Rational development of histone deacetylase inhibitors as anticancer agents: A review

Molecular Pharmacology

Volumn 68, Issue 4, 2005, Pages 917-932

  Acharya, Milin R ^a,b   Sparreboom, Alex ^a   Venitz, Jürgen ^b   Figg, William D ^a  

^a NATIONAL CANCER INSTITUTE   (United States)

^b VIRGINIA COMMONWEALTH UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 [4 ( CYANOPHENYL)PENOXY]HEPTANOHYDROXAMIC ACID; 2 AMINO 9,10 EPOXY 8 OXODECANOIC ACID; 3 CARBOXYCINNAMIC ACID BISHYDROXAMIC ACID; 3 PHENYLSULFAMOYLCINNAMOHYDROXAMIC ACID; 4 [N (2 HYDROXYETHYL) N [2 (3 INDOLYL)ETHYL]AMINOMETHYL]CINNAMOHYDROXAMIC ACID; 4 N ACETYLDINALINE; 6 (3 CHLOROPHENYLUREIDO)CAPROIC HYDROXAMIC ACID; 7 [4 (4 CYANOPHENYL)PHENOXY]HEPTANOHYDROXAMIC ACID; ANTINEOPLASTIC AGENT; APICIDIN; ARYLBUTYRIC ACID DERIVATIVE; BUTYRIC ACID; CYCLOPEPTIDE; DEPUDECIN; ETOPOSIDE; FATTY ACID DERIVATIVE; FR 901228; HISTONE DEACETYLASE INHIBITOR; HYDROXAMIC ACID DERIVATIVE; JNJ 16241199; KETONE DERIVATIVE; N (2 AMINOPHENYL) 4 (3 PYRIDINYLMETHOXYCARBONYLAMINOMETHYL)BENZAMIDE; N HYDROXY 3 [3 [(PHENYLAMINO)SULFONYL]PHENYL] 2 PROPENAMIDE; N HYDROXY 3 [4 [[(2 HYDROXYETHYL)[2 (1H INDOL 3 YL)ETHYL]AMINO]METHYL] PHENYL] 2 PROPENAMIDE; OXAMFLATIN; PHENYLACETIC ACID; PIVALOYLOXYMETHYL BUTYRATE; PYROXAMIDE; SUBERIC BISHYDROXAMIC ACID; TETRAPEPTIDE; TRAPOXIN; TRICHOSTATIN A; UNCLASSIFIED DRUG; UNINDEXED DRUG; VALPROIC ACID; VORINOSTAT;

ACETYLATION; ANEMIA; ANOREXIA; ANTINEOPLASTIC ACTIVITY; ANXIETY; ASTHENIA; BRAIN HEMORRHAGE; CANCER; CANCER CELL; CELL CYCLE; CENTRAL NERVOUS SYSTEM DEPRESSION; CHROMATIN; CLASSIFICATION; CLINICAL TRIAL; CONCENTRATION RESPONSE; CONFUSION; CONSTITUTIONAL SYMPTOM; DEACETYLATION; DIARRHEA; DISORIENTATION; DNA METHYLATION; DRUG FEVER; DRUG INDUCED DISEASE; DRUG INDUCED HEADACHE; DRUG MECHANISM; DYSGEUSIA; DYSPEPSIA; ELECTROCARDIOGRAPHY; FATIGUE; GASTROINTESTINAL TOXICITY; GENE EXPRESSION; GENE EXPRESSION REGULATION; GENE LOCATION; GENE SILENCING; GENETIC TRANSCRIPTION; GENOME; GRANULOCYTOPENIA; HEART ARRHYTHMIA; HUMAN; HYPERAMMONEMIA; HYPERBILIRUBINEMIA; HYPOCALCEMIA; HYPOGLYCEMIA; HYPOKALEMIA; HYPONATREMIA; HYPOPHOSPHATEMIA; INFECTION COMPLICATION; LETHARGY; LIVER FUNCTION TEST; MALAISE; MUSCLE WEAKNESS; NAUSEA; NEUROCORTICAL NAUSEA; NEUROCORTICAL SOMNOLENCE; NEUROTOXICITY; NEUTROPENIA; NONHUMAN; PARESTHESIA; PRIORITY JOURNAL; PROTEIN FUNCTION; SHORT SURVEY; SIDE EFFECT; SLURRED SPEECH; SOMNOLENCE; THROMBOCYTOPENIA; TRANSIENT TRANSAMINITIS; TUMOR CELL; VISUAL DISORDER; VOMITING;

ANIMALS; ANTINEOPLASTIC AGENTS; DRUG DESIGN; ENZYME INHIBITORS; HISTONE DEACETYLASES; HUMANS;

EID: 25144440127     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.105.014167     Document Type: Short Survey

References (233)

1. Annunziato AT and Hansen JC (2000) Role of histone acetylation in the assembly and modulation of chromatin structures. Gene Expr 9:37-61.
2. Archer SY, Meng S, Shei A, and Hodin RA (1998) p21(WAF1) is required for butyrate-mediated growth inhibition of human colon cancer cells. Proc Natl Acad Sci USA 95:6791-6796.
3. Aron JL, Parthun MR, Marcucci G, Kitada S, Mone AP, Davis ME, Shen T, Murphy T, Wickham J, Kanakry C, et al. (2003) Depsipeptide (FR901228) induces histone acetylation and inhibition of histone deacetylase in chronic lymphocytic leukemia cells concurrent with activation of caspase 8-mediated apoptosis and downregulation of c-FLIP protein. Blood 102:652-658.
4. Arts J, de Schepper S, and Van Emelen K (2003) Histone deacetylase inhibitors: from chromatin remodeling to experimental cancer therapeutics. Curr Med Chem 10:2343-2350.
5. Atadja P, Gao L, Kwon P, Trogani N, Walker H, Hsu M, Yeleswarapu L, Chandramouli N, Perez L, Versace R, et al. (2004a) Selective growth inhibition of tumor cells by a novel histone deacetylase inhibitor, NVP-LAQ824. Cancer Res 64:689-695.
6. Atadja P, Hsu M, Kwon P, Trogani N, Bhalla K, and Remiszewski S (2004b) Molecular and cellular basis for the anti-proliferative effects of the HDAC inhibitor LAQ824. Novartis Found Symp 259:249-266; discussion 266-8, 285-8.
7. Atmaca AM, Heinzel T, Göttlicher M, Neumann A, Al-Batran S-E, Martin E, Bartsch I, Knuth A, and Jaeger E (2004) A dose-escalating phase I study with valproic acid (VPA) in patients (pts) with advanced cancer. J Clin Oncol 22 (14 Suppl):Abstract 3169.
8. Bali P, George P, Cohen P, Tao J, Guo F, Sigua C, Vishvanath A, Scuto A, Annavarapu S, Fiskus W, et al. (2004) Superior activity of the combination of histone deacetylase inhibitor LAQ824 and the FLT-3 kinase inhibitor PKC412 against human acute myelogenous leukemia cells with mutant FLT-3. Clin Cancer Res 10:4991-4997.
9. Batova A, Shao LE, Diccianni MB, Yu AL, Tanaka T, Rephaeli A, Nudelman A, and Yu J (2002) The histone deacetylase inhibitor AN-9 has selective toxicity to acute leukemia and drug-resistant primary leukemia and cancer cell lines. Blood 100:3319-3324.
10. Baylin SB, Esteller M, Rountree MR, Bachman KE, Schuebel K, and Herman JG (2001) Aberrant patterns of DNA methylation, chromatin formation and gene expression in cancer. Hum Mol Genet 10:687-692.
11. Beck J, Fischer T, Rowinsky E, Huber C, Mita M, Atadja P, Peng B, Kwong C, Dugan M, and Patnaik A (2004) Phase I pharmacokinetic (PK) and pharmacodynamic (PD) study of LBH589A: a novel histone deacetylase inhibitor. J Clin Oncol 22 (14 Suppl):Abstract 3025.
12. Belinsky SA, Klinge DM, Stidley CA, Issa JP, Herman JG, March TH, and Baylin SB (2003) Inhibition of DNA methylation and histone deacetylation prevents murine lung cancer. Cancer Res 63:7089-7093.
13. Bernhard D, Ausserlechner MJ, Tonko M, Loffler M, Hartmann BL, Csordas A, and Kofler R (1999) Apoptosis induced by the histone deacetylase inhibitor sodium butyrate in human leukemic lymphoblasts. FASEB J 13:1991-2001.
14. Bhalla K and List A (2004) Histone deacetylase inhibitors in myelodysplastic syndrome. Best Pract Res Clin Haematol 17:595-611.
