toward a new STATe: the role of STATs in mitochondrial function
    • Meier J.A., Larner A.C. Toward a new STATe: the role of STATs in mitochondrial function. Semin. Immunol. 2014, 26:20-28.
    • (2014) Semin. Immunol. , vol.26 , pp. 20-28
    • Meier, J.A.1    Larner, A.C.2
  • 29
    • 84881267595 scopus 로고    scopus 로고
    • Therapeutic modulators of STAT signalling for human diseases
    • Miklossy G., Hilliard T.S., Turkson J. Therapeutic modulators of STAT signalling for human diseases. Nat. Rev. Drug Discov. 2013, 12:611-629.
    • (2013) Nat. Rev. Drug Discov. , vol.12 , pp. 611-629
    • Miklossy, G.1    Hilliard, T.S.2    Turkson, J.3
  • 32
    • 67649537602 scopus 로고    scopus 로고
    • Promoter-specific transcriptional interference and c-myc gene silencing by siRNAs in human cells
    • Napoli S., Pastori C., Magistri M., Carbone G.M., Catapano C.V. Promoter-specific transcriptional interference and c-myc gene silencing by siRNAs in human cells. EMBO J. 2009, 28:1708-1719.
    • (2009) EMBO J. , vol.28 , pp. 1708-1719
    • Napoli, S.1    Pastori, C.2    Magistri, M.3    Carbone, G.M.4    Catapano, C.V.5
  • 33
    • 84859972127 scopus 로고    scopus 로고
    • JAK and STAT signaling molecules in immunoregulation and immune-mediated disease
    • O'Shea J.J., Plenge R. JAK and STAT signaling molecules in immunoregulation and immune-mediated disease. Immunity 2012, 36:542-550.
    • (2012) Immunity , vol.36 , pp. 542-550
    • O'Shea, J.J.1    Plenge, R.2
  • 34
    • 54249083133 scopus 로고    scopus 로고
    • Activation of signal transducer and activator of transcription 3 through a phosphomimetic serine 727 promotes prostate tumorigenesis independent of tyrosine 705 phosphorylation
    • Qin H.R., Kim H.J., Kim J.Y., Hurt E.M., Klarmann G.J., Kawasaki B.T., Duhagon Serrat M.A., Farrar W.L. Activation of signal transducer and activator of transcription 3 through a phosphomimetic serine 727 promotes prostate tumorigenesis independent of tyrosine 705 phosphorylation. Cancer Res. 2008, 68:7736-7741.
    • (2008) Cancer Res. , vol.68 , pp. 7736-7741
    • Qin, H.R.1    Kim, H.J.2    Kim, J.Y.3    Hurt, E.M.4    Klarmann, G.J.5    Kawasaki, B.T.6    Duhagon Serrat, M.A.7    Farrar, W.L.8
  • 35
    • 84860630975 scopus 로고    scopus 로고
    • Targeting the interleukin-6/Jak/stat pathway in human malignancies
    • Sansone P., Bromberg J. Targeting the interleukin-6/Jak/stat pathway in human malignancies. J. Clin. Oncol. 2012, 30:1005-1014.
    • (2012) J. Clin. Oncol. , vol.30 , pp. 1005-1014
    • Sansone, P.1    Bromberg, J.2
  • 37
    • 33750982120 scopus 로고    scopus 로고
    • Stattic: a small-molecule inhibitor of STAT3 activation and dimerization
    • Schust J., Sperl B., Hollis A., Mayer T.U., Berg T. Stattic: a small-molecule inhibitor of STAT3 activation and dimerization. Chem. Biol. 2006, 13:1235-1242.
    • (2006) Chem. Biol. , vol.13 , pp. 1235-1242
    • Schust, J.1    Sperl, B.2    Hollis, A.3    Mayer, T.U.4    Berg, T.5
  • 38
    • 52949104437 scopus 로고    scopus 로고
    • Paradigm shifts in the cell biology of STAT signaling
    • Sehgal P.B. Paradigm shifts in the cell biology of STAT signaling. Semin. Cell Dev. Biol. 2008, 19:329-340.
    • (2008) Semin. Cell Dev. Biol. , vol.19 , pp. 329-340
    • Sehgal, P.B.1
  • 39
    • 58249119435 scopus 로고    scopus 로고
    • Cryptotanshinone inhibits constitutive signal transducer and activator of transcription 3 function through blocking the dimerization in DU145 prostate cancer cells
    • Shin D.S., Kim H.N., Shin K.D., Yoon Y.J., Kim S.J., Han D.C., Kwon B.M. Cryptotanshinone inhibits constitutive signal transducer and activator of transcription 3 function through blocking the dimerization in DU145 prostate cancer cells. Cancer Res. 2009, 69:193-202.
    • (2009) Cancer Res. , vol.69 , pp. 193-202
    • Shin, D.S.1    Kim, H.N.2    Shin, K.D.3    Yoon, Y.J.4    Kim, S.J.5    Han, D.C.6    Kwon, B.M.7
  • 41
    • 16344380754 scopus 로고    scopus 로고
    • A low-molecular-weight compound discovered through virtual database screening inhibits Stat3 function in breast cancer cells
    • 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, 102:4700-4705.
