Developing histone deacetylase inhibitors as anti-cancer therapeutics

Current Medicinal Chemistry

Volumn 18, Issue 11, 2011, Pages 1658-1671

  Venugopal, B ^a   Evans, T R J ^a  

^a UNIVERSITY OF GLASGOW   (United Kingdom)

Author keywords

Belinostat; Cancer; Epigenetics; HDAC; HDACi; Histone deacetylase inhibitors; Histone deacetylases; Romidepsin; Vorinostat

Indexed keywords

ALPHA INTERFERON; ANTINEOPLASTIC AGENT; BELINOSTAT; CARBOPLATIN; CYCLOPHOSPHAMIDE; DACARBAZINE; DACINOSTAT; DOCETAXEL; ENTINOSTAT; EPIRUBICIN; FLUOROURACIL; FOLINIC ACID; GEMCITABINE; HISTONE; HISTONE DEACETYLASE; HISTONE DEACETYLASE INHIBITOR; JNJ 26481585; LYSINE; MOCETINOSTAT; OXALIPLATIN; PACLITAXEL; PANOBINOSTAT; ROMIDEPSIN; TAMOXIFEN; UNCLASSIFIED DRUG; VALPROIC ACID; VORINOSTAT;

ACETYLATION; ADVANCED CANCER; ANOREXIA; ANTIANGIOGENIC ACTIVITY; ARTICLE; BREAST CANCER; CANCER CELL; CARCINOGENESIS; CARDIOTOXICITY; CELL CYCLE ARREST; CELL DEATH; CHROMATIN ASSEMBLY AND DISASSEMBLY; CLINICAL TRIAL (TOPIC); COLORECTAL CANCER; CUTANEOUS T CELL LYMPHOMA; DIARRHEA; DNA DAMAGE; DNA REPAIR; DRUG CYTOTOXICITY; DRUG EFFICACY; DRUG POTENCY; ECG ABNORMALITY; ELECTROCARDIOGRAM; EPIGENETICS; FATIGUE; GENE EXPRESSION REGULATION; GLIOBLASTOMA; HEART ARRHYTHMIA; HEART ATRIUM FIBRILLATION; HEART VENTRICLE TACHYCARDIA; HEMATOLOGIC MALIGNANCY; HUMAN; HYPERBILIRUBINEMIA; HYPERTRANSAMINASEMIA; KIDNEY CANCER; LUNG CANCER; LUNG NON SMALL CELL CANCER; LYMPHOMA; MELANOMA; MONOTHERAPY; MULTIPLE CYCLE TREATMENT; NAUSEA; NEUROTOXICITY; OVARY CARCINOMA; PANCREAS CANCER; PERITONEUM CANCER; PROSTATE CANCER; PROTEIN PROCESSING; QT PROLONGATION; SIDE EFFECT; SOLID TUMOR; ST SEGMENT; SUDDEN DEATH; SUPRAVENTRICULAR TACHYCARDIA; T WAVE; THROMBOCYTOPENIA; THYROID CANCER; VOMITING;

ANTINEOPLASTIC AGENTS; HISTONE DEACETYLASE INHIBITORS; HUMANS; NEOPLASMS; TREATMENT OUTCOME;

EID: 79955678223     PISSN: 09298673     EISSN: None     Source Type: Journal    
DOI: 10.2174/092986711795471284     Document Type: Article

References (151)

1. Hanahan, D.; Weinberg, R. A. The Hallmarks of Cancer. Cell., 2000, 100 (1), 57-70. (Pubitemid 30046295)
2. Esteller, M. Epigenetics in Cancer. N. Engl. J. Med., 2008, 358 (11), 1148-1159.
3. Jones, P. A.; Baylin, S. B. The Epigenomics of Cancer. Cell., 2007, 128 (4), 683-692. (Pubitemid 46273572)
4. Yoo, C. B.; Jones, P. A. Epigenetic therapy of cancer: past, present and future. Nat. Rev. Drug. Discov., 2006, 5 (1), 37-50.
5. Shahbazian, M. D.; Grunstein, M. Functions of Site-Specific Histone Acetylation and Deacetylation. Annu. Rev. Biochem., 2007, 76 (1), 75-100.
6. Kornberg, R. D.; Lorch, Y. Twenty-Five Years of the Nucleosome, Fundamental Particle of the Eukaryote Chromosome. Cell., 1999, 98 (3), 285-294. (Pubitemid 29380564)
7. Luger, K.; Mader, A. W.; Richmond, R. K.; Sargent, D. F.; Richmond, T. J. Crystal structure of the nucleosome core particle at 2.8A resolution. Nature., 1997, 389 (6648), 251-260. (Pubitemid 27406632)
8. Strahl, B. D.; Allis, C. D. The language of covalent histone modifications. Nature., 2000, 403 (6765), 41-45. (Pubitemid 30038513)
9. Jenuwein, T.; Allis, C. D. Translating the Histone Code. Science., 2001, 293 (5532), 1074-1080. (Pubitemid 32758077)
10. Felsenfeld, G.; Groudine, M. Controlling the double helix. Nature., 2003, 421 (6921), 448-453. (Pubitemid 36157954)
11. Marmorstein, R.; Roth, S. Y. Histone acetyltransferases: function, structure, and catalysis. Curr. Opin. Genet. Dev., 2001, 11 (2), 155-161. (Pubitemid 32209199)
12. Keppler, B. R.; Archer, T. K. Chromatin-modifying enzymes as therapeutic targets- Part 1. Expert. Opin. Ther. Targets., 2008, 12 (10), 1301-1312.
13. Iyer, N. G.; Ozdag, H.; Caldas, C. p300//CBP and cancer. Oncogene., 2004, 23 (24), 4225-4231.
14. Bolden, J. E.; Peart, M. J.; Johnstone, R. W. Anticancer activities of histone deacetylase inhibitors. Nat. Rev. Drug. Discov., 2006, 5 (9), 769-784. (Pubitemid 44348499)
15. Gregoretti, I.; Lee, Y.-M.; Goodson, H. V. Molecular Evolution of the Histone Deacetylase Family: Functional Implications of Phylogenetic Analysis. J. Mol. Biol., 2004, 338 (1), 17-31. (Pubitemid 38429783)
16. Yang, X.-J.; Seto, E. The Rpd3/Hda1 family of lysine deacetylases: from bacteria and yeast to mice and men. Nat. Rev. Mol. Cell. Biol., 2008, 9 (3), 206-218. (Pubitemid 351301825)
17. Haigis, M. C.; Guarente, L. P. Mammalian sirtuins"emerging roles in physiology, aging, and calorie restriction. Genes & Dev., 2006, 20 (21), 2913-2921. (Pubitemid 44771725)
18. Liu, T.; Liu, P. Y.; Marshall, G. M. The Critical Role of the Class III Histone Deacetylase SIRT1 in Cancer. Cancer. Res., 2009, 69 (5), 1702-1705.