15. Blagosklonny MV, Robey R, Sackett DL, Du L, Traganos F, Darzynkiewicz Z, Fojo T, and Bates SE (2002) Histone deacetylase inhibitors all induce p21 but differentially cause tubulin acetylation, mitotic arrest and cytotoxicity. Mol Cancer Ther 1:937-941.
16. Blumenschein G, Lu C, Kies M, Glisson B, Papadimitrakopoulou V, Zinner R, Kim E, Gillenwater A, Chiao J, and W Hong (2004) Phase II clinical trial of suberoylanilide hydroxamic acid (SAHA) in patients (pts) with recurrent and/or metastatic head and neck cancer(SCCHN). J Clin Oncol 22 (14 Suppl):Abstract 5578.
17. Bouchain G and Delorme D (2003) Novel hydroxamate and anilide derivatives as potent histone deacetylase inhibitors: synthesis and antiproliferative evaluation. Curr Med Chem 10:2359-2372.
18. Bouchain G, Leit S, Frechette S, Khalil EA, Lavoie R, Moradei O, Woo SH, Fournel M, Yan PT, Kalita A, et al. (2003) Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors. J Med Chem 46:820-830.
19. Butler LM, Agus DB, Scher HI, Higgins B, Rose A, Cordon-Cardo C, Thaler HT, Rifkind RA, Marks PA, and Richon VM (2000) Suberoylanilide hydroxamic acid, an inhibitor of histone deacetylase, suppresses the growth of prostate cancer cells in vitro and in vivo. Cancer Res 60:5165-5170.
20. Butler LM, Webb Y, Agus DB, Higgins B, Tolentino TR, Kutko MC, LaQuaglia MP, Drobnjak M, Cordon-Cardo C, Scher HI, et al. (2001) Inhibition of transformed cell growth and induction of cellular differentiation by pyroxamide, an inhibitor of histone deacetylase. Clin Cancer Res 7:962-970.
21. Butler LM, Zhou X, Xu WS, Scher HI, Rifkind RA, Marks PA, and Richon VM (2002) The histone deacetylase inhibitor SAHA arrests cancer cell growth, up-regulates thioredoxin-binding protein-2 and down-regulates thioredoxin. Proc Natl Acad Sci USA 99:11700-11705.
22. Byrd JC, Marcucci G, Parthun MR, Xiao JJ, Klisovic RB, Moran M, Lin TS, Liu S, Sklenar AR, Davis ME, et al. (2004) A phase I and pharmacodynamic study of depsipeptide (FK228) in chronic lymphocytic leukemia and acute myeloid leukemia. Blood 105:959-967.
23. Byrd JC, Shinn C, Ravi R, Willis CR, Waselenko JK, Flinn IW, Dawson NA, and Grever MR (1999) Depsipeptide (FR901228): a novel therapeutic agent with selective, in vitro activity against human B-cell chronic lymphocytic leukemia cells. Blood 94:1401-1408.
24. Cameron EE, Bachman KE, Myohanen S, Herman JG, and Baylin SB (1999) Synergy of demethylation and histone deacetylase inhibition in the re-expression of genes silenced in cancer. Nat Genet 21:103-107.
25. Carducci MA, Gilbert J, Bowling MK, Noe D, Eisenberger MA, Sinibaldi V, Zabelina Y, Chen TL, Grochow LB, and Donehower RC (2001) A phase I clinical and pharmacological evaluation of sodium phenylbutyrate on an 120-h infusion schedule. Clin Cancer Res 7:3047-3055.
26. Carducci MA, Nelson JB, Chan-Tack KM, Ayyagari SR, Sweatt WH, Campbell PA, Nelson WG, and Simons JW (1996) Phenylbutyrate induces apoptosis in human prostate cancer and is more potent than phenylacetate. Clin Cancer Res 2:379-387.
27. Catley L, Weisberg E, Tai YT, Atadja P, Remiszewski S, Hideshima T, Mitsiades N, Shringarpure R, LeBlanc R, Chauhan D, et al. (2003) NVP-LAQ824 is a potent novel histone deacetylase inhibitor with significant activity against multiple myeloma. Blood 102:2615-2622.
28. Chai F, Evdokiou A, Young GP, and Zalewski PD (2000) Involvement of p21(Waf1/Cip1) and its cleavage by DEVD-caspase during apoptosis of colorectal cancer cells induced by butyrate. Carcinogenesis 21:7-14.
29. Chang SM, Kuhn JG, Ian Robins H, Clifford Schold S, Spence AM, Berger MS, Mehta MP, Pollack I, Gilbert M, and Prados MD (2003) A study of a different dose-intense infusion schedule of phenylacetate in patients with recurrent primary brain tumors consortium report. Investig New Drugs 21:429-433.
30. Chang SM, Kuhn JG, Robins HI, Schold SC, Spence AM, Berger MS, Mehta MP, Bozik ME, Pollack I, Schiff D, et al. (1999) Phase II study of phenylacetate in patients with recurrent malignant glioma: a North American Brain Tumor Consortium report. J Clin Oncol 17:984-990.
31. Chen H, Tini M, and Evans RM (2001) HATs on and beyond chromatin. Curr Opin Cell Biol 13:218-224.
32. Cheng HL, Mostoslavsky R, Saito S, Manis JP, Gu Y, Patel P, Bronson R, Appella E, Alt FW, and Chua KF (2003) Developmental defects and p53 hyperacetylation in Sir2 homolog (SIRT1)-deficient mice. Proc Natl Acad Sci USA 100:10794-10799.
33. Chiba T, Yokosuka O, Arai M, Tada M, Fukai K, Imazeki F, Kato M, Seki N, and Saisho H (2004a) Identification of genes up-regulated by histone deacetylase inhibition with cDNA microarray and exploration of epigenetic alterations on hepatoma cells. J Hepatol 41:436-445.
34. Chiba T, Yokosuka O, Fukai K, Kojima H, Tada M, Arai M, Imazeki F, and Saisho H (2004b) Cell growth inhibition and gene expression induced by the histone deacetylase inhibitor, trichostatin A, on human hepatoma cells. Oncology 66:481-491.
35. Chung YL, Wang AJ, and Yao LF (2004) Antitumor histone deacetylase inhibitors suppress cutaneous radiation syndrome: implications for increasing therapeutic gain in cancer radiotherapy. Mol Cancer Ther 3:317-325.
36. Coffey DC, Kutko MC, Glick RD, Butler LM, Heller G, Rifkind RA, Marks PA, Richon VM, and La Quaglia MP (2001) The histone deacetylase inhibitor, CBHA, inhibits growth of human neuroblastoma xenografts in vivo, alone and synergistically with all-trans retinoic acid. Cancer Res 61:3591-3594.
37. Coffey DC, Kutko MC, Glick RD, Swendeman SL, Butler L, Rifkind R, Marks PA, Richon VM, and LaQuaglia MP (2000) Histone deacetylase inhibitors and retinoic acids inhibit growth of human neuroblastoma in vitro. Med Pediatr Oncol 35:577-581.
38. Cohen LA, Marks PA, Rifkind RA, Amin S, Desai D, Pittman B, and Richon VM (2002) Suberoylanilide hydroxamic acid (SAHA), a histone deacetylase inhibitor, suppresses the growth of carcinogen-induced mammary tumors. Anticancer Res 22:1497-1504.
39. Curtin M and Glaser K (2003) Histone deacetylase inhibitors: the Abbott experience. Curr Med Chem 10:2373-2392.
40. Curtin ML, Garland RB, Heyman HR, Frey RR, Michaelides MR, Li J, Pease LJ, Glaser KB, Marcotte PA, and Davidsen SK (2002) Succinimide hydroxamic acids as potent inhibitors of histone deacetylase (HDAC). Bioorg Med Chem Lett 12:2919-2923.
41. Davis PK and Brackmann RK (2003) Chromatin remodeling and cancer. Cancer Biol Ther 2:22-29.
42. de Ruijter AJ, van Gennip AH, Caron HN, Kemp S, and van Kuilenburg AB (2003) Histone deacetylases (HDACs): characterization of the classical HDAC family. Biochem J 370:737-749.
43. Donadelli M, Costanzo C, Faggioli L, Scupoli MT, Moore PS, Bassi C, Scarpa A, and Palmieri M (2003) Trichostatin A, an inhibitor of histone deacetylases, strongly suppresses growth of pancreatic adenocarcinoma cells. Mol Carcinog 38:59-69.
