Comparative screening and validation as a novel tool to identify STAT-specific inhibitors

European Journal of Pharmacology

Volumn 740, Issue , 2014, Pages 417-420

  Szeląg, Małgorzata ^a   Czerwoniec, Anna ^a   Wesoly, Joanna ^a   Bluyssen, Hans A R ^a  

^a ADAM MICKIEWICZ UNIVERSITY   (Poland)

Author keywords

Comparative drug identification assay; Cross binding specificity; STAT inhibition strategies; STAT SH2 modeling

Indexed keywords

5 HYDROXY 9,10 DIOXO 9,10 DIHYDROANTHRACENE 1 SULFONAMIDE; CRYPTOTANSHINONE; CURCUMIN; CYTOKINE; FLLL 32; GROWTH FACTOR; HJC 0123; NATURAL PRODUCT; OBP 31121; OLIGODEOXYNUCLEOTIDE; PHOSPHOTYROSINE; PROTEIN INHIBITOR; PROTEIN SH2; RESVERATROL; STA 21; STAT PROTEIN; STAT PROTEIN INHIBITOR; SULFONAMIDE; UNCLASSIFIED DRUG; MOLECULAR LIBRARY;

AUTOIMMUNITY; CELL NUCLEUS; COMPUTER MODEL; DIMERIZATION; DNA RESPONSIVE ELEMENT; DRUG IDENTIFICATION; DRUG SCREENING; DRUG SPECIFICITY; DRUG TARGETING; GENETIC TRANSCRIPTION; HUMAN; IN VITRO STUDY; INFLAMMATION; MOLECULAR LIBRARY; MOLECULAR MODEL; NEOPLASM; NONHUMAN; PROTEIN DOMAIN; PROTEIN MOTIF; PROTEIN PHOSPHORYLATION; REVIEW; SIGNAL TRANSDUCTION; SOLID TUMOR; STOMACH CANCER; ANIMAL; ANTAGONISTS AND INHIBITORS; CHEMICAL STRUCTURE; METABOLISM;

ANIMALS; HUMANS; MODELS, MOLECULAR; SMALL MOLECULE LIBRARIES; STAT TRANSCRIPTION FACTORS;

EID: 84919419803     PISSN: 00142999     EISSN: 18790712     Source Type: Journal    
DOI: 10.1016/j.ejphar.2014.05.047     Document Type: Article

References (42)