19. Lagger, G.; O'Carroll, D.; Rembold, M.; Khier, H.; Tischler, J.; Weitzer, G.; Schuettengruber, B.; Hauser, C.; Brunmeir, R.; Jenuwein, T.; Seiser, C. Essential function of histone deacetylase 1 in proliferation control and CDK inhibitor repression. EMBO J., 2002, 21 (11), 2672-2681. (Pubitemid 34619383)
20. Bhaskara, S.; Chyla, B. J.; Amann, J. M.; Knutson, S. K.; Cortez, D.; Sun, Z.-W.; Hiebert, S. W. Deletion of Histone Deacetylase 3 Reveals Critical Roles in S Phase Progression and DNA Damage Control. Mol. cell., 2008, 30 (1), 61-72. (Pubitemid 351470157)
21. Fischle, W.; Dequiedt, F.; Hendzel, M. J.; Guenther, M. G.; Lazar, M. A.; Voelter, W.; Verdin, E. Enzymatic Activity Associated with Class II HDACs Is Dependent on a Multiprotein Complex Containing HDAC3 and SMRT/NCoR. Mol. cell., 2002, 9 (1), 45-57. (Pubitemid 34127770)
22. Montgomery, R. L.; Davis, C. A.; Potthoff, M. J.; Haberland, M.; Fielitz, J.; Qi, X.; Hill, J. A.; Richardson, J. A.; Olson, E. N. Histone deacetylases 1 and 2 redundantly regulate cardiac morphogenesis, growth, and contractility. Genes & Dev., 2007, 21 (14), 1790-1802. (Pubitemid 47076478)
23. Vega, R. B.; Matsuda, K.; Oh, J.; Barbosa, A. C.; Yang, X.; Meadows, E.; McAnally, J.; Pomajzl, C.; Shelton, J. M.; Richardson, J. A.; Karsenty, G.; Olson, E. N. Histone Deacetylase 4 Controls Chondrocyte Hypertrophy during Skeletogenesis. Cell., 2004, 119 (4), 555-566. (Pubitemid 39482354)
24. Zhang, C. L.; McKinsey, T. A.; Chang, S.; Antos, C. L.; Hill, J. A.; Olson, E. N. Class II Histone Deacetylases Act as Signal-Responsive Repressors of Cardiac Hypertrophy. Cell., 2002, 110 (4), 479-488. (Pubitemid 35232291)
25. Chang, S.; Young, B. D.; Li, S.; Qi, X.; Richardson, J. A.; Olson, E. N. Histone Deacetylase 7 Maintains Vascular Integrity by Repressing Matrix Metalloproteinase 10. Cell., 2006, 126 (2), 321-334. (Pubitemid 44092958)
26. Zhang, Y.; Kwon, S.; Yamaguchi, T.; Cubizolles, F.; Rousseaux, S.; Kneissel, M.; Cao, C.; Li, N.; Cheng, H.-L.; Chua, K.; Lombard, D.; Mizeracki, A.; Matthias, G.; Alt, F. W.; Khochbin, S.; Matthias, P. Mice Lacking Histone Deacetylase 6 Have Hyperacetylated Tubulin but Are Viable and Develop Normally. Mol. Cell. Biol., 2008, 28 (5), 1688-1701.
27. Hubbert, C.; Guardiola, A.; Shao, R.; Kawaguchi, Y.; Ito, A.; Nixon, A.; Yoshida, M.; Wang, X.-F.; Yao, T.-P. HDAC6 is a microtubule-associated deacetylase. Nature., 2002, 417 (6887), 455-458. (Pubitemid 34563539)
28. Tran, A. D.-A.; Marmo, T. P.; Salam, A. A.; Che, S.; Finkelstein, E.; Kabarriti, R.; Xenias, H. S.; Mazitschek, R.; Hubbert, C.; Kawaguchi, Y.; Sheetz, M. P.; Yao, T.-P.; Bulinski, J. C. HDAC6 deacetylation of tubulin modulates dynamics of cellular adhesions. J. Cell. Sci., 2007, 120 (8), 1469-1479. (Pubitemid 46780039)
29. Kovacs, J. J.; Murphy, P. J. M.; Gaillard, S.; Zhao, X.; Wu, J.-T.; Nicchitta, C. V.; Yoshida, M.; Toft, D. O.; Pratt, W. B.; Yao, T.-P. HDAC6 Regulates Hsp90 Acetylation and Chaperone-Dependent Activation of Glucocorticoid Receptor. Mol. Cell., 2005, 18 (5), 601-607. (Pubitemid 40726236)
30. Kawaguchi, Y.; Kovacs, J. J.; McLaurin, A.; Vance, J. M.; Ito, A.; Yao, T.-P. The Deacetylase HDAC6 Regulates Aggresome Formation and Cell Viability in Response to Misfolded Protein Stress. Cell., 2003, 115 (6), 727-738. (Pubitemid 38030301)
31. Fraga, M. F.; Ballestar, E.; Villar-Garea, A.; Boix-Chornet, M.; Espada, J.; Schotta, G.; Bonaldi, T.; Haydon, C.; Ropero, S.; Petrie, K.; Iyer, N. G.; Perez-Rosado, A.; Calvo, E.; Lopez, J. A.; Cano, A.; Calasanz, M. J.; Colomer, D.; Piris, M. A.; Ahn, N.; Imhof, A.; Caldas, C.; Jenuwein, T.; Esteller, M. Loss of acetylation at Lys16 and trimethylation at Lys20 of histone H4 is a common hallmark of human cancer. Nat. Genet., 2005, 37 (4), 391-400.
32. Yasui, W.; Oue, N.; Ono, S.; Mitani, Y.; Ito, R.; Nakayama, H. Histone Acetylation and Gastrointestinal Carcinogenesis. Ann. N Y. Acad. Sci., 2003, 983 (1), 220-231. (Pubitemid 36399335)
33. Zhu, P.; Martin, E.; Mengwasser, J.; Schlag, P.; Janssen, K.-P.; Göttlicher, M. Induction of HDAC2 expression upon loss of APC in colorectal tumorigenesis. Cancer. Cell., 2004, 5 (5), 455-463. (Pubitemid 38610247)
34. Choi, J.; Kwon, H.; Yoon, B.; Yoon, J.; Hoon, S.; Soo, H.; Kim, D. Expression profile of histone deacetylase 1 in gastric cancer tissues. Jpn. J. Cancer. Res., 2001, 92(12), 1300-1304. (Pubitemid 34036893)
35. Song, J. Increased expression of histone deacetylase 2 is found in human gastric cancer. APMIS., 2005, 113, 264-268. (Pubitemid 40676807)
36. Wilson, A. J. Histone deacetylase 3 (HDAC3) and other class I HDACs regulate colon cell maturation and p21 expression and are deregulated in human colon cancer. J. Biol. Chem., 2006, 281, 13548-13558. (Pubitemid 43855268)
37. Halkidou, K. Upregulation and nuclear recruitment of HDAC1 in hormone refractory prostate cancer. Prostate., 2004, 59, 177-189. (Pubitemid 38481229)
38. Zhang, Z.; Yamashita, H.; Toyama, T.; Sugiura, H.; Omoto, Y.; Ando, Y.; Mita, K.; Hamaguchi, M.; Hayashi, S.-i.; Iwase, H. HDAC6 Expression Is Correlated with Better Survival in Breast Cancer. Clin. Cancer. Res., 2004, 10 (20), 6962-6968. (Pubitemid 39383047)
39. Weichert, W.; Röske, A.; Gekeler, V.; Beckers, T.; Ebert, M. P. A.; Pross, M.; Dietel, M.; Denkert, C.; Röcken, C. Association of patterns of class I histone deacetylase expression with patient prognosis in gastric cancer: a retrospective analysis. Lancet. Oncol., 2008, 9 (2), 139-148.
