Novel peptidomimetic inhibitors of signal transducer and activator of transcription 3 dimerization and biological activity

Molecular Cancer Therapeutics

Volumn 3, Issue 3, 2004, Pages 261-269

  Turkson, James ^a,b   Kim, Joon S ^c   Zhang, Shumin ^a,b   Yuan, Jing ^a,b   Huang, Mei ^a,b   Glenn, Matthew ^c   Haura, Eric ^b   Sebti, Said ^a,b   Hamilton, Andrew D ^c   Jove, Richard ^a,b  

^a H LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE   (United States)

^b UNIVERSITY OF SOUTH FLORIDA   (United States)

^c YALE UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ALANYLPHOSPHOTYROSYLLEUCINE; ANTINEOPLASTIC AGENT; ISS 219; ISS 221; ISS 223; ISS 248; ISS 249; ISS 265; ISS 352; ISS 353; ISS 355; ISS 360; ISS 363; ISS 375; ISS 493; ISS 593; ISS 610; ISS 637; PHOSPHOPEPTIDE; PHOSPHOTYROSINE; PROLYLPHOSPHOTYROSYLLEUCINE; PROTEIN INHIBITOR; PROTEIN KINASE P60; PROTEIN SH2; STAT3 PROTEIN; TRANSCRIPTION FACTOR; TRIPEPTIDE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL CELL; APOPTOSIS; ARTICLE; BIOCHEMISTRY; BREAST CARCINOMA; CANCER CELL CULTURE; CANCER GROWTH; CELL GROWTH; CELL SURVIVAL; CELL TRANSFORMATION; CONTROLLED STUDY; DIMERIZATION; DRUG ACTIVITY; DRUG DESIGN; DRUG STRUCTURE; DRUG TARGETING; FIBROBLAST; GROWTH INHIBITION; HUMAN; HUMAN CELL; IN VITRO STUDY; INHIBITION KINETICS; LUNG CARCINOMA; MOUSE; NONHUMAN; PRIORITY JOURNAL; PROTEIN DOMAIN; PROTEIN FUNCTION;

AGAR; ANIMALS; ANTINEOPLASTIC AGENTS; APOPTOSIS; BACULOVIRIDAE; BENZOATES; BENZOIC ACIDS; BROMODEOXYURIDINE; CELL DIVISION; CELL LINE; CELL LINE, TUMOR; CELL NUCLEUS; COLORING AGENTS; CYTOSOL; DIMERIZATION; DNA-BINDING PROTEINS; DOSE-RESPONSE RELATIONSHIP, DRUG; FIBROBLASTS; FLOW CYTOMETRY; HUMANS; HYDROGEN BONDING; INHIBITORY CONCENTRATION 50; INSECTS; LUCIFERASES; MICE; MODELS, CHEMICAL; MODELS, MOLECULAR; NIH 3T3 CELLS; PEPTIDES; PHOSPHORYLATION; PLASMIDS; PROTEIN BINDING; PROTEIN CONFORMATION; STAT3 TRANSCRIPTION FACTOR; TIME FACTORS; TRANS-ACTIVATORS;

EID: 3543055012     PISSN: 15357163     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (51)