44. Drummond DC, Noble CO, Kirpotin DB, Guo Z, Scott GK, and Benz CC (2004) Clinical development of histone deacetylase inhibitors as anticancer agents. Annu Rev Pharmacol Toxicol 45:495-528.
45. Eyal S, Yagen B, Sobol E, Altschuler Y, Shmuel M, and Bialer M (2004) The activity of antiepileptic drugs as histone deacetylase inhibitors. Epilepsia 45:737-744.
46. Fenrick R and Hiebert SW (1998) Role of histone deacetylases in acute leukemia. J Cell Biochem Suppl 30-31:194-202.
47. Ferrante RJ, Kubilus JK, Lee J, Ryu H, Beesen A, Zucker B, Smith K, Kowall NW, Ratan RR, Luthi-Carter R, et al. (2003) Histone deacetylase inhibition by sodium butyrate chemotherapy ameliorates the neurodegenerative phenotype in Huntington's disease mice. J Neurosci 23:9418-9427.
48. Finnin MS, Donigian JR, Cohen A, Richon VM, Rifkind RA, Marks PA, Breslow R, and Pavletich NP (1999) Structures of a histone deacetylase homologue bound to the TSA and SAHA inhibitors. Nature (Lond) 401:188-193.
49. Finzer P, Stohr M, Seibert N, and Rosl F (2003) Phenylbutyrate inhibits growth of cervical carcinoma cells independent of HPV type and copy number. J Cancer Res Clin Oncol 129:107-113.
50. Fournel M, Trachy-Bourget MC, Yan PT, Kalita A, Bonfils C, Beaulieu C, Frechette S, Leit S, Abou-Khalil E, Woo SH, et al. (2002) Sulfonamide anilides, a novel class of histone deacetylase inhibitors, are antiproliferative against human tumors. Cancer Res 62:4325-4330.
51. Frye RA (2000) Phylogenetic classification of prokaryotic and eukaryotic Sir2-like proteins. Biochem Biophys Res Commun 273:793-798.
52. Fuino L, Bali P, Wittmann S, Donapaty S, Guo F, Yamaguchi H, Wang HG, Atadja P, and Bhalla K (2003) Histone deacetylase inhibitor LAQ824 down-regulates Her-2 and sensitizes human breast cancer cells to trastuzumab, taxotere, gemcitabine and epothilone B. Mol Cancer Ther 2:971-984.
53. Furumai R, Komatsu Y, Nishino N, Khochbin S, Yoshida M, and Horinouchi S (2001) Potent histone deacetylase inhibitors built from trichostatin A and cyclic tetrapeptide antibiotics including trapoxin. Proc Natl Acad Sci USA 98:87-92.
54. Furumai R, Matsuyama A, Kobashi N, Lee KH, Nishiyama M, Nakajima H, Tanaka A, Komatsu Y, Nishino N, Yoshida M, et al. (2002) FK228 (depsipeptide) as a natural prodrug that inhibits class I histone deacetylases. Cancer Res 62:4916-4921.
55. Garcia-Manero G, Issa J-P, Cortes J, Koller C, O'Brien S, Estey E, Canalli AA, Chiao J, Richon V, and Kantarjian H (2004) Phase I study of oral suberoylanilide hydroxamic acid (SAHA), a histone deacetylase inhibitor, in patients (pts) with advanced leukemias or myelodysplastic syndromes (MDS). J Clin Oncol 22 (14 Suppl):Abstract 3027.
56. Gilbert J, Baker SD, Bowling MK, Grochow L, Figg WD, Zabelina Y, Donehower RC, and Carducci MA (2001) A phase I dose escalation and bioavailability study of oral sodium phenylbutyrate in patients with refractory solid tumor malignancies. Clin Cancer Res 7:2292-2300.
57. Gore L, Holden SN, Basche M, Raj SKS, Arnold I, O'Bryant C, Witta S, Rohde B, McCoy C, and Eckhardt SG (2004) Updated results from a phase I trial of the histone deacetylase (HDAC) inhibitor MS-275 in patients with refractory solid tumors. J Clin Oncol 22 (14 Suppl):Abstract 3026.
58. Gore SD and Carducci MA (2000) Modifying histones to tame cancer: clinical development of sodium phenylbutyrate and other histone deacetylase inhibitors. Expert Opin Investig Drugs 9:2923-2934.
59. Gore SD, Weng LJ, Figg WD, Zhai S, Donehower RC, Dover G, Grever MR, Griffin C, Grochow LB, Hawkins A, et al. (2002) Impact of prolonged infusions of the putative differentiating agent sodium phenylbutyrate on myelodysplastic syndromes and acute myeloid leukemia. Clin Cancer Res 8:963-970.
60. Gore SD, Weng LJ, Zhai S, Figg WD, Donehower RC, Dover GJ, Grever M, Griffin CA, Grochow LB, Rowinsky EK, et al. (2001) Impact of the putative differentiating agent sodium phenylbutyrate on myelodysplastic syndromes and acute myeloid leukemia. Clin Cancer Res 7:2330-2339.
61. Gozzini A, Rovida E, Dello Sbarba P, Galimberti S, Santini V, and Galimbert S (2003) Butyrates, as a single drug, induce histone acetylation and granulocytic maturation: possible selectivity on core binding factor-acute myeloid leukemia blasts. Cancer Res 63:8955-8961.
62. Gray SG and Ekstrom TJ (2001) The human histone deacetylase family. Exp Cell Res 262:75-83.
63. Graziano MJ, Pilcher GD, Walsh KM, Kasali OB, and Radulovic L (1997) Preclinical toxicity of a new oral anticancer drug, CI-994 (acetyldinaline), in rats and dogs. Investig New Drugs 15:295-310.
64. Gregoretti IV, Lee YM, and Goodson HV (2004) Molecular evolution of the histone deacetylase family: functional implications of phylogenetic analysis. J Mol Biol 338:17-31.
65. Gregory PD, Wagner K, and Horz W (2001) Histone acetylation and chromatin remodeling. Exp Cell Res 265:195-202.
66. Grozinger CM and Schreiber SL (2002) Deacetylase enzymes: biological functions and the use of small-molecule inhibitors. Chem Biol 9:3-16.
67. Guardiola AR and Yao TP (2002) Molecular cloning and characterization of a novel histone deacetylase HDAC10. J Biol Chem 277:3350-3356.
68. Gui CY, Ngo L, Xu WS, Richon VM, and Marks PA (2004) Histone deacetylase (HDAC) inhibitor activation of p21WAF1 involves changes in promoter-associated proteins, including HDAC1. Proc Natl Acad Sci USA 101:1241-1246.
69. Guo F, Sigua C, Tao J, Bali P, George P, Li Y, Wittmann S, Moscinski L, Atadja P, and Bhalla K (2004) Cotreatment with histone deacetylase inhibitor LAQ824 enhances Apo-2L/tumor necrosis factor-related apoptosis inducing ligand-induced death inducing signaling complex activity and apoptosis of human acute leukemia cells. Cancer Res 64:2580-2589.
70. Gurvich N, Tsygankova OM, Meinkoth JL, and Klein PS (2004) Histone deacetylase is a target of valproic acid-mediated cellular differentiation. Cancer Res 64:1079-1086.
71. Han JW, Ahn SH, Park SH, Wang SY, Bae GU, Seo DW, Kwon HK, Hong S, Lee HY, Lee YW, et al. (2000) Apicidin, a histone deacetylase inhibitor, inhibits proliferation of tumor cells via induction of p21WAF1/Cip1 and gelsolin. Cancer Res 60:6068-6074.
72. Hanahan D and Weinberg RA (2000) The hallmarks of cancer. Cell 100:57-70.
73. He LZ, Tolentino T, Grayson P, Zhong S, Warrell RP Jr, Rifkind RA, Marks PA, Richon VM, and Pandolfi PP (2001) Histone deacetylase inhibitors induce remission in transgenic models of therapy-resistant acute promyelocytic leukemia. J Clin Investig 108:1321-1330.
74. Heltweg B, Dequiedt F, Marshall BL, Brauch C, Yoshida M, Nishino N, Verdin E, and Jung M (2004) Subtype selective substrates for histone deacetylases. J Med Chem 47:5235-5243.
75. Herman JG and Baylin SB (2003) Gene silencing in cancer in association with promoter hypermethylation. N Engl J Med 349:2042-2054.
76. Herold C, Ganslmayer M, Ocker M, Hermann M, Geerts A, Hahn EG, and Schuppan D (2002) The histone-deacetylase inhibitor trichostatin A blocks proliferation and triggers apoptotic programs in hepatoma cells. J Hepatol 36:233-240.