40. Wilko, W.; Annika, R.; Volker, G.; Thomas, B.; Matthias, P. A. E.; Matthias, P.; Manfred, D.; Carsten, D.; Christoph, R. Association of patterns of class I histone deacetylase expression with patient prognosis in gastric cancer: a retrospective analysis. Lancet. Oncol., 2008, 9 (2), 139-148.
41. Weichert, W.; Raske, A.; Niesporek, S.; Noske, A.; Buckendahl, A.-C.; Dietel, M.; Gekeler, V.; Boehm, M.; Beckers, T.; Denkert, C. Class I Histone Deacetylase Expression Has Independent Prognostic Impact in Human Colorectal Cancer: Specific Role of Class I Histone Deacetylases In vitro and In vivo. Clin. Cancer. Res., 2008, 14 (6), 1669-1677. (Pubitemid 351469450)
42. Weichert, W. HDAC expression and clinical prognosis in human malignancies. Cancer. Lett., 2009, 280 (2), 168-176.
43. Oehme, I.; Deubzer, H. E.; Lodrini, M.; Milde, T.; Witt, O. Targeting of HDAC8 and investigational inhibitors in neuroblastoma. Expert. Opin. Inv. Drugs., 2009, 18 (11), 1605-1617.
44. Weichert, W.; C. Denkert; A. Noske; S. Darb-Esfahani; M. Dietel; S.E. Kalloger; Huntsman, D. G.; M. Köbel, Expression of class I histone deacetylases indicates poor prognosis in endometrioid subtypes of ovarian and endometrial carcinomas. Neoplasia., 2008, 10, 1021-1027.
45. Riggs, M. G.; Whittaker, R. G.; Neumann, J. R.; Ingram, V. M. n-Butyrate causes histone modification in HeLa and Friend erythroleukaemia cells. Nature., 1977, 268 (5619), 462-464.
46. Marks, P. A.; Breslow, R. Dimethyl sulfoxide to vorinostat: development of this histone deacetylase inhibitor as an anticancer drug. Nat. Biotech., 2007, 25 (1), 84-90. (Pubitemid 46087907)
47. Finnin, M. S.; Donigian, J. R.; Cohen, A.; Richon, V. M.; Rifkind, R. A.; Marks, P. A.; Breslow, R.; Pavletich, N. P. Structures of a histone deacetylase homologue bound to the TSA and SAHA inhibitors. Nature., 1999, 401 (6749), 188-193. (Pubitemid 29436325)
48. Miller, T. A.; Witter, D. J.; Belvedere, S. Histone Deacetylase Inhibitors. J. Med. Chem., 2003, 46 (24), 5097-5116. (Pubitemid 37414179)
49. Khan, N.; Jeffers, M.; Kumar, S.; Hackett, C.; Boldog, F.; Khramtsov, N.; Qian, X.; Mills, E.; Berghs, S. C.; Carey, N.; Finn, P. W.; Collins, L. S.; Tumber, A.; Ritchie, J. W.; Jensen, P. B.; Lichenstein, H. S.; Sehested, M. Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors. Biochem. J., 2008, 409 (2), 581-589. (Pubitemid 351184977)
50. Balasubramanian, S.; Verner, E.; Buggy, J. J. Isoform-specific histone deacetylase inhibitors: The next step? Cancer Lett., 2009, 280 (2), 211-221.
51. Johnstone, R. W.; Ruefli, A. A.; Lowe, S. W. Apoptosis: A Link between Cancer Genetics and Chemotherapy. Cell., 2002, 108 (2), 153-164. (Pubitemid 34161136)
52. Insinga, A.; Monestiroli, S.; Ronzoni, S.; Gelmetti, V.; Marchesi, F.; Viale, A.; Altucci, L.; Nervi, C.; Minucci, S.; Pelicci, P. G. Inhibitors of histone deacetylases induce tumor-selective apoptosis through activation of the death receptor pathway. Nat. Med., 2005, 11 (1), 71-76. (Pubitemid 40215840)
53. Minucci, S.; Pelicci, P. G. Histone deacetylase inhibitors and the promise of epigenetic (and more) treatments for cancer. Nat. Rev. Cancer., 2006, 6 (1), 38-51. (Pubitemid 43054973)
54. Ruefli, A. A.; Ausserlechner, M. J.; Bernhard, D.; Sutton, V. R.; Tainton, K. M.; Kofler, R.; Smyth, M. J.; Johnstone, R. W. The histone deacetylase inhibitor and chemotherapeutic agent suberoylanilide hydroxamic acid (SAHA) induces a cell-death pathway characterized by cleavage of Bid and production of reactive oxygen species. Proc. Natl. Acad. Sci. U S A., 2001, 98 (19), 10833-10838. (Pubitemid 32878706)
55. Peart, M. J.; Tainton, K. M.; Ruefli, A. A.; Dear, A. E.; Sedelies, K. A.; O' Reilly, L. A.; Waterhouse, N. J.; Trapani, J. A.; Johnstone, R. W. Novel Mechanisms of Apoptosis Induced by Histone Deacetylase Inhibitors. Cancer. Res., 2003, 63 (15), 4460-4471. (Pubitemid 36951018)
56. Ungerstedt, J. S.; Sowa, Y.; Xu, W. S.; Shao, Y.; Dokmanovic, M.; Perez, G.; Ngo, L.; Holmgren, A.; Jiang, X.; Marks, P. A. Role of thioredoxin in the response of normal and transformed cells to histone deacetylase inhibitors. Proc. Natl. Acad. Sci. U S A., 2005, 102 (3), 673-678. (Pubitemid 40282724)
57. Marks, P. A. Thioredoxin in cancer--Role of histone deacetylase inhibitors. Semin. Cancer. Biol., 2006, 16 (6), 436-443. (Pubitemid 44780137)
58. Butler, L. M.; Zhou, X.; Xu, W.-S.; Scher, H. I.; Rifkind, R. A.; Marks, P. A.; Richon, V. M. The histone deacetylase inhibitor SAHA arrests cancer cell growth, up-regulates thioredoxin-binding protein-2, and down-regulates thioredoxin. Proc. Natl. Acad. Sci. U S A., 2002, 99 (18), 11700-11705. (Pubitemid 34994462)
59. Vousden, K. H.; Ryan, K. M. p53 and metabolism. Nat. Rev. Cancer., 2009, 9 (10), 691-700.
60. Shao, Y.; Gao, Z.; Marks, P. A.; Jiang, X. Apoptotic and autophagic cell death induced by histone deacetylase inhibitors. Proc. Natl. Acad. Sci. U S A., 2004, 101 (52), 18030-18035. (Pubitemid 40054069)
61. Schrump, D. S. Cytotoxicity Mediated by Histone Deacetylase Inhibitors in Cancer Cells: Mechanisms and Potential Clinical Implications. Clin. Cancer. Res., 2009, 15 (12), 3947-3957.