1. Darnell JE Jr. Transcription factors as targets for cancer therapy. Nat Rev Cancer, 2002;2:740-9.
2. Stark GR, Kerr IM, Williams BR, Silverman RH, Schreiber RD. How cells respond to interferons. Annu Rev Biochem, 1998;67:227-64.
3. Horvath CM. STAT proteins and transcriptional responses to extracellular signals.Trends Biochem Sci, 2000;25:496-502.
4. Darnell JE Jr. STATs and gene regulation. Science, 1997;277:1630-5.
5. Schindler C, Darnell JE Jr. Transcriptional responses to polypeptide ligands: the JAK-STAT pathway. Annu Rev Biochem, 1995;64:621-51.
6. Bromberg J, Darnell JE Jr. The role of STATs in transcriptional control and their impact on cellular function. Oncogene, 2000;19:2468-73.
7. Heinrich PC, Behrmann I, Muller-Newen G, Schaper F, Graeve L. interieukin-6-type cytokine signaling through the gp130/Jak/STAT pathway. Biochem J, 1998;334:297-314.
8. Akira S. Roles of Stat3 defined by tissue-specific gene targeting. Oncogene, 2000;19:2607-11.
9. Hirano T, Ishihara K, Hibi M. Roles of Stat3 in mediating the cell growth, differentiation and survival signals relayed through the IL-6 family of cytokine receptors. Oncogene, 2000;19:2548-56.
10. Kotenko SV, Pestka S. Jak-STAT signal transduction pathway through the eyes of cytokine class II receptor complexes. Oncogene, 2000;19:2557-65.
11. Shuai K, Stark GR, Kerr IM, Darnell JE Jr. A single phosphotyrosine residue of Stat91 required for gene activation by interferon-γ. Science, 1993;261:1744-6.
12. Bowman T, Garcia R, Turkson J, Jove R. STATs in oncogenesis. Oncogene, 2000;19:2474-88.
13. Catlett-Falcone R, Dalton WS, Jove R. STAT proteins as novel targets for cancer therapy. Curr Opin Oncol, 1999;11:490-6.
14. Garcia R, Jove R. Activation of STAT transcription factors in oncogenic tyrosine kinase signaling. J Biomed Sci, 1998;5:79-85.
15. Turkson J, Jove R. STAT proteins: novel molecular targets for cancer drug discovery. Oncogene, 2000;19:6613-26.
16. Song JI, Grandis JR. STAT signaling in head and neck cancer. Oncogene, 2000;19:2489-95.
17. Lin TS, Mahajan S, Frank DA. STAT signaling in the pathogenesis and treatment of leukemias. Oncogene, 2000;19:2496-504.
18. Buettner R, Mora LB, Jove R. Activated STAT signaling in human tumors provides novel molecular targets for therapeutic intervention. Clin Cancer Res, 2002;8:945-54.
19. Shuai K, Horvath CM, Huang LH, Qureshi SA, Cowburn D, Darnell JE Jr. Interferon activation of the transcription factor Stat91 involves dimerization through SH2-phosphotyrosyl peptide interactions. Cell, 1994;76:821-8.
20. Sasse J, Hemmann U, Schwartz C, et al. Mutational analysis of acutephase response factor/Stat3 activation and dimerization. Mol Cell Biol, 1997;17:4677-86.
21. Turkson J, Ryan D, Kim JS, et al. Phosphotyrosyl peptides block Stat3-mediated DNA-binding activity, gene regulation and cell transformation. J Biol Chem, 2001;276:45443-55.
22. Berg T, Cohen SB, Desharnais J, et al. Small-molecule antagonists of Myc/Max dimerization inhibit Myc-induced transformation of chicken embryo fibroblasts. Proc Natl Acad Sci USA, 2002;99: 3830-5.
23. Garcia R, Yu CL, Hudnall A, et al. Constitutive activation of Stat3 in fibroblasts transformed by diverse oncoproteins and in breast carcinoma cells. Cell Growth & Differ, 1997;8:1267-76.
24. Yu CL, Meyer DJ, Campbell GS, et al. Enhanced DNA-binding activity of a Stat3-related protein in cells transformed by the Src oncoprotein. Science, 1995;269:81-3.
25. Johnson PJ, Coussens PM, Danko AV, Shalloway D. Overexpressed pp60c-src can induce focus formation without complete transformation of NIH 3T3 cells. Mol Cell Biol, 1985;5:1073-83.
26. Rojas M, Donahue JP, Tan Z, Lin YZ. Genetic engineering of proteins with cell membrane-permeability. Nat Biotechnol, 1998;16:370-5.
27. Turkson J, Bowman T, Garcia R, Caldenhoven E, De Groot RP, Jove R. Stat3 activation by Src induces specific gene regulation and is required for cell transformation. Mol Cell Biol, 1998;18:2545-52.
