A review of depsipeptide and other histone deacetylase inhibitors in clinical trials

Current Pharmaceutical Design

Volumn 10, Issue 19, 2004, Pages 2289-2298

  Piekarz, Richard ^a   Bates, Susan ^a,b  

^a NATIONAL CANCER INSTITUTE   (United States)

^b NONE   (United States)

Author keywords

Histone deacetylase inhibitors

Indexed keywords

4 [N (2 HYDROXYETHYL) N [2 (3 INDOLYL)ETHYL]AMINOMETHYL]CINNAMOHYDROXAMIC ACID; 4 N ACETYLDINALINE; ANTINEOPLASTIC AGENT; ARGININE BUTYRATE; BENZAMIDE DERIVATIVE; BUTYRIC ACID; BUTYRIC ACID DERIVATIVE; CAPECITABINE; CARBOPLATIN; DECITIBINE; DEPSIPEPTIDE; FLAVOPIRIDOL; FR 901228; GEMCITABINE; HISTONE DEACETYLASE INHIBITOR; HYDROXAMIC ACID DERIVATIVE; ISOBUTYRAMIDE; METHYLTRANSFERASE INHIBITOR; N (2 AMINOPHENYL) 4 (3 PYRIDINYLMETHOXYCARBONYLAMINOMETHYL)BENZAMIDE; PACLITAXEL; PHENYLACETIC ACID; PHENYLBUTYRATE; PIVALOYLOXYMETHYL BUTYRATE; RETINOIC ACID; SHORT CHAIN FATTY ACID; TRIBUTYRIN; TRICHOSTATIN A; UNCLASSIFIED DRUG; UNINDEXED DRUG; VALPROIC ACID; VORINOSTAT;

ABDOMINAL CRAMP; ANEMIA; ANOREXIA; ANTINEOPLASTIC ACTIVITY; ANXIETY DISORDER; BONE MARROW SUPPRESSION; CANCER; CANCER COMBINATION CHEMOTHERAPY; CARDIOTOXICITY; CELL DEATH; CELL DIFFERENTIATION; CELL GROWTH; CELL PROLIFERATION; CELL TRANSFORMATION; CENTRAL NERVOUS SYSTEM DISEASE; CLINICAL TRIAL; CONFUSION; DIARRHEA; DISEASE MARKER; DISORIENTATION; DRUG ACTIVITY; DRUG BLOOD LEVEL; DRUG EFFECT; DRUG EFFICACY; DRUG HALF LIFE; DRUG MECHANISM; DRUG POTENTIATION; DRUG SPECIFICITY; DRUG STRUCTURE; DYSGEUSIA; DYSPEPSIA; EMOTIONAL DISORDER; EVIDENCE BASED MEDICINE; FATIGUE; FEVER; GENE EXPRESSION REGULATION; HEADACHE; HEART ATRIUM FIBRILLATION; HUMAN; HYPERGLYCEMIA; HYPERURICEMIA; HYPOALBUMINEMIA; HYPOCALCEMIA; HYPOKALEMIA; HYPONATREMIA; HYPOPHOSPHATEMIA; LABORATORY TEST; LETHARGY; LEUKOPENIA; LIVER TOXICITY; MOLECULAR DYNAMICS; MYALGIA; NAUSEA; NEUTROPENIA; NONHUMAN; PLEURA EFFUSION; PRIORITY JOURNAL; PROTEINURIA; RESPIRATORY DISTRESS SYNDROME; REVIEW; SOMNOLENCE; T CELL LYMPHOMA; TASTE DISORDER; THROMBOCYTOPENIA; THROMBOSIS; VOMITING;

ANTINEOPLASTIC AGENTS; ANTINEOPLASTIC COMBINED CHEMOTHERAPY PROTOCOLS; CLINICAL TRIALS; DEPSIPEPTIDES; HISTONE DEACETYLASES; HUMANS; PEPTIDES, CYCLIC;

EID: 3042785975     PISSN: 13816128     EISSN: None     Source Type: Journal    
DOI: 10.2174/1381612043383980     Document Type: Review

References (105)

1. Allfrey VG, Faulkner R, Mirsky AE. Acetylation and methylation of histories and their possible role in the regulation of RNA synthesis. Proc Natl Acad Sci USA 1964; 51: 786-794.