77. Hockly E, Richon VM, Woodman B, Smith DL, Zhou X, Rosa E, Sathasivam K, Ghazi-Noori S, Mahal A, Lowden PA, et al. (2003) Suberoylanilide hydroxamic acid, a histone deacetylase inhibitor, ameliorates motor deficits in a mouse model of Huntington's disease. Proc Natl Acad Sci USA 100:2041-2046.
78. Hong J, Ishihara K, Yamaki K, Hiraizumi K, Ohno T, Ahn JW, Zee O, and Ohuchi K (2003) Apicidin, a histone deacetylase inhibitor, induces differentiation of HL-60 cells. Cancer Lett 189:197-206.
79. Hoshikawa Y, Kwon HJ, Yoshida M, Horinouchi S, and Beppu T (1994) Trichostatin A induces morphological changes and gelsolin expression by inhibiting histone deacetylase in human carcinoma cell lines. Exp Cell Res 214:189-197.
80. Hu E, Dul E, Sung CM, Chen Z, Kirkpatrick R, Zhang GF, Johanson K, Liu R, Lago A, Hofmann G, et al. (2003) Identification of novel isoform-selective inhibitors within class I histone deacetylases. J Pharmacol Exp Ther 307:720-728.
81. Huang L and Pardee AB (2000) Suberoylanilide hydroxamic acid as a potential therapeutic agent for human breast cancer treatment. Mol Med 6:849-866.
82. Huang L, Sowa Y, Sakai T, and Pardee AB (2000) Activation of the p21WAF1/CIP1 promoter independent of p53 by the histone deacetylase inhibitor suberoylanilide hydroxamic acid (SAHA) through the Sp1 sites. Oncogene 19:5712-5719.
83. Huang Y, Horvath CM, and Waxman S (2000) Regrowth of 5-fluorouracil- treated human colon cancer cells is prevented by the combination of interferon gamma, indomethacin and phenylbutyrate. Cancer Res 60:3200-3206.
84. Huang Y and Waxman S (1998) Enhanced growth inhibition and differentiation of fluorodeoxyuridine-treated human colon carcinoma cells by phenylbutyrate. Clin Cancer Res 4:2503-2509.
85. Imai S, Armstrong CM, Kaeberlein M, and Guarente L (2000) Transcriptional silencing and longevity protein Sir2 is an NAD-dependent histone deacetylase. Nature (Lond) 403:795-800.
86. Jaboin J, Wild J, Hamidi H, Khanna C, Kim CJ, Robey R, Bates SE, and Thiele CJ (2002) MS-27-275, an inhibitor of histone deacetylase, has marked in vitro and in vivo antitumor activity against pediatric solid tumors. Cancer Res 62:6108-6115.
87. Jang ER, Lim SJ, Lee ES, Jeong G, Kim TY, Bang YJ, and Lee JS (2004) The histone deacetylase inhibitor trichostatin A sensitizes estrogen receptor alpha-negative breast cancer cells to tamoxifen. Oncogene 23:1724-1736.
88. Jansen MS, Nagel SC, Miranda PJ, Lobenhofer EK, Afshari CA, and McDonnell DP (2004) Short-chain fatty acids enhance nuclear receptor activity through mitogen-activated protein kinase activation and histone deacetylase inhibition. Proc Natl Acad Sci USA 101:7199-7204.
89. Johnstone RW (2002) Histone-deacetylase inhibitors: novel drugs for the treatment of cancer. Nat Rev Drug Discov 1:287-299.
90. Johnstone RW and Licht JD (2003) Histone deacetylase inhibitors in cancer therapy: is transcription the primary target? Cancer Cell 4:13-18.
91. Jones PA and Baylin SB (2002) The fundamental role of epigenetic events in cancer. Nat Rev Genet 3:415-428.
92. Jung M (2001) Inhibitors of histone deacetylase as new anticancer agents. Curr Med Chem 8:1505-1511.
93. Jung M, Brosch G, Kolle D, Scherf H, Gerhauser C, and Loidl P (1999) Amide analogues of trichostatin A as inhibitors of histone deacetylase and inducers of terminal cell differentiation. J Med Chem 42:4669-4679.
94. Kamitani H, Taniura S, Watanabe K, Sakamoto M, Watanabe T, and Eling T (2002) Histone acetylation may suppress human glioma cell proliferation when p21 WAF/Cip1 and gelsolin are induced. Neuro-oncol 4:95-101.
95. Kao HY, Verdel A, Tsai CC, Simon C, Juguilon H, and Khochbin S (2001) Mechanism for nucleocytoplasmic shuttling of histone deacetylase 7. J Biol Chem 276:47496-47507.
96. Keen JC, Yan L, Mack KM, Pettit C, Smith D, Sharma D, and Davidson NE (2003) A novel histone deacetylase inhibitor, scriptaid, enhances expression of functional estrogen receptor alpha (ER) in ER negative human breast cancer cells in combination with 5-aza 2′-deoxycytidine. Breast Cancer Res Treat 81:177-186.
97. Kelly WK, Richon VM, O'Connor O, Curley T, MacGregor-Curtelli B, Tong W, Klang M, Schwartz L, Richardson S, Rosa E, et al. (2002) A phase I clinical trial of an oral formulation of the histone deacetylase inhibitor of suberoylanilide hydroxamic acid (SAHA) (Abstract 286). 14th EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics; 2002 Nov 19-22; Frankfurt, Germany. Eur J Cancer 38 (Suppl 7):S1-S188.
98. Kelly WK, Richon VM, O'Connor O, Curley T, MacGregor-Curtelli B, Tong W, Klang M, Schwartz L, Richardson S, Rosa E, et al. (2003) Phase I clinical trial of histone deacetylase inhibitor: suberoylanilide hydroxamic acid administered intravenously. Clin Cancer Res 9:3578-3588.
99. Kijima M, Yoshida M, Sugita K, Horinouchi S, and Beppu T (1993) Trapoxin, an antitumor cyclic tetrapeptide, is an irreversible inhibitor of mammalian histone deacetylase. J Biol Chem 268:22429-22435.
100. Kim DH, Kim M, and Kwon HJ (2003) Histone deacetylase in carcinogenesis and its inhibitors as anti-cancer agents. J Biochem Mol Biol 36:110-119.
101. Kim MS, Blake M, Baek JH, Kohlhagen G, Pommier Y, and Carrier F (2003) Inhibition of histone deacetylase increases cytotoxicity to anticancer drugs targeting DNA. Cancer Res 63:7291-7300.
102. Kim SH, Ahn S, Han JW, Lee HW, Lee HY, Lee YW, Kim MR, Kim KW, Kim WB, and Hong S (2004) Apicidin is a histone deacetylase inhibitor with anti-invasive and anti-angiogenic potentials. Biochem Biophys Res Commun 315:964-970.
103. Kim YB, Ki SW, Yoshida M, and Horinouchi S (2000) Mechanism of cell cycle arrest caused by histone deacetylase inhibitors in human carcinoma cells. J Antibiot (Tokyo) 53:1191-1200.
104. Kim YB, Lee KH, Sugita K, Yoshida M, and Horinouchi S (1999) Oxamflatin is a novel antitumor compound that inhibits mammalian histone deacetylase. Oncogene 18:2461-2470.
105. Komatsu Y, Tomizaki KY, Tsukamoto M, Kato T, Nishino N, Sato S, Yamori T, Tsuruo T, Furumai R, Yoshida M, et al. (2001) Cyclic hydroxamic-acid-containing peptide 31, a potent synthetic histone deacetylase inhibitor with antitumor activity. Cancer Res 61:4459-4466.
106. Kosugi H, Towatari M, Hatano S, Kitamura K, Kiyoi H, Kinoshita T, Tanimoto M, Murate T, Kawashima K, Saito H, et al. (1999) Histone deacetylase inhibitors are the potent inducer/enhancer of differentiation in acute myeloid leukemia: a new approach to anti-leukemia therapy. Leukemia 13:1316-1324.
107. Kouraklis G and Theocharis S (2002) Histone deacetylase inhibitors and anticancer therapy. Curr Med Chem Anti-Canc Agents 2:477-484.
108. Kramer OH, Zhu P, Ostendorff HP, Golebiewski M, Tiefenbach J, Peters MA, Brill B, Groner B, Bach I, Heinzel T, et al. (2003) The histone deacetylase inhibitor valproic acid selectively induces proteasomal degradation of HDAC2. EMBO (Eur Mol Biol Organ) J 22:3411-3420.
109. Kristeleit R, Stimson L, Workman P, and Aherne W (2004) Histone modification enzymes: novel targets for cancer drugs. Expert Opin Emerg Drugs 9:135-154.