28. Yamauchi K, Holt K, Pessin JE. Phosphatidylinositol 3-kinase functions upstream of Ras and Raf in mediating insulin stimulation of c-fos transcription. J Biol Chem, 1993;268:14597-600.
29. Turkson J, Bowman T, Adnane J, et al. Requirement for Ras/Rac1-mediated p38 and c-Jun N-terminal kinase signaling in Stat3 transcriptional activity induced by the Src oncoprotein. Mol Cell Biol, 1999;19: 7519-28.
30. Zhang Y, Turkson J, Carter-Su C, et al. Activation of Stat3 in v-Src transformed fibroblasts requires cooperation of Jak1 kinase activity. J Biol Chem, 2000;275:24935-44.
31. Wagner BJ, Hayes TE, Hoban CJ, Cochran BH. The SIF binding element confers sis/PDGF inducibility onto the c-fos promoter. EMBO J, 1990;9:4477-84.
32. Gouilleux F, Moritz D, Humar M, Moriggl R, Berchtold S, Groner B. Prolactin and interleukin-2 receptors in T lymphocytes signal through MFG-STAT5-like transcription factor. Endocrinology, 1995;136:5700-8.
33. Seidel HM, Milocco LH, Lamb P, Darnell JE Jr, Stein RB, Rosen J. Spacing of palindromic half sites as a determinant of selective STAT (Signal transducers and activators of transcription) DNA bindingand transcriptional activity. Proc Natl Acad Sci USA, 1995;92: 3041-5.
34. Smithgall TE, Briggs SD, Schreiner S, Lerner EC, Chang H, Wilson MB. Control of myeloid differentiation and survival by stats. Oncogene, 2000;19:2612-8.
35. Lin J, Leonard WJ. The role of Stat5a and Stat5b in signaling by IL-2 family cytokines. Oncogene, 2000;19:2566-76.
36. Garcia R, Bowman TL, Niu G, et al. Constitutive activation of Stat3 by the Src and JAK tyrosine kinases participates in growth regulation of human breast carcinoma cells. Oncogene, 2001;20:2499-513.
37. Song L, Turkson J, Karras JG, Jove R, Haura EB. Activation of Stat3 by receptor tyrosine kinases and cytokines regulates survival in human non-small cell carcinoma cells. Oncogene, 2003;22:4150-65.
38. Bromberg JF, Horvath CM, Besser D, Lathem WW, Darnell JE Jr. Stat3 activation is required for cellular transformation by v-src. Mol Cell Biol, 1998;18:2553-8.
39. Catlett-Falcone R, Landowski TH, Oshiro, MM, et al. Constitutive activation of Stat3 signaling confers resistance to apoptosis in human U266 myeloma cells. Immunity, 1999;10:105-15.
40. Epling-Burnette PK, Lui JH, Catlette-Falcone R, et al. Inhibition of Stat3 signaling leads to apoptosis of leukemic large granular lymphocytes and decreased Mcl-1 expression. J Clin Invest, 2001;107:351-62.
41. Grandis JR, Drenning SD, Zang Q, et al. Constitutive activation of Stat3 signaling abrogates apoptosis in squamous cell carcinogenesis in vivo. Proc Natl Acad Sci USA, 2000;97:4227-32.
42. Bowman T, Broome M, Sinibaldi N, et al. Stat3-mediated Myc expression is required for Src oncogenesis and PDGF-induced mitogenesis. Proc Natl Acad Sci USA, 2000;98:7319-24.
43. Bromberg JF, Wrzeszczynska MH, Devgan G, et al. Stat3 as an oncogene. Cell, 1999;98:295-303.
44. Frank DA. STAT signaling in the pathogenesis and treatment of cancer. Mol Med, 1999;5:432-56.
45. Seidel H, Lamb P, Rosen J. Pharmacological intervention in the JAK/STAT signaling pathway. Oncogene, 2000;19:2645-56.
46. Grandis JR, Drenning SD, Chakraborty A, et al. Requirement of Stat3 but not Stat1 activation for epidermal growth factor-mediated cell growth in vitro. J Clin Invest, 1998;102:1385-92.
47. Niu G, Shain K, Huang M, et al. Overexpression of dominant-negative signal transducer and activator of transcription 3 variant in tumor cells leads to production of soluble factors that induce apoptosis and cell cycle arrest. Cancer Res, 2001;61:3276-80.
48. Levitzki A. Protein tyrosine kinases inhibitors as novel therapeutic agents. Pharmacol Ther, 1999;82:231-9.
49. Becker S, Groner B, Muller CW. Three-dimensional structure of the Stat3β homodimer bound to DNA. Nature, 1998;394:145-51.
50. Chen X, Vinkemeier U, Zhao Y, Jeruzalmi D, Darnell JE Jr, Kuriyan J. Crystal structure of a tyrosine phosphorylated STAT-1 dimer bound to DNA. Cell, 1998;93:827-39.
51. Jones G, Willett P, Glen RC, Leach AR, Taylor R. Development and validation of a genetic algorithm for flexible docking. J Mol Biol, 1997; 267:727-48.