2. Gu W, Roeder RG. Activation of p53 sequence-specific DNA binding by acetylation of the p53 C-terminal domain. Cell 1997; 90: 595-606.
3. Brooks CL, Gu W. Ubiquitination, phosphorylation and acetylation: the molecular basis for p53 regulation. Current Opinion in Cell Biology 2003; 15: 164-71.
4. Marks PA, Rifkind RA, Richon VM, Breslow R, Miller T, Kelly WK. Histone deacetylases and cancer: Causes and therapies. Nat Rev Cancer 2001; 1: 194-202.
5. de Ruijter AJ, van Gennip AH, Caron HN, Kemp S, van Kuilenburg AB. Historic deacetylases (HDACs): characterization of the classical HDAC family. Biochem J 2003; 370: 737-49.
6. Thiagalingam S, Cheng KH, Lee HJ, Mineva N, Thiagalingam A, Ponte JF. Histone deacetylases: unique players in shaping the epigenetic histone code. Annals of the New York Academy of Sciences 2003; 983: 84-100.
7. Furumai R, Matsuyama A, Kobashi N, Lee KH, Nishiyama N, Nakajima I, et al. FK228 (depsipeptide) as a natural prodrug that inhibits class I histone deacetylases. Cancer Res 2002; 62: 4916-4921.
8. Schwer B, North BJ, Frye RA, Ott M, Verdin E. The human silent information regulator (Sir)2 homologue hSIRT3 is a mitochondrial nicotinamide adenine dinucleotide-dependent deacetylase. J Cell Biol 2002; 158: 647-57.
9. Wang J, Hoshino T, Redner RL, Kajigaya S, Liu JM. ETO, fusion partner in t(8;21) acute myeloid leukemia, represses transcription by interaction with the human N-CoR/mSin3/HDAC1 complex. Proc Natl Acad Sci USA 1998; 95: 10860-5.
10. Wang JX, Saunthararajah Y, Redner RL, Liu JM. Inhibitors of histone deacetylase relieve ETO-mediated repression and induce differentiation of AML1-ETO leukemia cells. Cancer Res 1999; 59: 2766-2769.
11. Klisovic MI, Maghraby EA, Parthun MR, Guimond M, Sklenar AR, Whitman SP, et al. Depsipeptide (FR 901228) promotes histone acetylation, gene transcription, apoptosis and its activity is enhanced by DNA methyltransferase inhibitors in AML1/ETO-positive leukemic cells. Leukemia 2003; 17: 350-8.
12. He LZ, Guidez F, Tribioli C, Peruzzi D, Ruthardt M, Zelent A, et al. Distinct interactions of PML-RARalpha and PLZF-RARalpha with co-repressors determine differential responses to RA in APL. Nature Genetics 1998; 18: 126-35.
13. Lin RJ, Nagy L, Inoue S, Shao W, Miller WH, Jr, Evans RM. Role of the histone deacetylase complex in acute promyelocytic leukaemia. Nature 1998; 391: 811-4.
14. Grignani F, De Matteis S, Nervi C, Tomassoni L, Gelmetti V, Cioce M, et al. Fusion proteins of the retinoic acid receptor-alpha recruit histone deacetylase in promyelocytic leukaemia. Nature 1998; 391: 815-8.
15. Coffey DC, Kutko MC, Glick RD, Butler LM, Heller G, Rifkind RA, et al. The histone deacetylase inhibitor, CBHA, inhibits growth of human neuroblastoma xenografts in vivo, alone and synergistically with all-trans retinoic acid. Cancer Res 2001; 61: 3591-3594.
16. He LZ, Tolentino T, Grayson P, Zhong S, Warrell RP, Rifkind RA, et al. Histone deacetylase inhibitors induce remission in transgenic models of therapy-resistant acute promyelocytic leukemia. J Clin Invest 2001; 108: 1321-1330.