    • (2005) Proc. Natl. Acad. Sci. U. S. A. , vol.102 , pp. 4700-4705
    • Song, H.1    Wang, R.2    Wang, S.3    Lin, J.4
  • 43
    • 79961026922 scopus 로고    scopus 로고
    • Direct reprogramming of stem cell properties in colon cancer cells by CD44
    • Su Y.J., Lai H.M., Chang Y.W., Chen G.Y., Lee J.L. Direct reprogramming of stem cell properties in colon cancer cells by CD44. EMBO J. 2011, 30:3186-3199.
    • (2011) EMBO J. , vol.30 , pp. 3186-3199
    • Su, Y.J.1    Lai, H.M.2    Chang, Y.W.3    Chen, G.Y.4    Lee, J.L.5
  • 47
    • 0029117304 scopus 로고
    • Maximal activation of transcription by Stat1 and Stat3 requires both tyrosine and serine phosphorylation
    • Wen Z., Zhong Z., Darnell J.E. Maximal activation of transcription by Stat1 and Stat3 requires both tyrosine and serine phosphorylation. Cell 1995, 82:241-250.
    • (1995) Cell , vol.82 , pp. 241-250
    • Wen, Z.1    Zhong, Z.2    Darnell, J.E.3
  • 48
    • 35048878660 scopus 로고    scopus 로고
    • Live cell imaging of interleukin-6-induced targeting of "transcription factor" STAT3 to sequestering endosomes in the cytoplasm
    • Xu F., Mukhopadhyay S., Sehgal P.B. Live cell imaging of interleukin-6-induced targeting of "transcription factor" STAT3 to sequestering endosomes in the cytoplasm. Am. J. Physiol. Cell Physiol. 2007, 293:C1374-C1382.
    • (2007) Am. J. Physiol. Cell Physiol. , vol.293 , pp. C1374-C1382
    • Xu, F.1    Mukhopadhyay, S.2    Sehgal, P.B.3
  • 49
    • 34249868449 scopus 로고    scopus 로고
    • Unphosphorylated STAT3 accumulates in response to IL-6 and activates transcription by binding to NFkappaB
    • Yang J., Liao X., Agarwal M.K., Barnes L., Auron P.E., Stark G.R. Unphosphorylated STAT3 accumulates in response to IL-6 and activates transcription by binding to NFkappaB. Genes Dev. 2007, 21:1396-1408.
    • (2007) Genes Dev. , vol.21 , pp. 1396-1408
    • Yang, J.1    Liao, X.2    Agarwal, M.K.3    Barnes, L.4    Auron, P.E.5    Stark, G.R.6
  • 50
    • 84908161000 scopus 로고    scopus 로고
    • Revisiting STAT3 signalling in cancer: new and unexpected biological functions
    • Yu H., Lee H., Herrmann A., Buettner R., Jove R. Revisiting STAT3 signalling in cancer: new and unexpected biological functions. Nat. Rev. Cancer 2014, 14:736-746.
    • (2014) Nat. Rev. Cancer , vol.14 , pp. 736-746
    • Yu, H.1    Lee, H.2    Herrmann, A.3    Buettner, R.4    Jove, R.5
  • 51
    • 70350500225 scopus 로고    scopus 로고
    • STATs in cancer inflammation and immunity: a leading role for STAT3
    • Yu H., Pardoll D., Jove R. STATs in cancer inflammation and immunity: a leading role for STAT3. Nat. Rev. Cancer 2009, 9:798-809.
    • (2009) Nat. Rev. Cancer , vol.9 , pp. 798-809
    • Yu, H.1    Pardoll, D.2    Jove, R.3
  • 52
    • 12244251445 scopus 로고    scopus 로고
    • Stat3 dimerization regulated by reversible acetylation of a single lysine residue
    • Yuan Z.L., Guan Y.J., Chatterjee D., Chin Y.E. Stat3 dimerization regulated by reversible acetylation of a single lysine residue. Science 2005, 307:269-273.
    • (2005) Science , vol.307 , pp. 269-273
    • Yuan, Z.L.1    Guan, Y.J.2    Chatterjee, D.3    Chin, Y.E.4
  • 53
    • 0028942656 scopus 로고
    • Requirement of serine phosphorylation for formation of STAT-promoter complexes
    • Zhang X., Blenis J., Li H.C., Schindler C., Chen-Kiang S. Requirement of serine phosphorylation for formation of STAT-promoter complexes. Science 1995, 267:1990-1994.
    • (1995) Science , vol.267 , pp. 1990-1994
    • Zhang, X.1    Blenis, J.2    Li, H.C.3    Schindler, C.4    Chen-Kiang, S.5
  • 54
    • 0028349735 scopus 로고
    • Stat3: a STAT family member activated by tyrosine phosphorylation in response to epidermal growth factor and interleukin-6
    • Zhong Z., Wen Z., Darnell J.E. Stat3: a STAT family member activated by tyrosine phosphorylation in response to epidermal growth factor and interleukin-6. Science 1994, 264:95-98.
    • (1994) Science , vol.264 , pp. 95-98
    • Zhong, Z.1    Wen, Z.2    Darnell, J.E.3


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