110. Kuefer R, Hofer MD, Altug V, Zorn C, Genze F, Kunzi-Rapp K, Hautmann RE, and Gschwend JE (2004) Sodium butyrate and tributyrin induce in vivo growth inhibition and apoptosis in human prostate cancer. Br J Cancer 90:535-541.
111. Kutko MC, Glick RD, Butler LM, Coffey DC, Rifkind RA, Marks PA, Richon VM, and LaQuaglia MP (2003) Histone deacetylase inhibitors induce growth suppression and cell death in human rhabdomyosarcoma in vitro. Clin Cancer Res 9:5749-5755.
112. Kwon HJ, Kim MS, Kim MJ, Nakajima H, and Kim KW (2002) Histone deacetylase inhibitor FK228 inhibits tumor angiogenesis. Int J Cancer 97:290-296.
113. Lavelle D, Chen YH, Hankewych M, and DeSimone J (2001) Histone deacetylase inhibitors increase p21(WAF1) and induce apoptosis of human myeloma cell lines independent of decreased IL-6 receptor expression. Am J Hematol 68:170-178.
114. Lemaire M, Momparler LF, Farinha NJ, Bernstein M, and Momparler RL (2004) Enhancement of antineoplastic action of 5-aza-2′-deoxycytidine by phenylbutyrate on L1210 leukemic cells. Leuk Lymphoma 45:147-154.
115. Li H and Wu X (2004) Histone deacetylase inhibitor, Trichostatin A, activates p21(WAF1/CIP1) expression through downregulation of c-myc and release of the repression of c-myc from the promoter in human cervical cancer cells. Biochem Biophys Res Commun 324:860-867.
116. Liu LT, Chang HC, Chiang LC, and Hung WC (2003) Histone deacetylase inhibitor up-regulates RECK to inhibit MMP-2 activation and cancer cell invasion. Cancer Res 63:3069-3072.
117. LoRusso PM, Demchik L, Foster B, Knight J, Bissery MC, Polin LM, Leopold WR, 3rd and Corbett TH (1996) Preclinical antitumor activity of CI-994. Investig New Drugs 14:349-356.
118. Lucas DM, Davis ME, Parthun MR, Mone AP, Kitada S, Cunningham KD, Flax EL, Wickham J, Reed JC, Byrd JC, et al. (2004) The histone deacetylase inhibitor MS-275 induces caspase-dependent apoptosis in B-cell chronic lymphocytic leukemia cells. Leukemia 18:1207-1214.
119. Luo J, Nikolaev AY, Imai S, Chen D, Su F, Shiloh A, Guarente L, and Gu W (2001) Negative control of p53 by Sir2alpha promotes cell survival under stress. Cell 107:137-148.
120. Maggio SC, Rosato RR, Kramer LB, Dai Y, Rahmani M, Paik DS, Czarnik AC, Payne SG, Spiegel S, and Grant S (2004) The histone deacetylase inhibitor MS-275 interacts synergistically with fludarabine to induce apoptosis in human leukemia cells. Cancer Res 64:2590-2600.
121. Mahlknecht U and Hoelzer D (2000) Histone acetylation modifiers in the pathogenesis of malignant disease. Mol Med 6:623-644.
122. Marchion DC, Bicaku E, Daud AI, Richon V, Sullivan DM, and Munster PN (2004) Sequence-specific potentiation of topoisomerase II inhibitors by the histone deacetylase inhibitor suberoylanilide hydroxamic acid. J Cell Biochem 92:223-237.
123. Margueron R, Licznar A, Lazennec G, Vignon F, and Cavailles V (2003) Oestrogen receptor alpha increases p21(WAF1/CIP1) gene expression and the antiproliferative activity of histone deacetylase inhibitors in human breast cancer cells. J Endocrinol 179:41-53.
124. Marks PA (2004) The mechanism of the anti-tumor activity of the histone deacetylase inhibitor, suberoylanilide hydroxamic acid (SAHA). Cell Cycle 3:534-535.
125. Marks PA, Miller T, and Richon VM (2003) Histone deacetylases. Curr Opin Pharmacol 3:344-351.
126. Marks PA, Richon VM, Miller T, and Kelly WK (2004) Histone deacetylase inhibitors. Adv Cancer Res 91:137-168.
127. Marks PA, Richon VM, and Rifkind RA (2000) Histone deacetylase inhibitors: inducers of differentiation or apoptosis of transformed cells. J Natl Cancer Inst 92:1210-1216.
128. Marks P, Rifkind RA, Richon VM, Breslow R, Miller T, and Kelly WK (2001) Histone deacetylases and cancer: causes and therapies. Nat Rev Cancer 1:194-202.
129. Marshall JL, Rizvi N, Kauh J, Dahut W, Figuera M, Kang MH, Figg WD, Wainer I, Chaissang C, Li MZ, et al. (2002) A phase I trial of depsipeptide (FR901228) in patients with advanced cancer. J Exp Ther Oncol 2:325-332.
130. McLaughlin F and La Thangue NB (2004) Histone deacetylase inhibitors open new doors in cancer therapy. Biochem Pharmacol 68:1139-1144.
131. Meinke PT, Colletti SL, Doss G, Myers RW, Gurnett AM, Dulski PM, Darkin-Rattray SJ, Allocco JJ, Galuska S, Schmatz DM, et al. (2000) Synthesis of apicidin-derived quinolone derivatives: parasite-selective histone deacetylase inhibitors and antiproliferative agents. J Med Chem 43:4919-4922.
132. Melchior SW, Brown LG, Figg WD, Quinn JE, Santucci RA, Brunner J, Thuroff JW, Lange PH, and Vessella RL (1999) Effects of phenylbutyrate on proliferation and apoptosis in human prostate cancer cells in vitro and in vivo. Int J Oncol 14:501-508.
133. Michaelis M, Michaelis UR, Fleming I, Suhan T, Cinatl J, Blaheta RA, Hoffmann K, Kotchetkov R, Busse R, Nau H, et al. (2004) Valproic acid inhibits angiogenesis in vitro and in vivo. Mol Pharmacol 65:520-527.
134. Mie Lee Y, Kim SH, Kim HS, Jin Son M, Nakajima H, Jeong Kwon H, and Kim KW (2003) Inhibition of hypoxia-induced angiogenesis by FK228, a specific histone deacetylase inhibitor, via suppression of HIF-1alpha activity. Biochem Biophys Res Commun 300:241-246.
135. Mielnicki LM, Ying AM, Head KL, Asch HL, and Asch BB (1999) Epigenetic regulation of gelsolin expression in human breast cancer cells. Exp Cell Res 249:161-176.
136. Miller TA, Witter DJ, and Belvedere S (2003) Histone deacetylase inhibitors. J Med Chem 46:5097-5116.
137. Mitsiades N, Mitsiades CS, Richardson PG, McMullan C, Poulaki V, Fanourakis G, Schlossman R, Chauhan D, Munshi NC, Hideshima T, et al. (2003) Molecular sequelae of histone deacetylase inhibition in human malignant B cells. Blood 101:4055-4062.
138. Motta MC, Divecha N, Lemieux M, Kamel C, Chen D, Gu W, Bultsma Y, McBurney M, and Guarente L (2004) Mammalian SIRT1 represses forkhead transcription factors. Cell 116:551-563.
139. Munster PN, Troso-Sandoval T, Rosen N, Rifkind R, Marks PA, and Richon VM (2001) The histone deacetylase inhibitor suberoylanilide hydroxamic acid induces differentiation of human breast cancer cells. Cancer Res 61:8492-8497.
140. Nakatani Y (2001) Histone acetylases-versatile players. Genes Cells 6:79-86.
141. Nemunaitis JJ, Orr D, Eager R, Cunningham CC, Williams A, Mennel R, Grove W, and Olson S (2003) Phase I study of oral CI-994 in combination with gemcitabine in treatment of patients with advanced cancer. Cancer J 9:58-66.
142. Nguyen DM, Schrump WD, Tsai WS, Chen A, Stewart JHT, Steiner F, and Schrump DS (2003) 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 125:1132-1142.
143. Nimmanapalli R and Bhalla K (2002) Mechanisms of resistance to imatinib mesylate in Bcr-Abl-positive leukemias. Curr Opin Oncol 14:616-620.
144. Nimmanapalli R, Fuino L, Bali P, Gasparetto M, Glozak M, Tao J, Moscinski L, Smith C, Wu J, Jove R, et al. (2003a) 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 Res 63:5126-5135.