62. Qiu, L.; Burgess, A.; Fairlie, D. P.; Leonard, H.; Parsons, P. G.; Gabrielli, B. G. Histone Deacetylase Inhibitors Trigger a G2 Checkpoint in Normal Cells That Is Defective in Tumor Cells. Mol. Biol. Cell., 2000, 11 (6), 2069-2083. (Pubitemid 30408065)
63. Lee, J. H.; Choy, M. L.; Ngo, L.; Foster, S. S.; Marks, P. A. Histone deacetylase inhibitor induces DNA damage, which normal but not transformed cells can repair. Proc. Natl. Acad. Sci. U S A., 2010, 107 (33), 14639-14644.
64. Adimoolam, S.; Sirisawad, M.; Chen, J.; Thiemann, P.; Ford, J. M.; Buggy, J. J. HDAC inhibitor PCI-24781 decreases RAD51 expression and inhibitshomologous recombination. Proc. Natl. Acad. Sci. U S A., 2007, 104 (49), 19482-19487.
65. Cohen, H. Y.; Lavu, S.; Bitterman, K. J.; Hekking, B.; Imahiyerobo, T. A.; Miller, C.; Frye, R.; Ploegh, H.; Kessler, B. M.; Sinclair, D. A. Acetylation of the C Terminus of Ku70 by CBP and PCAF Controls Bax-Mediated Apoptosis. Mol. cell., 2004, 13 (5), 627-638. (Pubitemid 38368121)
66. Eot-Houllier, G.; Fulcrand, G.; Magnaghi-Jaulin, L.; Jaulin, C. Histone deacetylase inhibitors and genomic instability. Cancer. Lett., 2009, 274 (2), 169-176.
67. Kim, M. S.; Blake, M.; Baek, J. H.; Kohlhagen, G.; Pommier, Y.; Carrier, F. Inhibition of Histone Deacetylase Increases Cytotoxicity to Anticancer Drugs Targeting DNA. Cancer. Res., 2003, 63 (21), 7291-7300. (Pubitemid 37413470)
68. VanLint, C.; Emiliani, S.; Verdin, E. The expression of a small fraction of cellular genes is changed in response to histone hyperacetylation. Gene. Expr., 1996, 5(4-5), 245-253.
69. Peart, M. J.; Smyth, G. K.; van Laar, R. K.; Bowtell, D. D.; Richon, V. M.; Marks, P. A.; Holloway, A. J.; Johnstone, R. W. Identification and functional significance of genes regulated by structurally different histone deacetylase inhibitors. Proc. Natl. Acad. Sci. U S A., 2005, 102 (10), 3697-3702. (Pubitemid 40354674)
70. Glaser, K. B.; Staver, M. J.; Waring, J. F.; Stender, J.; Ulrich, R. G.; Davidsen, S. K. Gene expression profiling of multiple histone deacetylase (HDAC) inhibitors: defining a common gene set produced by HDAC inhibition in T24 and MDA carcinoma cell lines. Mol. Cancer. Ther., 2003, 2 (2), 151-163.
71. Gui, C. Y.; Ngo, L.; Xu, W. S.; Richon, V. M.; Marks, P. A. Histone deacetylase (HDAC) inhibitor activation of p21WAF1 involves changes in promoter-associated proteins, including HDAC1. Proc. Natl. Acad. Sci. U S A., 2004, 101 (5), 1241-1246 (Pubitemid 38182673)
72. Richon, V. M.; Sandhoff, T. W.; Rifkind, R. A.; Marks, P. A. Histone deacetylase inhibitor selectively induces p21WAF1 expression and geneassociated histone acetylation. Proc. Natl. Acad. Sci. U S A., 2000, 97 (18), 10014-10019.
73. Zhao, Y.; Lu, S.; Wu, L.; Chai, G.; Wang, H.; Chen, Y.; Sun, J.; Yu, Y.; Zhou, W.; Zheng, Q.; Wu, M.; Otterson, G. A.; Zhu, W.-G. Acetylation of p53 at Lysine 373/382 by the Histone Deacetylase Inhibitor Depsipeptide Induces Expression of p21Waf1/Cip1. Mol. Cell. Biol., 2006, 26 (7), 2782-2790.
74. Juan, L.-J.; Shia, W.-J.; Chen, M.-H.; Yang, W.-M.; Seto, E.; Lin, Y.-S.; Wu, C.-W. Histone Deacetylases Specifically Down-regulate p53-dependent Gene Activation. Journal of Biological Chemistry., 2000, 275 (27), 20436-20443. (Pubitemid 30457621)
75. Luo, J.; Su, F.; Chen, D.; Shiloh, A.; Gu, W. Deacetylation of p53 modulates its effect on cell growth and apoptosis. Nature., 2000, 408 (6810), 377-381.
76. Wang, L. G.; Ossowski, L.; Ferrari, A. C. Androgen receptor level controlled by a suppressor complex lost in an androgen-independent prostate cancer cell line. Oncogene., 2004, 23 (30), 5175-5184. (Pubitemid 38980350)
77. Welsbie, D. S.; Xu, J.; Chen, Y.; Borsu, L.; Scher, H. I.; Rosen, N.; Sawyers, C. L. Histone Deacetylases Are Required for Androgen Receptor Function in Hormone-Sensitive and Castrate-Resistant Prostate Cancer. Cancer. Res., 2009, 69 (3), 958-966.
78. Ferrara, N.; Kerbel, R. S. Angiogenesis as a therapeutic target. Nature., 2005, 438 (7070), 967-974. (Pubitemid 43093963)
79. Kim, M. S.; Kwon, H. J.; Lee, Y. M.; Baek, J. H.; Jang, J.-E.; Lee, S.-W.; Moon, E.-J.; Kim, H.-S.; Lee, S.-K.; Chung, H. Y.; Kim, C. W.; Kim, K.-W. Histone deacetylases induce angiogenesis by negative regulation of tumor suppressor genes. Nat. Med., 2001, 7 (4), 437-443. (Pubitemid 32298546)
80. Qian, D. Z.; Kato, Y.; Shabbeer, S.; Wei, Y.; Verheul, H. M. W.; Salumbides, B.; Sanni, T.; Atadja, P.; Pili, R. Targeting Tumor Angiogenesis with Histone Deacetylase Inhibitors: the Hydroxamic Acid Derivative LBH589. Clin. Cancer. Res., 2006, 12 (2), 634-642. (Pubitemid 43166159)
81. Ellis, L.; Hammers, H.; Pili, R. Targeting tumor angiogenesis with histone deacetylase inhibitors. Cancer. Lett., 2009, 280 (2), 145-153.