17. Kosugi H, Ito M, Yamamoto Y, Towatari M, Ueda R, Saito H, et al. In vivo effects of a histone deacetylase inhibitor, FK228, on human acute promyelocytic leukemia in NOD/Shi-scid/scid mice. Jpn J Cancer Res 2001; 92: 529-536.
18. Ueda H, Nakajima H, Hori Y, Goto T, Okuhara M. Action of FR901228, a novel antitumor bicyclic depsipeptide produced by Chromobacterium violaceum no. 968, on Ha-ras transformed NIH3T3 cells. Biosci Biotechnol Biochem 1994; 58: 1579-83.
19. Ueda H, Manda T, Matsumoto S, Mukumoto S, Nishigaki F, Kawamura I, et al. FR901228, a novel antitumor bicyclic depsipeptide produced by Chromobacterium violaceum No. 968. III. Antitumor activities on experimental tumors in mice. J Antibiot (Tokyo) 1994; 47: 315-23.
20. Kitazono M, Robey R, Zhan ZR, Sarlis NJ, Skarulis MC, Aikou T, et al. Low concentrations of the histone deacetylase inhibitor, depsipeptide (FR901228), increase expression of the Na+/I-symporter and iodine accumulation in poorly differentiated thyroid carcinoma cells. J Clin Endocrinol Metab 2001; 86: 3430-3435.
21. Sandor V, Senderowicz A, Mertins S, Sackett D, Sausville E, Blagosklonny MV, et al. P21-dependent G(1) arrest with downregulation of cyclin D1 and upregulation of cyclin E by the histone deacetylase inhibitor FR901228. Br J Cancer 2000; 83: 817-825.
22. Finnin MS, Donigian JR, Cohen A, Richon VM, Rifkind RA, Marks PA, et al. Structures of a histone deacetylase homologue bound to the TSA and SAHA inhibitors. Nature 1999; 401: 188-93.
23. Sowa Y, Orita T, Hiranabe-Minamikawa S, Nakano K, Mizuno T, Nomura H, et al. Histone deacetylase inhibitor activates the p21/WAF1/Cip1 gene promoter through the Sp1 sites. Ann NY Acad Sci 1999; 886: 195-199.
24. Jin S K, Scotto KW. Transcriptional regulation of the MDR1 gene by histone acetyltransferase and deacetylase is mediated by NF-Y. Mol Cell Biol 1998; 18: 4377-4384.
25. Archer SY, Meng SF, Shei A, Hodin RA. p21(WAF1) is required for butyrate-mediated growth inhibition of human colon cancer cells. Proc Natl Acad Sci USA 1998; 95: 6791-6796.
26. Burgess AJ, Pavey S, Warrener R, Hunter LJK, Piva TJ, Musgrove EA, et al. Up-regulation of p21(WAF1)/(CIP1) by histone deacetylase inhibitors reduces their cytotoxicity. Mol Pharmacol 2001; 60: 828-837.
27. Qiu L, Burgess A, Fairlie DP, Leonard H, Parsons PG, Gabrielli BG. Histone deacetylase inhibitors trigger a G2 checkpoint in normal cells that is defective in tumor cells. Mol Biol Cell 2000; 11: 2069-+.
28. Sandor V, Robbins AR, Robey R, Myers T, Sausville E, Bates SE, et al. FR901228 causes mitotic arrest but does not alter microtubule polymerization. Anti-Cancer Drugs 2000; 11: 445-454.
29. Vrana JA, Decker RH, Johnson CR, Wang Z, Jarvis WD, Richon VM, et al. Induction of apoptosis in U937 human leukemia cells by suberoylanilide hydroxamic acid (SAHA) proceeds through pathways that are regulated by Bcl-2/Bcl-X-L, c-Jun, and p21(CIP1), but independent of p53. Oncogene 1999; 18: 7016-7025.
30. Kwon SH, Ahn SH, Kim YK, Bae GU, Yoon JW, Hong S, et al. Apicidin, a histone deacetylase inhibitor, induces apoptosis and Fas/Fas ligand expression in human acute promyelocytic leukemia cells. Journal of Biological Chemistry 2002; 277: 2073-80.