1. L. Adamkova, K. Souckova, and J. Kovarik Transcription protein STAT1: biology and relation to cancer Folia Biol. 53 2007 1 6
2. S. Agrawal, M. Febbraio, E. Podrez, M.K. Cathcart, G.R. Stark, and G.M. Chisolm Signal transducer and activator of transcription 1 is required for optimal foam cell formation and atherosclerotic lesion development Circulation 115 2007 2939 2947
3. M.A. Bill, J.R. Fuchs, C. Li, J. Yui, C. Bakan, D.M. Benson Jr.; E.B. Schwartz, D. Abdelhamid, J. Lin, D.G. Hoyt, S.L. Fossey, G.S. Young, W.E. Carson 3rd, P.K. Li, and G.B. Lesinski The small molecule curcumin analog FLLL32 induces apoptosis in melanoma cells via STAT3 inhibition and retains the cellular response to cytokines with anti-tumor activity Mol. Cancer 9 2010 165
4. M.A. Bill, C. Nicholas, T.A. Mace, J.P. Etter, C. Li, E.B. Schwartz, J.R. Fuchs, G.S. Young, L. Lin, J. Lin, L. He, M. Phelps, P.K. Li, and G.B. Lesinski Structurally modified curcumin analogs inhibit STAT3 phosphorylation and promote apoptosis of human renal cell carcinoma and melanoma cell lines PloS One 7 2012 e40724
5. T. Bowman, R. Garcia, J. Turkson, and R. Jove STATs in oncogenesis Oncogene 19 2000 2474 2488
6. H. Chen, Z. Yang, C. Ding, L. Chu, Y. Zhang, K. Terry, H. Liu, Q. Shen, and J. Zhou Fragment-based drug design and identification of HJC0123, a novel orally bioavailable STAT3 inhibitor for cancer therapy Eur. J. Med. Chem. 62 2013 498 507
7. Y. Chiba, S. Nakazawa, M. Todoroki, K. Shinozaki, H. Sakai, and M. Misawa Interleukin-13 augments bronchial smooth muscle contractility with an up-regulation of RhoA protein Am. J. Respir. Cell. Mol. Biol. 40 2009 159 167
8. Y. Chiba, M. Todoroki, Y. Nishida, M. Tanabe, and M. Misawa A novel STAT6 inhibitor AS1517499 ameliorates antigen-induced bronchial hypercontractility in mice Am. J. Respir. Cell. Mol. Biol. 41 2009 516 524
9. I. Cotarla, S. Ren, Y. Zhang, E. Gehan, B. Singh, and P.A. Furth Stat5a is tyrosine phosphorylated and nuclear localized in a high proportion of human breast cancers. International journal of cancer J. Int. du Cancer 108 2004 665 671
10. J.E. Darnell Validating Stat3 in cancer therapy Nat. Med. 11 2005 595 596
11. B. Debnath, S. Xu, and N. Neamati Small molecule inhibitors of signal transducer and activator of transcription 3 (Stat3) protein J. Med. Chem. 55 2012 6645 6668
12. A.M. Gamero, M.R. Young, R. Mentor-Marcel, G. Bobe, A.J. Scarzello, J. Wise, and N.H. Colburn STAT2 contributes to promotion of colorectal and skin carcinogenesis Cancer Prev. Res. 3 2010 495 504
13. P.T. Gunning, W.P. Katt, M. Glenn, K. Siddiquee, J.S. Kim, R. Jove, S.M. Sebti, J. Turkson, and A.D. Hamilton Isoform selective inhibition of STAT1 or STAT3 homo-dimerization via peptidomimetic probes: structural recognition of STAT SH2 domains Bioorg. Med. Chem. Lett. 17 2007 1875 1878
14. C.M. Horvath STAT proteins and transcriptional responses to extracellular signals Trends. Biochem. Sci. 25 2000 496 502
15. J. Hou, U. Schindler, W.J. Henzel, T.C. Ho, M. Brasseur, and S.L. McKnight An interleukin-4-induced transcription factor: IL-4 Stat Science 265 1994 1701 1706
16. N. Jing, and D.J. Tweardy Targeting Stat3 in cancer therapy Anti-Cancer Drugs 16 2005 601 607
17. M.J. Kim, H.J. Nam, H.P. Kim, S.W. Han, S.A. Im, T.Y. Kim, D.Y. Oh, and Y.J. Bang OPB-31121, a novel small molecular inhibitor, disrupts the JAK2/STAT3 pathway and exhibits an antitumor activity in gastric cancer cells Cancer. Lett. 335 2013 145 152
18. D.E. Levy, and J.E. Darnell Jr. Stats: transcriptional control and biological impact Nat. Rev. Mol. Cell. Biol. 3 2002 651 662
19. L. Lin, B. Hutzen, P.K. Li, S. Ball, M. Zuo, S. DeAngelis, E. Foust, M. Sobo, L. Friedman, D. Bhasin, L. Cen, C. Li, and J. Lin A novel small molecule, LLL12, inhibits STAT3 phosphorylation and activities and exhibits potent growth-suppressive activity in human cancer cells Neoplasia 12 2010 39 50
20. L. Lin, B. Hutzen, M. Zuo, S. Ball, S. Deangelis, E. Foust, B. Pandit, M.A. Ihnat, S.S. Shenoy, S. Kulp, P.K. Li, C. Li, J. Fuchs, and J. Lin Novel STAT3 phosphorylation inhibitors exhibit potent growth-suppressive activity in pancreatic and breast cancer cells Cancer. Res. 70 2010 2445 2454
21. A.E. Lovett-Racke, Y. Yang, and M.K. Racke Th1 versus Th17: are T cell cytokines relevant in multiple sclerosis? Biochim. Biophys. Acta. 1812 2011 246 251
22. J. Menke, T. Bork, B. Kutska, K.T. Byrne, M. Blanfeld, M. Relle, V.R. Kelley, and A. Schwarting Targeting transcription factor Stat4 uncovers a role for interleukin-18 in the pathogenesis of severe lupus nephritis in mice Kidney. Int. 79 2011 452 463