82. Qian, D. Z.; Kachhap, S. K.; Collis, S. J.; Verheul, H. M. W.; Carducci, M. A.; Atadja, P.; Pili, R. Class II Histone Deacetylases Are Associated with VHL-Independent Regulation of Hypoxia-Inducible Factor 1-. Cancer. Res., 2006, 66 (17), 8814-8821. (Pubitemid 44449199)
83. Bali, P.; Pranpat, M.; Bradner, J.; Balasis, M.; Fiskus, W.; Guo, F.; Rocha, K.; Kumaraswamy, S.; Boyapalle, S.; Atadja, P.; Seto, E.; Bhalla, K. Inhibition of Histone Deacetylase 6 Acetylates and Disrupts the Chaperone Function of Heat Shock Protein 90. J. Bio. Chem., 2005, 280 (29), 26729-26734.
84. Yu, X.; Guo, Z. S.; Marcu, M. G.; Neckers, L.; Nguyen, D. M.; Chen, G. A.; Schrump, D. S. Modulation of p53, ErbB1, ErbB2, and Raf-1 Expression in Lung Cancer Cells by Depsipeptide FR901228. J. Natl. Cancer. Inst., 2002, 94 (7), 504-513. (Pubitemid 34411289)
85. Trepel, J.; Mollapour, M.; Giaccone, G.; Neckers, L. Targeting the dynamic HSP90 complex in cancer. Nat. Rev. Cancer., 2009,10 (8), 537-549.
86. de Bono, J. S.; Kristeleit, R.; Tolcher, A.; Fong, P.; Pacey, S.; Karavasilis, V.; Mita, M.; Shaw, H.; Workman, P.; Kaye, S.; Rowinsky, E. K.; Aherne, W.; Atadja, P.; Scott, J. W.; Patnaik, A. Phase I Pharmacokinetic and Pharmacodynamic Study of LAQ824, a Hydroxamate Histone Deacetylase Inhibitor with a Heat Shock Protein-90 Inhibitory Profile, in Patients with Advanced Solid Tumors. Clin. Cancer. Res., 2008, 14 (20), 6663-6673.
87. Chen, L.; Meng, S.; Wang, H.; Bali, P.; Bai, W.; Li, B.; Atadja, P.; Bhalla, K. N.; Wu, J. Chemical ablation of androgen receptor in prostate cancer cells by the histone deacetylase inhibitor LAQ824. Mol. Cancer. Ther., 2005, 4 (9), 1311-1319.
88. Thomas, S.; Munster, P. N. Histone deacetylase inhibitor induced modulation of anti-estrogen therapy. Cancer. Lett., 2009, 280 (2), 184-191.
89. National cancer institute-Clinical trials search results. http://www.cancer. gov/Search/ResultsClinicalTrials.aspx?protocolsearchid= 8231689, (accessed 24th September 2010).
90. Ma, X.; Ezzeldin, H. H.; Diasio, R. B. Histone Deacetylase Inhibitors: Current Status and Overview of Recent Clinical Trials. Drugs., 2009, 69 (14), 1911-1934.
91. Prince, H. M.; Bishton, M. J.; Harrison, S. J. Clinical Studies of Histone Deacetylase Inhibitors Clin. Cancer. Res., 2009, 15 (12), 3958-3969.
92. Stimson, L.; Wood, V.; Khan, O.; Fotheringham, S.; La Thangue, N. B. HDAC inhibitor-based therapies and haematological malignancy. Ann. Oncol., 2009, 20 (8), 1293-1302.
93. Yoshida, M.; Kijima, M.; Akita, M.; Beppu, T. Potent and specific inhibition of mammalian histone deacetylase both in vivo and in vitro by trichostatin A. J. Bio. Chem., 1990, 265 (28), 17174-17179.
94. Mann, B. S.; Johnson, J. R.; Sridhara, R.; Abraham, E.; Booth, b.; Verbois, L. Vorinostat for treatment of cutaneous manifestations of advanced primary cutaneous T-cell lymphoma. Clin. Cancer. Res., 2007, 13, 2318-2322 (Pubitemid 46698579)
95. Richon, V. M.; Emiliani, S.; Verdin, E.; Webb, Y.; Breslow, R.; Rifkind, R. A.; Marks, P. A. A class of hybrid polar inducers of transformed cell differentiation inhibits histone deacetylases. Proc. Natl. Acad. Sci. U S A., 1998, 95 (6), 3003-3007. (Pubitemid 28135844)
96. Kelly, W. K.; Richon, V. M.; O'Connor, O.; Curley, T.; MacGregor-Curtelli, B.; Tong, W. Phase I clinical trial of histone deacetylase inhibitor: suberoylanilide hydroxamic acid administered intravenously. Clin. Cancer. Res., 2003, 9, 3578-3588.
97. Kelly, W. K.; O'Connor, O. A.; Krug, L. M.; Chiao, J. H.; Heaney, M.; Curley, T. Phase I study of an oral histone deacetylase inhibitor, suberoylanilide hydroxamic acid, in patients with advanced cancer. J. Clin. Oncol., 2005, 23, 3923-3931. (Pubitemid 46218695)
98. O'Connor, O. A.; Heaney, M. L.; Schwartz, L.; Richardson, S.; Willim, R.; MacGregor-Cortelli, B.; Curly, T.; Moskowitz, C.; Portlock, C.; Horwitz, S.; Zelenetz, A. D.; Frankel, S.; Richon, V.; Marks, P.; Kelly, W. K. Clinical Experience With Intravenous and Oral Formulations of the Novel Histone Deacetylase Inhibitor Suberoylanilide Hydroxamic Acid in Patients With Advanced Hematologic Malignancies. J. Clin. Oncol., 2006, 24 (1), 166-173. (Pubitemid 46630509)
99. Piekarz, R. L.; Robey, R.; Sandor, V.; Bakke, S.; Wilson, W. H.; Dahmoush, L.; Kingma, D. M.; Turner, M. L.; Altemus, R.; Bates, S. E. Inhibitor of histone deacetylation, depsipeptide (FR901228), in the treatment of peripheral and cutaneous T-cell lymphoma: a case report. Blood., 2001, 98 (9), 2865-2868.
100. Duvic, M.; Talpur, R.; Ni, X.; Zhang, C.; Hazarika, P.; Kelly, C.; Chiao, J. H.; Reilly, J. F.; Ricker, J. L.; Richon, V. M.; Frankel, S. R. Phase 2 trial of oral vorinostat (suberoylanilide hydroxamic acid, SAHA) for refractory cutaneous T-cell lymphoma (CTCL). Blood., 2007, 109 (1), 31-39. (Pubitemid 46053039)
101. Olsen, E. A.; Kim, Y. H.; Kuzel, T. M.; Pacheco, T. R.; Foss, F. M.; Parker, S.; Frankel, S. R.; Chen, C.; Ricker, J. L.; Arduino, J. M.; Duvic, M. Phase IIB Multicenter Trial of Vorinostat in Patients With Persistent, Progressive, or Treatment Refractory Cutaneous T-Cell Lymphoma. J. Clin. Oncol., 2007, 25 (21), 3109-3115. (Pubitemid 47218059)
102. Luu, T. H.; Morgan, R. J.; Leong, L.; Lim, D.; McNamara, M.; Portnow, J.; Frankel, P.; Smith, D. D.; Doroshow, J. H.; Gandara, D. R.; Aparicio, A.; Somlo, G.; Wong, C. A Phase II Trial of Vorinostat (Suberoylanilide Hydroxamic Acid) in Metastatic Breast Cancer: A California Cancer Consortium Study. Clin. Cancer. Res., 2008, 14 (21), 7138-7142.