145. Nimmanapalli R, Fuino L, Stobaugh C, Richon V, and Bhalla K (2003b) Cotreatment with the histone deacetylase inhibitor suberoylanilide hydroxamic acid (SAHA) enhances imatinib-induced apoptosis of Bcr-Abl-positive human acute leukemia cells. Blood 101:3236-3239.
146. Nishino N, Jose B, Okamura S, Ebisusaki S, Kato T, Sumida Y, and Yoshida M (2003) Cyclic tetrapeptides bearing a sulfhydryl group potently inhibit histone deacetylases. Org Lett 5:5079-5082.
147. +-dependent tubulin deacetylase. Mol Cell 11:437-444.
148. Olivares J, Williams A, Olson S, Pauer LR, Grove W, and Nemunaitis J (2001) Phase I pharmacokinetic (PK) study of CI-994 in combination with carboplatin (C) and paclitaxel (T) in patients (pts) with advanced solid tumors (Abstract 346). Proceedings of the 37th Annual Meeting of the American Society for Clinical Oncology; 2001 May 12-15; San Francisco, California. American Society for Clinical Oncology, Alexandria, VA.
149. O'Shaughnessy J, Flaherty L, Fiorica J, and Grove W (1999) Phase II trial of CI-994 in patients (pts) with metastatic renal cell carcinoma (RCC). (Abstract 1346). Proceedings of the 35th Annual Meeting of the American Society for Clinical Oncology; 1999 May 15-18; Atlanta, Georgia. American Society for Clinical Oncology, Alexandria, VA.
150. Ottmann OG, Deangelo DJ, Stone RM, Pfeifer H, Lowenberg B, Atadja P, Peng B, Scott JW, Dugan M, and Sonneveld P (2004) A phase I, pharmacokinetic (PK) and pharmacodynamic (PD) study of a novel histone deacetylase inhibitor LAQ824 in patients with hematologic malignancies. J Clin Oncol 22 (14 Suppl):Abstract 3024.
151. Pandolfi PP (2001) Histone deacetylases and transcriptional therapy with their inhibitors. Cancer Chemother Pharmacol 48 (Suppl 1):S17-S19.
152. Park WH, Jung CW, Park JO, Kim K, Kim WS, Im YH, Lee MH, Kang WK, and Park K (2003) Trichostatin inhibits the growth of ACHN renal cell carcinoma cells via cell cycle arrest in association with p27, or apoptosis. Int J Oncol 22:1129-1134.
153. Patnaik A, Rowinsky EK, Villalona MA, Hammond LA, Britten CD, Siu LL, Goetz A, Felton SA, Burton S, Valone FH, et al. (2002) A phase I study of pivaloyloxymethyl butyrate, a prodrug of the differentiating agent butyric acid, in patients with advanced solid malignancies. Clin Cancer Res 8:2142-2148.
154. Peart MJ, Tainton KM, Ruefli AA, Dear AE, Sedelies KA, O'Reilly LA, Waterhouse NJ, Trapani JA, and Johnstone RW (2003) Novel mechanisms of apoptosis induced by histone deacetylase inhibitors. Cancer Res 63:4460-4471.
155. Pei XY, Dai Y, and Grant S (2004) Synergistic induction of oxidative injury and apoptosis in human multiple myeloma cells by the proteasome inhibitor bortezomib and histone deacetylase inhibitors. Clin Cancer Res 10:3839-3852.
156. Penner E, Muller S, Zimmermann D, and Van Regenmortel MH (1987) High prevalence of antibodies to histones among patients with primary biliary cirrhosis. Clin Exp Immunol 70:47-52.
157. Piekarz R and Bates S (2004) A review of depsipeptide and other histone deacetylase inhibitors in clinical trials. Curr Pharm Des 10:2289-2298.
158. Piekarz RL, Robey R, Sandor V, Bakke S, Wilson WH, Dahmoush L, Kingma DM, Turner ML, Altemus R, and Bates SE (2001) Inhibitor of histone deacetylation, depsipeptide (FR901228), in the treatment of peripheral and cutaneous T-cell lymphoma: a case report. Blood 98:2865-2868.
159. Piscitelli SC, Thibault A, Figg WD, Tompkins A, Headlee D, Lieberman R, Samid D, and Myers CE (1995) Disposition of phenylbutyrate and its metabolites, phenylacetate and phenylacetylglutamine. J Clin Pharmacol 35:368-373.
160. Plumb JA, Finn PW, Williams RJ, Bandara MJ, Romero MR, Watkins CJ, La Thangue NB, and Brown R (2003) Pharmacodynamic response and inhibition of growth of human tumor xenografts by the novel histone deacetylase inhibitor PXD101. Mol Cancer Ther 2:721-728.
161. Plumb JA, Steele N, Finn PW, and Brown R (2004) Epigenetic approaches to cancer therapy. Biochem Soc Trans 32:1095-1097.
162. Prakash S, Foster BJ, Meyer M, Wozniak A, Heilbrun LK, Flaherty L, Zalupski M, Radulovic L, Valdivieso M, and LoRusso PM (2001) Chronic oral administration of CI-994: a phase 1 study. Investig New Drugs 19:1-11.
163. Qian DZ, Wang X, Kachhap SK, Kato Y, Wei Y, Zhang L, Atadja P and Pili R (2004) The histone deacetylase inhibitor NVP-LAQ824 inhibits angiogenesis and has a greater antitumor effect in combination with the vascular endothelial growth factor receptor tyrosine kinase inhibitor PTK787/ZK222584. Cancer Res 64:6626-6634.
164. Rahmani M, Yu C, Dai Y, Reese E, Ahmed W, Dent P, and Grant S (2003) Coadministration of the heat shock protein 90 antagonist 17-allylamino- 17-demethoxygeldanamycin with suberoylanilide hydroxamic acid or sodium butyrate synergistically induces apoptosis in human leukemia cells. Cancer Res 63:8420-8427.
165. Reid T, Valone F, Lipera W, Irwin D, Paroly W, Natale R, Sreedharan S, Keer H, Lum B, Scappaticci F, et al. (2004) Phase II trial of the histone deacetylase inhibitor pivaloyloxymethyl butyrate (Pivanex, AN-9) in advanced non-small cell lung cancer. Lung Cancer 45:381-386.
166. Reid T, Weeks A, Vakil T, Cosgriff T, Harper F, Valone F, Magnuson A, and Bhatnagar A (2004) Dose escalation study of pivanex (a histone deacetylase inhibitor) in combination with docetaxel for advanced non-small cell lung cancer. J Clin Oncol 22 (14 Suppl):Abstract 7279.
167. Remiszewski SW (2002) Recent advances in the discovery of small molecule histone deacetylase inhibitors. Curr Opin Drug Discov Dev 5:487-499.
168. Remiszewski SW (2003) The discovery of NVP-LAQ824: from concept to clinic. Curr Med Chem 10:2393-2402.
169. Remiszewski SW, Sambucetti LC, Atadja P, Bair KW, Cornell WD, Green MA, Howell KL, Jung M, Kwon P, Trogani N, et al. (2002) Inhibitors of human histone deacetylase: synthesis and enzyme and cellular activity of straight chain hydroxamates. J Med Chem 45:753-757.
170. Richon VM, Emiliani S, Verdin E, Webb Y, Breslow R, Rifkind RA, and Marks PA (1998) A class of hybrid polar inducers of transformed cell differentiation inhibits histone deacetylases. Proc Natl Acad Sci USA 95:3003-3007.
171. Richon VM, Sandhoff TW, Rifkind RA, and Marks PA (2000) Histone deacetylase inhibitor selectively induces p21WAF1 expression and gene-associated histone acetylation. Proc Natl Acad Sci USA 97:10014-10019.
172. Richon VM, Webb Y, Merger R, Sheppard T, Jursic B, Ngo L, Civoli F, Breslow R, Rifkind RA, and Marks PA (1996) Second generation hybrid polar compounds are potent inducers of transformed cell differentiation. Proc Natl Acad Sci USA 93:5705-5708.
173. Richon VM, Zhou X, Rifkind RA, and Marks PA (2001) Histone deacetylase inhibitors: development of suberoylanilide hydroxamic acid (SAHA) for the treatment of cancers. Blood Cells Mol Dis 27:260-264.
174. Rosato RR, Almenara JA, Cartee L, Betts V, Chellappan SP, and Grant S (2002) The cyclin-dependent kinase inhibitor flavopiridol disrupts sodium butyrate-induced p21WAF1/CIP1 expression and maturation while reciprocally potentiating apoptosis in human leukemia cells. Mol Cancer Ther 1:253-266.