23. M.A. Meraz, J.M. White, K.C. Sheehan, E.A. Bach, S.J. Rodig, A.S. Dighe, D.H. Kaplan, J.K. Riley, A.C. Greenlund, D. Campbell, K. Carver-Moore, R.N. DuBois, R. Clark, M. Aguet, and R.D. Schreiber Targeted disruption of the Stat1 gene in mice reveals unexpected physiologic specificity in the JAK-STAT signaling pathway Cell 84 1996 431 442
24. G. Miklossy, T.S. Hilliard, and J. Turkson Therapeutic modulators of STAT signalling for human diseases Nat. Rev. Drug Discov. 12 2013 611 629
25. E.A. Nelson, S.R. Walker, E. Weisberg, M. Bar-Natan, R. Barrett, L.B. Gashin, S. Terrell, J.L. Klitgaard, L. Santo, M.R. Addorio, B.L. Ebert, J.D. Griffin, and D.A. Frank The STAT5 inhibitor pimozide decreases survival of chronic myelogenous leukemia cells resistant to kinase inhibitors Blood 117 2011 3421 3429
26. B.D. Page, S. Fletcher, P. Yue, Z. Li, X. Zhang, S. Sharmeen, A. Datti, J.L. Wrana, S. Trudel, A.D. Schimmer, J. Turkson, and P.T. Gunning Identification of a non-phosphorylated, cell permeable, small molecule ligand for the Stat3 SH2 domain Bioorg. Med. Chem. Lett. 21 2011 5605 5609
27. B.D. Page, H. Khoury, R.C. Laister, S. Fletcher, M. Vellozo, A. Manzoli, P. Yue, J. Turkson, M.D. Minden, and P.T. Gunning Small molecule STAT5-SH2 domain inhibitors exhibit potent antileukemia activity J. Med. Chem. 55 2012 1047 1055
28. Z. Ren, L.A. Cabell, T.S. Schaefer, and J.S. McMurray Identification of a high-affinity phosphopeptide inhibitor of Stat3 Bioorg. Med. Chem. Lett. 13 2003 633 636
29. J. Schust, B. Sperl, A. Hollis, T.U. Mayer, and T. Berg Stattic: a small-molecule inhibitor of STAT3 activation and dimerization Chem. Biol. 13 2006 1235 1242
30. M. Sen, P.J. Tosca, C. Zwayer, M.J. Ryan, J.D. Johnson, K.A. Knostman, P.C. Giclas, J.O. Peggins, J.E. Tomaszewski, T.P. McMurray, C. Li, M.S. Leibowitz, R.L. Ferris, W.E. Gooding, S.M. Thomas, D.E. Johnson, and J.R. Grandis Lack of toxicity of a STAT3 decoy oligonucleotide Cancer. Chemother. Pharmacol. 63 2009 983 995
31. V.M. Shahani, P. Yue, S. Haftchenary, W. Zhao, J.L. Lukkarila, X. Zhang, D. Ball, C. Nona, P.T. Gunning, and J. Turkson Identification of purine-scaffold small-molecule inhibitors of stat3 activation by qsar studies ACS Med. Chem. Lett. 2 2011 79 84
32. M. Shakibaei, K.B. Harikumar, and B.B. Aggarwal Resveratrol addiction: to die or not to die Mol. Nutr. Food. Res. 53 2009 115 128
33. K. Sikorski, S. Chmielewski, A. Olejnik, J.Z. Wesoly, U. Heemann, M. Baumann, and H. Bluyssen STAT1 as a central mediator of IFNgamma and TLR4 signal integration in vascular dysfunction Jak-Stat 1 2012 241 249
34. K. Sikorski, A. Czerwoniec, J.M. Bujnicki, J. Wesoly, and H.A. Bluyssen STAT1 as a novel therapeutical target in pro-atherogenic signal integration of IFNgamma, TLR4 and IL-6 in vascular disease Cytokine. Growth Factor. Rev. 22 2011 211 219
35. H. Song, R. Wang, S. Wang, and J. Lin A low-molecular-weight compound discovered through virtual database screening inhibits Stat3 function in breast cancer cells Proc. Natl. Acad. Sci. U.S.A. 102 2005 4700 4705
36. B. Sperl, M.H. Seifert, and T. Berg Natural product inhibitors of protein-protein interactions mediated by Src-family SH2 domains Bioorg. Med. Chem. Lett. 19 2009 3305 3309
37. M. Szelag, K. Sikorski, A. Czerwoniec, K. Szatkowska, J. Wesoly, and H.A. Bluyssen In silico simulations of STAT1 and STAT3 inhibitors predict SH2 domain cross-binding specificity Eur. J. Pharmacol. 720 2013 38 48
38. S.P. Tu, H. Jin, J.D. Shi, L.M. Zhu, Y. Suo, G. Lu, A. Liu, T.C. Wang, and C.S. Yang Curcumin induces the differentiation of myeloid-derived suppressor cells and inhibits their interaction with cancer cells and related tumor growth Cancer Prev. Res. 5 2012 205 215
39. M.K. Urlam, R. Pireddu, Y. Ge, X. Zhang, Y. Sun, H.R. Lawrence, W.C. Guida, S.M. Sebti, and N.J. Lawrence Development of new-arylbenzamides as stat3 dimerization inhibitors MedChemComm 4 2013 932 941
40. C.L. Yang, Y.Y. Liu, Y.G. Ma, Y.X. Xue, D.G. Liu, Y. Ren, X.B. Liu, Y. Li, and Z. Li Curcumin blocks small cell lung cancer cells migration, invasion, angiogenesis, cell cycle and neoplasia through Janus kinase-STAT3 signalling pathway PloS one 7 2012 e37960
41. H. Yu, and R. Jove The STATs of cancer:new molecular targets come of age Nat. Rev. Cancer 4 2004 97 105
42. H. Yu, M. Kortylewski, and D. Pardoll Crosstalk between cancer and immune cells: role of STAT3 in the tumour microenvironment Nat. Rev. Immunol. 7 2007 41 51