103. Modesitt, S. C.; Sill, M.; Hoffman, J. S.; Bender, D. P. A phase II study of vorinostat in the treatment of persistent or recurrent epithelial ovarian or primary peritoneal carcinoma: A Gynecologic Oncology Group study. Gynecol. Oncol. , 2008, 109 (2), 182-186.
104. Vansteenkiste, J.; Cutsem, E. V.; Dumez, H.; Chen, C.; Ricker, J. L.; Randolph, S. S. Early phase II trial of oral vorinostat in relapsed or refractory breast, colorectal, or non-small cell lung cancer. Invest. New. Drugs., 2008, 26, 483-488.
105. Woyach, J. A.; Kloos, R. T.; Ringel, M. D.; Arbogast, D.; Collamore, M.; Zwiebel, J. A.; Grever, M.; Villalona-Calero, M.; Shah, M. H. Lack of Therapeutic Effect of the Histone Deacetylase Inhibitor Vorinostat in Patients with Metastatic Radioiodine-Refractory Thyroid Carcinoma. J. Clin. Endocrinol. Metab., 2009, 94 (1), 164-170.
106. Galanis, E.; Jaeckle, K. A.; Maurer, M. J.; Reid, J. M.; Ames, M. M.; Hardwick, J. S.; Reilly, J. F.; Loboda, A.; Nebozhyn, M.; Fantin, V. R.; Richon, V. M.; Scheithauer, B.; Giannini, C.; Flynn, P. J.; Moore, D. F.; Zwiebel, J.; Buckner, J. C. Phase II Trial of Vorinostat in Recurrent Glioblastoma Multiforme: A North Central Cancer Treatment Group Study. J. Clin. Oncol., 2009, 27 (12), 2052-2058.
107. Siegel, D.; Hussein, M.; Belani, C.; Robert, F.; Galanis, E.; Richon, V.; Garcia-Vargas, J.; Sanz-Rodriguez, C.; Rizvi, S. Vorinostat in solid and hematologic malignancies. J. Hematol. Oncol., 2009, 2 (1), 31.
108. Plumb, J. A.; Finn, P. W.; Williams, R. J.; Bandara, M. J.; Romero, M. R.; Watkins, C. J.; La Thangue, N. B.; Brown, R. Pharmacodynamic Response and Inhibition of Growth of Human Tumor Xenografts by the Novel Histone Deacetylase Inhibitor PXD101. Mol. Cancer. Ther., 2003, 2 (8), 721-728.
109. Steele, N. L.; Plumb, J. A.; Vidal, L.; Tjornelund, J.; Knoblauch, P.; Rasmussen, A.; Ooi, C. E.; Buhl-Jensen, P.; Brown, R.; Evans, T. R. J.; DeBono, J. S. A phase 1 pharmacokinetic and pharmacodynamic study of the histone deacetylase inhibitor belinostat in patients with advanced solid tumors. Clin. Cancer. Res., 2008, 14 (3), 804-10. (Pubitemid 351231163)
110. Ramalingam, S. S.; Belani, C. P.; Ruel, C.; Frankel, P.; Gitlitz, B.; Koczywas, M.; Espinoza-Delgado, I.; Gandara, D. Phase II Study of Belinostat (PXD101), a Histone Deacetylase Inhibitor, for Second Line Therapy of Advanced Malignant Pleural Mesothelioma. J. Thorac. Oncol., 2009, 4 (1), 97-101.
111. Mackay, H.; Hirte, H. W.; Covens, A.; MacAlpine, K.; Wang, L.; Tsao, M. S.; Pan, J.; Zwiebel, J. A.; Oza, A. M. A phase II trial of the histone deacetylase inhibitor belinostat (PXD101) in patients with platinum resistant epithelial ovarian tumors and micropapillary/borderline (LMP) ovarian tumors. A PMH phase II consortium trial. J. Clin. Oncol. (Meeting Abstracts)., 2008, 26 (15 suppl), 5518.
112. Giles, F.; Fischer, T.; Cortes, J.; Garcia-Manero, G.; Beck, J.; Ravandi, F.; Masson, E.; Rae, P.; Laird, G.; Sharma, S.; Kantarjian, H.; Dugan, M.; Albitar, M.; Bhalla, K. A Phase I Study of Intravenous LBH589, a Novel Cinnamic Hydroxamic Acid Analogue Histone Deacetylase Inhibitor, in Patients with Refractory Hematologic Malignancies. Clin. Cancer. Res., 2006, 12 (15), 4628-4635. (Pubitemid 44297814)
113. Atadja, P. Development of the pan-HDAC inhibitor panobinostat (LBH589): Successes and challenges. Cancer. Lett., 2009, 280 (2), 233-241.
114. Sandor, V.; Bakke, S.; Robey, R. W.; Kang, M. H.; Blagosklonny, M. V.; Bender, J.; Brooks, R.; Piekarz, R. L.; Tucker, E.; Figg, W. D.; Chan, K. K.; Goldspiel, B.; Fojo, A. T.; Balcerzak, S. P.; Bates, S. E. Phase I Trial of the Histone Deacetylase Inhibitor, Depsipeptide (FR901228, NSC 630176), in Patients with Refractory Neoplasms. Clin. Cancer. Res., 2002, 8 (3), 718-728. (Pubitemid 34742100)
115. Marshall, J. L.; Rizvi, N.; Kauh, J.; Dahut, W.; Figuera, M.; Kang, M. H.; Figg, W. D.; Wainer, I.; Chaissang, C.; Zhaoyang Li, M.; Hawkins, M. J. A phase I trial of Depsipeptide (FR901228) in patients with advanced cancer. J. Exp. Ther. Oncol., 2002, 2 (6), 325-332. (Pubitemid 35265981)
116. Piekarz, R. L.; Frye, R.; Turner, M.; Wright, J. J.; Allen, S. L.; Kirschbaum, M. H.; Zain, J.; Prince, H. M.; Leonard, J. P.; Geskin, L. J.; Reeder, C.; Joske, D.; Figg, W. D.; Gardner, E. R.; Steinberg, S. M.; Jaffe, E. S.; Stetler- Stevenson, M.; Lade, S.; Fojo, A. T.; Bates, S. E. Phase II Multi-Institutional Trial of the Histone Deacetylase Inhibitor Romidepsin As Monotherapy for Patients With Cutaneous T-Cell Lymphoma. J. Clin. Oncol., 2009, 27 (32), 5410-5417.
117. Demierre, M.; Whittaker, S.; Kim, Y.; Kim, E.; Piekarz, R.; Prince, M.; Nichols, J.; Balser, J.; Prentice, A.; Bates, S. Pooled analyses of two international, multicenter clinical studies of romidepsin in 167 patients with cutaneous T-cell lymphoma (CTCL). J. Clin. Oncol.(Meeting Abstracts)., 2009, 27 (15S), 8546.