31. Yu XD, Guo ZS, Marcu MG, Neckers L, Nguyen DM, Chen GA, et al. Modulation of p53, ErbB1, FrbB2, and Raf-1 expression in lung cancer cells by depsipeptide FR901228. J Natl Cancer Inst 2002; 94: 504-513.
32. Donapaty S, Fuino L, Wittmann S, Nimmanapalli R, Bali P, Yamaguchi H, et al. Histone deacetylase inhibitor LAQ824 downregulates HER-2, induces growth arrest and apoptosis and sensitizes human breast cancer cells to herceptin and tubulin polymerizing agents. Proc Asco 2003; 22.
33. Nimmanapalli R, Fuino L, Bali P, Gasparetto M, Glozak M, Tao J, et al. Histone deacetylase inhibitor LAQ824 both lowers expression and promotes proteasomal degradation of Bcr-Abl and induces apoptosis of imatinib mesylate-sensitive or -refractory chronic myelogenous leukemia-blast crisis cells. Cancer Research 2003; 63: 5126-35.
34. Huang HC, Liu YC, Liu SH, Tzang BS, Lee WC. Geldanamycin inhibits trichostatin A-induced cell death and histone H4 hyperacelylation in COS-7 cells. Life Sciences 2002; 70: 1763-75.
35. Pei X, Dai Y, Grant S. The Proteasome Inhibitor Bortezomib Interacts Synergistically with Histone Deacetylase Inhibitors To Induce Apoptosis in Human Multiple Myeloma Cells. Blood 2003; 102: 685a.
36. Kim MS, Kwon HJ, Lee YM, Baek JH, Jang JE, Lee SW, et al. Histone deacetylases induce angiogenesis by negative regulation of tumor suppressor genes. Nat Med 2001; 7: 437-443.
37. Sasakawa Y, Naoe Y, Noto T, Inoue T, Sasakawa T, Matsuo M, et al. Antitumor efficacy of FK228, a novel histone deacetylase inhibitor, depends on the effect on expression of anglogenesis factors. Biochem Pharmacol 2003; 66: 897-906.
38. Gore SD, Carducci MA. Modifying histones to tame cancer: clinical development of sodium phenylbutyrate and other histone deacetylase inhibitors. Expert Opinion on Investigational Drugs 2000; 9: 2923-34.
39. Novogrodsky A, Dvir A, Ravid A, Shkolnik T, Stenzel KH, Rubin AL, et al. Effect of polar organic compounds on leukemic cells. Butyrate-induced partial remission of acute myelogenous leukemia in a child. Cancer 1983; 51: 9-14.
40. Miller AA, Kurschel E, Osieka R, Schmidt CG. Clinical pharmacology of sodium butyrate in patients with acute leukemia. European Journal of Cancer & Clinical Oncology 1987; 23: 1283-7.
41. Sanders DA, Arthur V, Tansan S, McCaffrey R, Faller DV, Foss F. Phase I clinical trial of the differentiation agent isobutyramide in patients with refractory neoplasms. Proc AACR 1995; 36: 215.
42. Domenica Cappellini M, Graziadei G, Ciceri L, Comino A, Bianchi P, Porcella A, et al. Oral isobutyramide therapy in patients with thalassemia intermedia: results of a phase II open study. Blood Cells, Molecules, & Diseases 2000; 26: 105-11.
43. Sanders DA, Tansan S, Arthur V, Faller DV, McCaffrey R, Foss F. Phase I clinical trial of arginine butyrate in patients with refractory neoplasms. Proc Am Soc Clin Oncol 1995; 14: 476.
44. Carducci MA, Gilbert J, Bowling MK, Noe D, Eisenberger MA, Sinibaldi V, et al. A phase I clinical and pharmacological evaluation of sodium phenylbutyrate on an 120-h infusion schedule. Clin Cancer Res 2001; 7: 3047-3055.
45. Gilbert J, Baker SD, Bowling MK, Grochow L, Figg WD, Zabelina Y, et al. A phase I dose escalation and bioavailability study of oral sodium phenylbutyrate in patients with refractory solid tumor malignancies. Clinical Cancer Research 2001; 7: 2292-300.