175. Rosato RR, Almenara JA, Dai Y, and Grant S (2003) Simultaneous activation of the intrinsic and extrinsic pathways by histone deacetylase (HDAC) inhibitors and tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) synergistically induces mitochondrial damage and apoptosis in human leukemia cells. Mol Cancer Ther 2:1273-1284.
176. Rosato RR, Almenara JA, and Grant S (2003) The histone deacetylase inhibitor MS-275 promotes differentiation or apoptosis in human leukemia cells through a process regulated by generation of reactive oxygen species and induction of p21CIP1/WAF1 1. Cancer Res 63:3637-3645.
177. Rosato RR, Almenara JA, Yu C, and Grant S (2004) Evidence of a functional role for p21WAF1/CIP1 down-regulation in synergistic antileukemic interactions between the histone deacetylase inhibitor sodium butyrate and flavopiridol. Mol Pharmacol 65:571-581.
178. Rosato RR and Grant S (2003) Histone deacetylase inhibitors in cancer therapy. Cancer Biol Ther 2:30-37.
179. Rosato RR, Wang Z, Gopalkrishnan RV, Fisher PB, and Grant S (2001) Evidence of a functional role for the cyclin-dependent kinase-inhibitor p21WAF1/CIP1/MDA6 in promoting differentiation and preventing mitochondrial dysfunction and apoptosis induced by sodium butyrate in human myelomonocytic leukemia cells (U937). Int J Oncol 19:181-191.
180. Roth SY, Denu JM, and Allis CD (2001) Histone acetyltransferases. Annu Rev Biochem 70:81-120.
181. Rowinsky EK, Pacey S, Patnaik A, O'Donnell A, Mita MM, Atadja P, Peng B, Dugan M, Scott JW, and De Bono JS (2004) A phase I, pharmacokinetic (PK) and pharmacodynamic (PD) study of a novel histone deacetylase (HDAC) inhibitor LAQ824 in patients with advanced solid tumors. J Clin Oncol 22 (14 Suppl): Abstract 3022.
182. Ruefli AA, Ausserlechner MJ, Bernhard D, Sutton VR, Tainton KM, Kofler R, Smyth MJ, and Johnstone RW (2001) 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 USA 98:10833-10838.
183. Ryan QC, Headlee D, Sparreboom A, Figg W, Zhai S, Trepel J, Murgo A, Elsayed Y, Karp J, and Sausville E (2003) A phase I trial of an oral histone deacetylase inhibitor, MS-275, in advanced solid tumor and lymphoma patients. Proc Am Soc Clin Oncol 22:200 (Abstract 802).
184. Saito A, Yamashita T, Mariko Y, Nosaka Y, Tsuchiya K, Ando T, Suzuki T, Tsuruo T, and Nakanishi O (1999) A synthetic inhibitor of histone deacetylase, MS-27-275, with marked in vivo antitumor activity against human tumors. Proc Natl Acad Sci USA 96:4592-4597.
185. Sandor V, Bakke S, Robey RW, Kang MH, Blagosklonny MV, Bender J, Brooks R, Piekarz RL, Tucker E, Figg WD, et al. (2002) Phase I trial of the histone deacetylase inhibitor, depsipeptide (FR901228, NSC 630176), in patients with refractory neoplasms. Clin Cancer Res 8:718-728.
186. Sandor V, Senderowicz A, Mertins S, Sackett D, Sausville E, Blagosklonny MV, and Bates SE (2000) P21-dependent g(1)arrest with downregulation of cyclin D1 and upregulation of cyclin E by the histone deacetylase inhibitor FR901228. Br J Cancer 83:817-825.
187. Sasakawa Y, Naoe Y, Inoue T, Sasakawa T, Matsuo M, Manda T, and Mutoh S (2002) Effects of FK228, a novel histone deacetylase inhibitor, on human lymphoma U-937 cells in vitro and in vivo. Biochem Pharmacol 64:1079-1090.
188. Sasakawa Y, Naoe Y, Inoue T, Sasakawa T, Matsuo M, Manda T, and Mutoh S (2003a) Effects of FK228, a novel histone deacetylase inhibitor, on tumor growth and expression of p21 and c-myc genes in vivo. Cancer Lett 195:161-168.
189. Sasakawa Y, Naoe Y, Noto T, Inoue T, Sasakawa T, Matsuo M, Manda T, and Mutoh S (2003b) Antitumor efficacy of FK228, a novel histone deacetylase inhibitor, depends on the effect on expression of angiogenesis factors. Biochem Pharmacol 66:897-906.
190. Sawa H, Murakami H, Ohshima Y, Murakami M, Yamazaki I, Tamura Y, Mima T, Satone A, Ide W, Hashimoto I, et al. (2002) Histone deacetylase inhibitors such as sodium butyrate and trichostatin A inhibit vascular endothelial growth factor (VEGF) secretion from human glioblastoma cells. Brain Tumor Pathol 19:77-81.
191. Schreiber SL and Bernstein BE (2002) Signaling network model of chromatin. Cell 111:771-778.
192. Schwer B, North BJ, Frye RA, Ott M, and Verdin E (2002) The human silent information regulator (Sir)2 homologue hSIRT3 is a mitochondrial nicotinamide adenine dinucleotide-dependent deacetylase. J Cell Biol 158:647-657.
193. Shaker S, Bernstein M, Momparler LF, and Momparler RL (2003) Preclinical evaluation of antineoplastic activity of inhibitors of DNA methylation (5-aza-2′-deoxycytidine) and histone deacetylation (trichostatin A, depsipeptide) in combination against myeloid leukemic cells. Leuk Res 27:437-444.
194. Siavoshian S, Segain JP, Kornprobst M, Bonnet C, Cherbut C, Galmiche JP, and Blottiere HM (2000) Butyrate and trichostatin A effects on the proliferation/differentiation of human intestinal epithelial cells: induction of cyclin D3 and p21 expression. Gut 46:507-514.
195. Singh SB, Zink DL, Liesch JM, Dombrowski AW, Darkin-Rattray SJ, Schmatz DM, and Goetz MA (2001) Structure, histone deacetylase and antiprotozoal activities of apicidins B and C, congeners of apicidin with proline and valine substitutions. Org Lett 3:2815-2818.
196. Singh SB, Zink DL, Liesch JM, Mosley RT, Dombrowski AW, Bills GF, Darkin-Rattray SJ, Schmatz DM, and Goetz MA (2002) Structure and chemistry of apicidins, a class of novel cyclic tetrapeptides without a terminal alpha-keto epoxide as inhibitors of histone deacetylase with potent antiprotozoal activities. J Org Chem 67:815-825.
197. Sowa Y, Orita T, Hiranabe-Minamikawa S, Nakano K, Mizuno T, Nomura H, and Sakai T (1999) Histone deacetylase inhibitor activates the p21/WAF1/Cip1 gene promoter through the Sp1 sites. Ann NY Acad Sci 886:195-199.
198. Sowa Y, Orita T, Minamikawa-Hiranabe S, Mizuno T, Nomura H, and Sakai T (1999) Sp3, but not Sp1, mediates the transcriptional activation of the p21/WAF1/Cip1 gene promoter by histone deacetylase inhibitor. Cancer Res 59:4266-4270.
199. Strait KA, Dabbas B, Hammond EH, Warnick CT, Iistrup SJ, and Ford CD (2002) Cell cycle blockade and differentiation of ovarian cancer cells by the histone deacetylase inhibitor trichostatin A are associated with changes in p21, Rb and Id proteins. Mol Cancer Ther 1:1181-1190.
200. Su GH, Sohn TA, Ryu B, and Kern SE (2000) A novel histone deacetylase inhibitor identified by high-throughput transcriptional screening of a compound library. Cancer Res 60:3137-3142.
201. Suzuki T, Ando T, Tsuchiya K, Fukazawa N, Saito A, Mariko Y, Yamashita T, and Nakanishi O (1999) Synthesis and histone deacetylase inhibitory activity of new benzamide derivatives. J Med Chem 42:3001-3003.
202. Takai N, Desmond JC, Kumagai T, Gui D, Said JW, Whittaker S, Miyakawa I, and Koeffler HP (2004) Histone deacetylase inhibitors have a profound antigrowth activity in endometrial cancer cells. Clin Cancer Res 10:1141-1149.
203. Tang R, Faussat AM, Majdak P, Perrot JY, Chaoui D, Legrand O, and Marie JP (2004) Valproic acid inhibits proliferation and induces apoptosis in acute myeloid leukemia cells expressing P-gp and MRP1. Leukemia 18:1246-1251.