118. US Food and Drug Administration -Centre for Drug Evaluation and Research. http://www.fda.gov/AboutFDA/CentersOffices/CDER/ucm189466. htm (Accessed 24th Septmber 2010).
119. Schrump, D. S.; Fischette, M. R.; Nguyen, D. M.; Zhao, M.; Li, X.; Kunst, T. F.; Hancox, A.; Hong, J. A.; Chen, G. A.; Kruchin, E.; Wright, J. J.; Rosing, D. R.; Sparreboom, A.; Figg, W. D.; Steinberg, S. M. Clinical and Molecular Responses in Lung Cancer Patients Receiving Romidepsin. Clin. Cancer. Res., 2008, 14 (1), 188-198. (Pubitemid 351377995)
120. Stadler, W. M.; Margolin, K.; Ferber, S.; McCulloch, W.; Thompson, J. A. A phase II study of depsipeptide in refractory metastatic renal cell cancer. Clin. Genitourin. Cancer 2006, 5, 57-60.
121. Molife, L. R.; Attard, G.; Fong, P. C.; Karavasilis, V.; Reid, A. H. M.; Patterson, S.; Riggs, C. E.; Higano, C.; Stadler, W. M.; McCulloch, W.; Dearnaley, D.; Parker, C.; de Bono, J. S. Phase II, two-stage, single-arm trial of the histone deacetylase inhibitor (HDACi) romidepsin in metastatic castration-resistant prostate cancer (CRPC). Ann. Oncol., 2010, 21 (1), 109-113.
122. Saito, A.; Yamashita, T.; Mariko, Y.; Nosaka, Y.; Tsuchiya, K.; Ando, T.; Suzuki, T.; Tsuruo, T.; Nakanishi, O. A synthetic inhibitor of histone deacetylase, MS-27-275, with marked in vivo antitumor activity against human tumors. Proc. Natl. Acad. Sci. U S A., 1999, 96 (8), 4592-4597. (Pubitemid 29190381)
123. Gore, L.; Rothenberg, M. L.; O'Bryant, C. L.; Schultz, M. K.; Sandler, A. B.; Coffin, D.; McCoy, C.; Schott, A.; Scholz, C.; Eckhardt, S. G. A Phase I and Pharmacokinetic Study of the Oral Histone Deacetylase Inhibitor, MS-275, in Patients with Refractory Solid Tumors and Lymphomas. Clin. Cancer. Res., 2008, 14 (14), 4517-4525.
124. Ryan, Q. C.; Headlee, D.; Acharya, M.; Sparreboom, A.; Trepel, J. B.; Ye, J.; Figg, W. D.; Hwang, K.; Chung, E. J.; Murgo, A.; Melillo, G.; Elsayed, Y.; Monga, M.; Kalnitskiy, M.; Zwiebel, J.; Sausville, E. A. Phase I and Pharmacokinetic Study of MS-275, a Histone Deacetylase Inhibitor, in Patients With Advanced and Refractory Solid Tumors or Lymphoma. J. Clin. Oncol., 2005, 23 (17), 3912-3922. (Pubitemid 46218694)
125. Siu, L. L.; Pili, R.; Duran, I.; Messersmith, W. A.; Chen, E. X.; Sullivan, R.; MacLean, M.; King, S.; Brown, S.; Reid, G. K.; Li, Z.; Kalita, A. M.; Laille, E. J.; Besterman, J. M.; Martell, R. E.; Carducci, M. A. Phase I study of MGCD0103 given as a three-times-per-week oral dose in patients with advanced solid tumors. J. Clin. Oncol., 2008, 26 (12), 1940-7.
126. Hurwitz, H.; Nelson, B.; O'Dwyer, P. J.; Chiorean, E. G.; Gabrail, N.; Li, Z.; Laille, E.; Drouin, M.; Rothenberg, M. L.; Chan, E. Phase I/II: The oral isotype-selective HDAC inhibitor MGCD0103 in combination with gemcitabine (Gem) in patients (pts) with refractory solid tumors. J. Clin. Oncol. (Meeting Abstracts)., 2008, 26 (15-suppl), 4625.
127. Atmaca, A.; Al-Batran, S. E.; Maurer, A.; Neumann, A.; Heinzel, T.; Hentsch, B.; Schwarz, S. E.; Hovelmann, S.; Gottlicher, M.; Knuth, A.; Jager, E. Valproic acid (VPA) in patients with refractory advanced cancer: a dose escalating phase I clinical trial. Br. J. Cancer., 2007, 97 (2), 177-182. (Pubitemid 47057472)
128. Rocca, A.; Minucci, S.; Tosti, G.; Croci, D.; Contegno, F.; Ballarini, M.; Nole, F.; Munzone, E.; Salmaggi, A.; Goldhirsch, A.; Pelicci, P. G.; Testori, A. A phase I-II study of the histone deacetylase inhibitor valproic acid plus chemoimmunotherapy in patients with advanced melanoma. Br. J. Cancer., 2009, 100 (1), 28-36.
129. Nolan, L.; Johnson, P. W. M.; Ganesan, A.; Packham, G.; Crabb, S. J. Will histone deacetylase inhibitors require combination with other agents to fulfil their therapeutic potential[quest] Br. J. Cancer., 2008, 99 (5), 689-694.
130. Bali, P.; Pranpat, M.; Swaby, R.; Fiskus, W.; Yamaguchi, H.; Balasis, M.; Rocha, K.; Wang, H.-G.; Richon, V.; Bhalla, K. Activity of Suberoylanilide Hydroxamic Acid Against Human Breast Cancer Cells with Amplification of Her-2. Clin. Cancer. Res., 2005, 11 (17), 6382-6389. (Pubitemid 41262970)
131. Bots, M.; Johnstone, R. W. Rational Combinations Using HDAC Inhibitors. Clin. Cancer. Res., 2009, 15 (12), 3970-3977.
132. Shah, M. H.; Binkley, P.; Chan, K.; Xiao, J.; Arbogast, D.; Collamore, M.; Farra, Y.; Young, D.; Grever, M. Cardiotoxicity of Histone Deacetylase Inhibitor Depsipeptide in Patients with Metastatic Neuroendocrine Tumors. Clin. Cancer. Res., 2006, 12 (13), 3997-4003. (Pubitemid 44078086)
133. Piekarz, R. L.; Frye, A. R.; Wright, J. J.; Steinberg, S. M.; Liewehr, D. J.; Rosing, D. R.; Sachdev, V.; Fojo, T.; Bates, S. E. Cardiac Studies in Patients Treated with Depsipeptide, FK228, in a Phase II Trial for T-Cell Lymphoma. Clin. Cancer. Res., 2006, 12 (12), 3762-3773. (Pubitemid 44000258)
134. Strevel, E. L.; Ing, D. J.; Siu, L. L. Molecularly Targeted Oncology Therapeutics and Prolongation of the QT Interval. J. Clin. Oncol., 2007, 25 (22), 3362-3371. (Pubitemid 47325624)
135. Wood, A. J. J.; Roden, D. M. Drug-Induced Prolongation of the QT Interval. N. Engl. J. Med., 2004, 350 (10), 1013-1022. (Pubitemid 38269278)
136. Ritchie, D.; Piekarz, R. L.; Blombery, P.; Karai, L. J.; Pittaluga, S.; Jaffe, E. S.; Raffeld, M.; Janik, J. E.; Prince, H. M.; Bates, S. E. Reactivation of DNA viruses in association with histone deacetylase inhibitor therapy: a case series report. Haematologica., 2009, 94 (11), 1618-1622.