46. Gore SD, Weng LJ, Zhai S, Figg WD, Donehower RC, Dover GJ, et al. Impact of the putative differentiating agent sodium phenylbutyrate on myelodysplastic syndromes and acute myeloid leukemia. Clinical Cancer Research 2001; 7: 2330-9.
47. Gore SD, Weng LJ, Figg WD, Zhai S, Donehower RC, Dover G, et al. Impact of prolonged infusions of the putative differentiating agent sodium phenylbutyrate on myelodysplastic syndromes and acute myeloid leukemia. Clinical Cancer Research 2002; 8: 963-70.
48. Conley BA, Egorin MJ, Tait N, Rosen DM, Sausville EA, Dover G, et al. Phase I study of the orally administered butyrate prodrug, tributyrin, in patients with solid tumors. Clinical Cancer Research 1998; 4: 629-34.
49. Edelman MJ, Bauer K, Khanwani S, Tait N, Trepel J, Karp J, et al. Clinical and pharmacologic study of tributyrin: an oral butyrate prodrug. Cancer Chemotherapy & Pharmacology 2003; 51: 439-44.
50. Patnaik A, Rowinsky EK, Villalona MA, Hammond LA, Britten CD, Siu LL, et al. A phase I study of pivaloyloxymethyl butyrate, a prodrug of the differentiating agent butyric acid, in patients with advanced solid malignancies. Clinical Cancer Research 2002; 8: 2142-8.
51. Luger SM, Bagg A, Stadtmauer EA, Porter DL, Cherian S, Gurvich N, et al. Pilot study of valproic acid in patients with myelodysplasia. Blood 2003; 102: 334b.
52. Kuendgen AM, Strupp C, Tapprich C, Hildebrandt B, Habersang K, Junge B, et al. Valproic acid alone or in combination with all-trans-retinoic acid (ATRA) for the treatment of myelodysplastic syndromes and sAML/MDS. Blood 2003; 102: 428a.
53. 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 Biol Chem 1990; 265: 17174-9.
54. Richon VM, Webb Y, Merger R. Sheppard T, Jursic B, Ngo L, et al. Second generation hybrid polar compounds are potent inducers of transformed cell differentiation. Proceedings of the National Academy of Sciences of the United States of America 1996; 93: 5705-8.
55. Kelly WK, Richon VM, O'Connor O, Curley T, MacGregor-Curtelli B, Tong W, et al. Phase I clinical trial of histone deacetylase inhibitor: Suberoylanilide hydroxamic acid administered intravenously. Clin Cancer Res 2003; 9: 3578-3588.
56. Garci-Manero G, Cannalli AA, Wierda W, Cortes J, O'Brien S, Cupo A, et al. Phase I study of oral suberoylanilide hydroxamic acid (SAHA) in patients with advanced leukemias or myelodysplastic syndrome. Blood 2003; 102: 254b.
57. LoRusso PM, Wozniak A, Foster B, Zalupski M, Shields AF. Phase I clinical trial of C1994. Proc Am Soc Clin Oncol 1997; 16: 213a.
58. Wozniak A, O'Shaughnessy J, Fiorica J, Grove W. Phase II trial of CI-994 in patients with advanced nonsmall cell lung cancer. Proc Am Soc Clin Oncol 1999; 16: 1878.
59. O'Shaughnessy J, Flaherty L, Fiorica J, Grove W. Phase II trial of CI-994 in patients with metastatic renal cell carcinoma. Proc ASCO 1999; 18.
60. Zalupski M, O'Shaughnessy J, Vukelja S, Shields AF, Diener K, Grove W. Phase II trial of CI-994 in patients with advanced pancreatic cancer. Proc ASCO 2000; 19.
61. Ryan QC, Headlee D, Sparreboom A, Figg WD, Zhai S, Trepel J, et al. A phase I trial of an oral histone deacetylase inhibitor, MS-275, in advanced solid tumors and lymphoma patients. Proc Am Soc Clin Oncol 2003; 22: 200.