204. Thelen P, Schweyer S, Hemmerlein B, Wuttke W, Seseke F, and Ringert RH (2004) Expressional changes after histone deacetylase inhibition by valproic acid in LNCaP human prostate cancer cells. Int J Oncol 24:25-31.
205. Thiagalingam S, Cheng KH, Lee HJ, Mineva N, Thiagalingam A, and Ponte JF (2003) Histone deacetylases: unique players in shaping the epigenetic histone code. Ann NY Acad Sci 983:84-100.
206. Thibault A, Cooper MR, Figg WD, Venzon DJ, Sartor AO, Tompkins AC, Weinberger MS, Headlee DJ, McCall NA, Samid D, and et al. (1994) A phase I and pharmacokinetic study of intravenous phenylacetate in patients with cancer. Cancer Res 54:1690-1694.
207. Thibault A, Samid D, Cooper MR, Figg WD, Tompkins AC, Patronas N, Headlee DJ, Kohler DR, Venzon DJ, and Myers CE (1995) Phase I study of phenylacetate administered twice daily to patients with cancer. Cancer 75:2932-2938.
208. Timmermann S, Lehrmann H, Polesskaya A, and Harel-Bellan A (2001) Histone acetylation and disease. Cell Mol Life Sci 58:728-736.
209. Undevia SD, Kindler HL, Janisch L, Olson SC, Schilsky RL, Vogelzang NJ, Kimmel KA, Macek TA, and Ratain MJ (2004) A phase I study of the oral combination of CI-994, a putative histone deacetylase inhibitor and capecitabine. Ann Oncol 15:1705-1711.
210. Vrana JA, Decker RH, Johnson CR, Wang Z, Jarvis WD, Richon VM, Ehinger M, Fisher PB, and Grant S (1999) Induction of apoptosis in U937 human leukemia cells by suberoylanilide hydroxamic acid (SAHA) proceeds through pathways that are regulated by Bcl-2/Bcl-XL, c-Jun and p21CIP1, but independent of p53. Oncogene 18:7016-7025.
211. Wade PA (2001) Transcriptional control at regulatory checkpoints by histone deacetylases: molecular connections between cancer and chromatin. Hum Mol Genet 10:693-698.
212. Wang ZM, Hu J, Zhou D, Xu ZY, Panasci LC, and Chen ZP (2002) Trichostatin A inhibits proliferation and induces expression of p21WAF and p27 in human brain tumor cell lines. Ai Zheng 21:1100-1105.
213. Warrener R, Beamish H, Burgess A, Waterhouse NJ, Giles N, Fairlie D, and Gabrielli B (2003) Tumor cell-selective cytotoxicity by targeting cell cycle checkpoints. FASEB J 17:1550-1552.
214. Williams RJ (2001) Trichostatin A, an inhibitor of histone deacetylase, inhibits hypoxia-induced angiogenesis. Expert Opin Investig Drugs 10:1571-1573.
215. Wozniak A, O'Shaughnessy, Fiorica J, and Grove W (1999) Phase II trial of CI-994 in patients (pts) with advanced nonsmall cell lung cancer (NSCLC) (Abstract 1878). Proceedings of the 35th Annual Meeting of the American Society for Clinical Oncology; 1999 May 15-18; Atlanta, Georgia. American Society for Clinical Oncology, Alexandria, VA.
216. Yang X, Phillips DL, Ferguson AT, Nelson WG, Herman JG, and Davidson NE (2001) Synergistic activation of functional estrogen receptor (ER)-alpha by DNA methyltransferase and histone deacetylase inhibition in human ER-alpha-negative breast cancer cells. Cancer Res 61:7025-7029.
217. Yao Q, Nishiuchi R, Li Q, Kumar AR, Hudson WA, and Kersey JH (2003) FLT3 expressing leukemias are selectively sensitive to inhibitors of the molecular chaperone heat shock protein 90 through destabilization of signal transduction-associated kinases. Clin Cancer Res 9:4483-4493.
218. Yokota T, Matsuzaki Y, Miyazawa K, Zindy F, Roussel MF, and Sakai T (2004) Histone deacetylase inhibitors activate INK4d gene through Sp1 site in its promoter. Oncogene 23:5340-5349.
219. Yoshida M, Furumai R, Nishiyama M, Komatsu Y, Nishino N, and Horinouchi S (2001). Histone deacetylase as a new target for cancer chemotherapy. Cancer Chemother Pharmacol 48 (Suppl 1):S20-S26.
220. Yoshida M, Horinouchi S, and Beppu T (1995) Trichostatin A and trapoxin: novel chemical probes for the role of histone acetylation in chromatin structure and function. Bioessays 17:423-430.
221. Yu C, Rahmani M, Almenara J, Subler M, Krystal G, Conrad D, Varticovski L, Dent P, and Grant S (2003) Histone deacetylase inhibitors promote STI571-mediated apoptosis in STI571-sensitive and -resistant Bcr/Abl+ human myeloid leukemia cells. Cancer Res 63:2118-2126.
222. Yu C, Rahmani M, Conrad D, Subler M, Dent P, and Grant S (2003) The proteasome inhibitor bortezomib interacts synergistically with histone deacetylase inhibitors to induce apoptosis in Bcr/Abl+ cells sensitive and resistant to STI571. Blood 102:3765-3774.
223. Yu C, Subler M, Rahmani M, Reese E, Krystal G, Conrad D, Dent P, and Grant S (2003) Induction of apoptosis in BCR/ABL+ cells by histone deacetylase inhibitors involves reciprocal effects on the RAF/MEK/ERK and JNK pathways. Cancer Biol Ther 2:544-551.
224. Zalupski M, O'Shaughnessy J, Vukelja S, Shields A, Diener K, and Grove W (2000) Phase II trial of II-994 in patients (PTS) with advanced pancreatic cancer (APC). (Abstract 1115). Proceedings of the 36th Annual Meeting of the American Society for Clinical Oncology; 2000 May 20-23; New Orleans, Louisiana. American Society for Clinical Oncology, Alexandria, VA.
225. Zhang XD, Gillespie SK, Borrow JM, and Hersey P (2003) The histone deacetylase inhibitor suberic bishydroxamate: a potential sensitizer of melanoma to TNFrelated apoptosis-inducing ligand (TRAIL) induced apoptosis. Biochem Pharmacol 66:1537-1545.
226. Zhang XD, Gillespie SK, Borrow JM, and Hersey P (2004a) The histone deacetylase inhibitor suberic bishydroxamate regulates the expression of multiple apoptotic mediators and induces mitochondria-dependent apoptosis of melanoma cells. Mol Cancer Ther 3:425-435.
227. Zhang Y, Adachi M, Zhao X, Kawamura R, and Imai K (2004b) Histone deacetylase inhibitors FK228, N-(2-aminophenyl)-4-[N-(pyridin-3-yl- methoxycarbonyl)aminomethyl] benzamide and m-carboxycinnamic acid bis-hydroxamide augment radiation-induced cell death in gastrointestinal adenocarcinoma cells. Int J Cancer 110:301-308.
228. Zhou Y, Santoro R, and Grummt I (2002) The chromatin remodeling complex NoRC targets HDAC1 to the ribosomal gene promoter and represses RNA polymerase I transcription. EMBO (Eur Mol Biol Organ) J 21:4632-4640.
229. Zhu WG, Dai Z, Ding H, Srinivasan K, Hall J, Duan W, Villalona-Calero MA, Plass C, and Otterson GA (2001a) Increased expression of unmethylated CDKN2D by 5-aza-2′-deoxycytidine in human lung cancer cells. Oncogene 20:7787-7796.
230. Zhu WG, Lakshmanan RR, Beal MD, and Otterson GA (2001b) DNA methyltransferase inhibition enhances apoptosis induced by histone deacetylase inhibitors. Cancer Res 61:1327-1333.
231. Zhu WG and Otterson GA (2003) The interaction of histone deacetylase inhibitors and DNA methyltransferase inhibitors in the treatment of human cancer cells. Curr Med Chem Anti-Canc Agents 3:187-199.
232. Zimra Y, Nudelman A, Zhuk R, Rabizadeh E, Shaklai M, Aviram A, and Rephaeli A (2000) Uptake of pivaloyloxymethyl butyrate into leukemic cells and its intracellular esterase-catalyzed hydrolysis. J Cancer Res Clin Oncol 126:693-698.
233. Zimra Y, Wasserman L, Maron L, Shaklai M, Nudelman A, and Rephaeli A (1997) Butyric acid and pivaloyloxymethyl butyrate, AN-9, a novel butyric acid derivative, induce apoptosis in HL-60 cells. J Cancer Res Clin Oncol 123:152-160.