137. Contreras, X.; Schweneker, M.; Chen, C.-S.; McCune, J. M.; Deeks, S. G.; Martin, J.; Peterlin, B. M. Suberoylanilide Hydroxamic Acid Reactivates HIV from Latently Infected Cells. J. Bio. Chem., 2009, 284 (11), 6782-6789.
138. Steele, N. L.; Plumb, J. A.; Vidal, L.; Tjornelund, J.; Knoblauch, P.; Rasmussen, A.; Ooi, C. E.; Buhl-Jensen, P.; Brown, R.; Evans, T. R. J.; DeBono, J. S. A Phase 1 Pharmacokinetic and Pharmacodynamic Study of the Histone Deacetylase Inhibitor Belinostat in Patients with Advanced Solid Tumors. Clin. Cancer. Res., 2008, 14 (3), 804-810. (Pubitemid 351231163)
139. Fotheringham, S.; Epping, M. T.; Stimson, L.; Khan, O.; Wood, V.; Pezzella, F.; Bernards, R.; La Thangue, N. B. Genome-wide Loss-of-Function Screen Reveals an Important Role for the Proteasome in HDAC Inhibitor-Induced Apoptosis. Cancer cell., 2009, 15 (1), 57-66.
140. Fantin, V. R.; Richon, V. M. Mechanisms of resistance to histone deacetylase inhibitors and their therapeutic implications. Clin. Cancer. Res., 2007, 13, 7237-7242.
141. Atadja, P.; Gao, L.; Kwon, P.; Trogani, N.; Walker, H.; Hsu, M.; Yeleswarapu, L.; Chandramouli, N.; Perez, L.; Versace, R.; Wu, A.; Sambucetti, L.; Lassota, P.; Cohen, D.; Bair, K.; Wood, A.; Remiszewski, S. Selective Growth Inhibition of Tumor Cells by a Novel Histone Deacetylase Inhibitor, NVP-LAQ824. Cancer. Res., 2004, 64 (2), 689-695. (Pubitemid 38120911)
142. Arts, J.; King, P.; Marian, A.; Floren, W.; Belian, A.; Janssen, L.; Pilatte, I.; Roux, B.; Decrane, L.; Gilissen, R.; Hickson, I.; Vreys, V.; Cox, E.; Bol, K.; Talloen, W.; Goris, I.; Andries, L.; Du Jardin, M.; Janicot, M.; Page, M.; van Emelen, K.; Angibaud, P. JNJ-26481585, a Novel "Second-Generation" Oral Histone Deacetylase Inhibitor, Shows Broad-Spectrum Preclinical Antitumoral Activity. Clin. Cancer. Res., 2009, 15 (22), 6841-6851.
143. Wang, H.; Dymock, B. W. New patented histone deacetylase inhibitors. Expert Opin. Ther. Patents., 2009, 19 (12), 1727-1757.
144. Ryan, Q. C.; Headlee, D.; Acharya, M.; Sparreboom, A.; Trepel, J. B.; Ye, J.; Figg, W. D.; Hwang, K.; Chung, E. J.; Murgo, A.; Melillo, G.; Elsayed, Y.; Monga, M.; Kalnitskiy, M.; Zwiebel, J.; Sausville, E. A. Phase I and Pharmacokinetic Study of MS-275, a Histone Deacetylase Inhibitor, in Patients With Advanced and Refractory Solid Tumors or Lymphoma. J. Clin. Oncol., 2005, 23 (17), 3912-3922. (Pubitemid 46218694)
145. Crump, M.; Coiffier, B.; Jacobsen, E. D.; Sun, L.; Ricker, J. L.; Xie, H.; Frankel, S. R.; Randolph, S. S.; Cheson, B. D. Phase II trial of oral vorinostat (suberoylanilide hydroxamic acid) in relapsed diffuse large-B-cell lymphoma. Ann. Oncol., 2008, 19 (5), 964-969. (Pubitemid 351627315)
146. Ramalingam, S. S.; Parise, R. A.; Ramananthan, R. K.; Lagattuta, T. F.; Musguire, L. A.; Stoller, R. G.; Potter, D. M.; Argiris, A. E.; Zwiebel, J. A.; Egorin, M. J.; Belani, C. P. Phase I and Pharmacokinetic Study of Vorinostat, A Histone Deacetylase Inhibitor, in Combination with Carboplatin and Paclitaxel for Advanced Solid Malignancies. Clin. Cancer. Res., 2007, 13 (12), 3605-3610. (Pubitemid 46955122)
147. Fakih, M. G.; Pendyala, L.; Fetterly, G.; Toth, K.; Zwiebel, J. A.; Espinoza- Delgado, I. A phase I, pharmacokinetic and pharmacodynamic study on vorinostat in combination with 5-fluorouracil, leucovorin, and oxaliplatin inpatients with refractory colorectal cancer. Clin. Cancer. Res., 2009, 15, 3189-3195.
148. Munster, P. N.; Lacevic, M.; Schmitt, M.; Bicaku, E.; Marchion, D.; Stephens, A.; Sullivan, L.; Minton, S. Phase II trial of vorinostat, a histone deacetylase inhibitor to restore the hormone sensitivity to the anti-estrogen tamoxifen in patients with advanced breast cancer having failed prior aromatase inhibitor therapy. J. Clin. Oncol.(Meeting Abstracts)., 2008, 26 (15 suppl), 3501.
149. Lassen, U.; Molife, L. R.; Sorensen, M.; Engelholm, S. A.; Vidal, L.; Sinha, R.; Penson, R. T.; Buhl-Jensen, P.; Crowley, E.; Tjornelund, J.; Knoblauch, P.; de Bono, J. S. A phase I study of the safety and pharmacokinetics of the histone deacetylase inhibitor belinostat administered in combination with carboplatin and/or paclitaxel in patients with solid tumours. Br. J. Cancer., 2010, 103 (1), 12-7.
150. Rathkopf, D. E.; Wong, B. Y.; Ross, R. W.; George, D. J.; Picus, J.; Tanaka, E.; Chen, Y.; Atadja, P.; Yang, W.; Culver, K. W.; Scher, H. I. A phase I study of oral panobinostat (LBH589) alone and in combination with docetaxel (Doc) and prednisone in castration-resistant prostate cancer (CRPC). J. Clin. Oncol. (Meeting Abstracts)., 2008, 26 (15 suppl), 5152.
151. Munster, P.; Marchion, D.; Bicaku, E.; Lacevic, M.; Kim, J.; Centeno, B.; Daud, A.; Neuger, A.; Minton, S.; Sullivan, D. Clinical and biological effects of valproic acid as a histone deacetylase inhibitor on tumor and surrogate tissues: phase I/II trial of valproic acid and epirubicin/FEC. Clin. Cancer. Res., 2009, 15 (7), 2488-96.