62. Gojo I, Gore SD, Jiemjit A, Greer J, Tidwell M.L, Sparreboom A, et al. Phase I study of histone deacetylase inhibitor MS-275 in adults with refractory or relapsed hematologic malignancies. Blood 2003; 102: 388a.
63. Nakajima, H., Kim, Y. B., Terano, H., Yoshida, M., Horinouchi, S. FR901228, a potent antitumor antibiotic, is a novel histone deacetylase inhibitor. Exp Cell Res 1998; 241: 126-33.
64. Sandor V, Bakke S, Robey RW, Kang MH, Blagosklonny MV, Bender J, et al. Phase I trial of the histone deacetylase inhibitor, depsipeptide (FR901228, NSC 630176), in patients with refractory neoplasms. Clin Cancer Res 2002; 8: 718-728.
65. Marshall JL, Rizvi N, Kauh J, Dahut W, Figuera M, Kang MH, et al. A phase I trial of depsipeptide (FR901228) in patients with advanced cancer. Journal of Experimental Therapeutics & Oncology 2002; 2: 325-32.
66. Byrd JC, Shinn C, Ravi R, Willis CR, Waselenko JK, Flinn I.W, et al. Depsipeptide (FR901228): a novel therapeutic agent with selective, in vitro activity against human B-cell chronic lymphocytic leukemia cells. Blood 1999; 94: 1401-8.
67. Piekarz RL, Jewell S, Bakke S, Cannon R, Wright J, Bates S. Cardiac effecs of depsipeptide, FK228, in patients with T-cell lymphoma. Proc Am Soc Clin Oncol 2003; 22: 201.
68. Piekarz RL, Robey R, Sandor V, Bakke S, Wilson WH, Dahmoush L, et al. Inhibitor of histone deacetylation, depsipeptide (FR901228), in the treatment of peripheral and cutaneous T-cell lymphoma: a case report. Blood 2001; 98: 2865-2868.
69. Kraker AJ, Mizzen C, Pauer LR, Olson SC, Allis CD, Nemunaitis J. Modulation of histone acetylation in peripneral blood lymphocytes from patients with advanced solid tumors by CI-994 administered in combination with carboplatin and paclitaxel. Proc Asco 2002; 21.
70. Piekarz R, Robey R, Fojo A, Bakke S, Wilson W, Jaffe ES, et al. Analysis of molecular markers and targets in trials of depsipeptide, FR 901228, a histone deacetylase inhibitor with clinical activity in T-cell lymphoma. Proc Asco 2002; 21.
71. Piekarz RL, Robey R, Zhan ZR, Kayastha G, Bakke S, Fojo A, et al. Analysis of molecular markers and induction of molecular targets in clinical trials with histone deacetylase inhibitors. Proceedings of the AACR 2003; 44.
72. Odenike O, Alkan S, Godwin JE, Brandt SJ, Sher D, Stiff PJ, et al. Phase II study of the histone deacetylase inhibitor depsipeptide in patients with relapsed or refractory acute myeloid leukemia (AML). Blood 2003; 102: 241a.
73. Duvic M, Talpur R, Chiao N, Chiao J. Phase II Trial of Oral Suberoylanilide Hydroxamic Acid (SAHA) for Cutaneous T-Cell Lymphoma (CTCL) and Peripheral T-Cell Lymphoma (PTCL). Blood 2003; 102: 179a.
74. Tabe Y, Contractor R, Konopleva M, Igari J, Andreeff M. Combination of hetone deacetylase inhibitor depsipeptide (FK228) and ATRA enhances differentiation in ATRA-sensitive and - resistant APL cell lines. Blood 2003; 102: 258b.
75. Amin HM, Saeed S, Alkan S. Histone deacetylase inhibitors induce caspase-dependent apoptosis and downregulation of daxx in acute promyelocytic leukaemia with t(15;17). British Journal of Haematology 2001; 115: 287-97.
76. Petti MC, Fazi F, Gentile M, Diverio D, De Fabritiis P, De Propris MS, et al. Complete remission through blast cell differentiation in PLZF/RARalpha-positive acute promyelocytic leukemia: in vitro and in vivo studies. Blood 2002; 100: 1065-7.
77. Warrell RP, Jr, He LZ, Richon V, Calleja E, Pandolfi PP. Therapeutic targeting of transcription in acute promyelocytic leukemia by use of an inhibitor of histone deacetylase. [comment]. Journal of the National Cancer Institute 1998; 90: 1621-5.
78. Sidell N, Wada R, Han GY, Chang BS, Shack S, Moore T, et al. Phenylacetate Synergizes with Retinoic Acid in Inducing the Differentiation of Human Neuroblastoma-Cells. Int J Cancer 1995; 60: 507-514.
79. Yu KH, Weng LJ, Fu S, Piantadosi S, Gore SD. Augmentation of phenylbutyrate-induced differentiation of myeloid leukemia cells using all-trans retinoic acid. Leukemia 1999; 13: 1258-65.
80. Buommino E, Pasquali D, Sinisi AA, Bellastella A, Morelli F, Metafora S. Sodium butyrate/retinoic acid costimulation induces apoptosis- independent growth arrest and cell differentiation in normal and ras- transformed seminal vesicle epithelial cells unresponsive to retinoic acid. J Mol Endocrinol 2000; 24: 83-94.
81. Ferrara FF, Fazi F, Bianchini A, Padula F, Gelmetti V, Minucci S, et al. Histone deacetylase-targeted treatment restores retinoic acid signaling and differentiation in acute myeloid leukemia. Cancer Res 2001; 61: 2-7.
82. Roman-Gomez J, Castillejo JA, Jimenez A, Gonzalez MG, Moreno F, Rodriguez Mdel C, et al. 5′ CpG island hypermethylation is associated with transcriptional silencing of the p21(CIP1/WAF1/SDI1) gene and confers poor prognosis in acute lymphoblastic leukemia. [comment]. Blood 2002; 99: 2291-6.
83. Cameron EE, Bachman KE, Myohanen S, Herman JG, Baylin SB. Synergy of demethylation and histone deacetylase inhibition in the re-expression of genes silenced in cancer. Nature Genet 1999; 21: 103-107.
84. Zhu WG, Lakshmanan RR, Beal MD, Otterson GA. DNA methyltransferase inhibition enhances apoptosis induced by histone deacetylase inhibitors. Cancer Res 2001; 61: 1327-1333.
85. Cartee L, Wang Z, Decker RH, Chellappan SP, Fusaro G, Hirsch KG, et al. The cyclin-dependent kinase inhibitor (CDKI) flavopiridol disrupts phorbol 12-myristate 13-acetate-induced differentiation and CDKI expression while enhancing apoptosis in human myeloid leukemia cells. Cancer Research 2001; 61: 2583-91.
86. Rosato RR, Almenara JA, Cartee L, Betts V, Chellappan SP, Grant S. The cyclin-dependent kinase inhibitor flavopiridol disrupts sodium butyrate-induced p21(WAF1/CIP1) expression and maturation while reciprocally potentiating apoplosis in human leukemia cells. Mol Cancer Ther 2002; 1: 253-266.
87. Almenara J, Rosato R, Grant S. Synergistic induction of mitochondrial damage and apoptosis in human leukemia cells by flavopiridol and the histone deacetylase inhibitor suberoylanilide hydroxamic acid (SAHA). Leukemia 2002; 16: 1331-1343.
88. Nguyen DM, Schrump WD, Tsai WS, Chen A, Stewart JH, Steiner F, et al. Enhancement of depsipeptide-mediated apoptosis of lung or esophageal cancer cells by flavopiridol: Activation of the mitochondria-dependent death-signaling pathway. J Thorac Cardiovasc Surg 2003; 125: 1132-1142.
89. Urbano A, Koc Y, Foss FM. Arginine butyrate downregulates p210 bcr-abl expression and induces apoptosis in chronic myelogenous leukemia cells. Leukemia 1998; 12: 930-6.
90. Nimmanapalli R, Fuino L, Stobaugh C, Richon V, Bhalla K. Cotreatment with the histone deacetylase inhibitor suberoylanilide hydroxarmic acid (SAHA) enhances imatinib- induced apoptosis of Bcr-Abl-positive human acute leukemia cells. Blood 2003; 101: 3236-3239.
91. Yu C, Rahmani M, Almenara J, Subler M, Krystal G, Conrad D, et al. Histone deacetylase inhibitors promote STI571-mediated apoptosis in STI571-sensitive and -resistant Bcr/Abl+ human myeloid leukemia cells. Cancer Research 2003; 63: 2118-26.
92. Kim JS, Cheong JW, Maeng H, Lee ST, Min YH. Apicidin Potentiates the STI571-Induced Apoptosis of Bcr-Abl-Positive Human Leukemia Cells by Enhancing the Activation of Mitochondria-Dependent Caspase Cascades. Blood 2003; 102: 174b.
93. Yu X, Guo Z, Marcu MG, Neckers L, Chen G, Nguyen DM, et al. Depsipeptide-mediated apoptosis coincides with depletion of mutant p53, erbB1, erbB2, and raf-1 protein levels in lung cancer cells. Clin Cancer Res 2001; 7: 228.
94. Shack S, Miller A, Liu L, Prasanna P, Thibault A, Samid D. Vulnerability of multidrug-resistant tumor cells to the aromatic fatty acids phenylacetate and phenylbutyrate. Clinical Cancer Research 1996; 2: 865-72.
95. Conway RM, Madigan MC, Billson FA, Penfold PL. Vincristine- and cisplatin-induced apoptosis in human retinoblastoma. Potentiation by sodium butyrate. Eur J Cancer 1998; 34: 1741-1748.
96. Tsai SC, Valkov N, Yang WM, Gump J, Sullivan D, Seto E. Histone deacetylase interacts directly with DNA topoisomerase II. Nature Genet 2000; 26: 349-353.
97. Adachi N, Nomoto M, Kohno K, Koyama H. Cell-cycle regulation of the DNA topoisomerase II alpha promoter is mediated by proximal CCAAT boxes: possible involvement of acetylation. Gene 2000; 245: 49-57.
98. Niitsu N, Kasukabe T, Yokoyama A, Okabe-Kado J, Yamamoto-Yamaguchi Y, Umeda M, et al. Anticancer derivative of butyric acid (pivalyloxymethyl butyrate) specifically potentiates the cytotoxicity of doxorubicin and daunorubicin through the suppression of microsomal glycosidic activity. Mol Pharmacol 2000; 58: 27-36.
99. Johnson CA, Padget K, Austin CA, Turner BM. Deacetylase activity associates with topoisomerase II and is necessary for etoposide-induced apoptosis. J Biol Chem 2001; 276: 4539-4542.
100. Kurz EU, Wilson SE, Leader KB, Sampey BP, Allan WP, Yalowich JC, et al. The histone deacetylase inhibitor sodium butyrate induces DNA topoisomerase II alpha expression and confers hypersensitivity to etoposide in human leukemic cell lines. Mol Cancer Ther 2001; 1: 121-131.
101. Piekarz R, Robey R, Fojo A, Bakke S, Wilson W, Jaffe ES, et al. Analysis of molecular markers and targets in trials of depsipeptide, FR901228, a histone deacetylase inhibitor with clincal activity in T-cell lymphoma. Proc Asco 2002; 21.
102. Lee JS, Paull K, Alvarez M, Hose C, Monks A, Grever M, et al. Rhodamine efflux patterns predict P-glycoprotein substrates in the National Cancer Institute drug screen. Mol Pharmacol 1994; 46: 627-38.
103. Bleesing JJ. Autoimmune lymphoproliferative syndrome (ALPS). Curr Pharm. Design 2003; 9(3): 265-78.
104. Crump M. Inhibition of raf kinase in the treatment of acute myeloid leukemia. Curr Pharm Design 2002; 8(25): 2243-8.
105. Meisel H, FitzGerald RJ. Biofunctional peptides from milk proteins: mineral binding and cytomodulatory effects. Curr Pharm Design 2003; 9(16): 1289-95.