Histone deacetylase inhibitors: From target to clinical trials

Expert Opinion on Investigational Drugs

Volumn 11, Issue 12, 2002, Pages 1695-1713

  Kelly, William K ^a   O'Connor, Owen A ^a   Marks, Paul A ^a  

^a MEMORIAL SLOAN KETTERING CANCER CENTER   (United States)

Author keywords

Chromatin; Histone acetyl transferases; Histone deacetylase inhibitors; Histone deacetylases; Histones; Suberoylanilide hydroxamic acid; Trichostatin A

Indexed keywords

3 PHENYLSULFAMOYLCINNAMOHYDROXAMIC ACID; 4 [N (2 HYDROXYETHYL) N [2 (3 INDOLYL)ETHYL]AMINOMETHYL]CINNAMOHYDROXAMIC ACID; 4 N ACETYLDINALINE; 7 [4 (4 CYANOPHENYL)PHENOXY]HEPTANOHYDROXAMIC ACID; ACYLTRANSFERASE; AMIDE; APIDICIN; ARYLBUTYRIC ACID DERIVATIVE; AZACITIDINE; BENZAMIDE DERIVATIVE; BUTYRIC ACID DERIVATIVE; CAPECITABINE; CG 1521; CHLAMYDOCIN; CHROMOSOME PROTEIN; DEPUDECIN; DNA; FR 901228; HISTONE; HISTONE DEACETYLASE; HISTONE DEACETYLASE INHIBITOR; HYDROXAMIC ACID DERIVATIVE; N (2 AMINOPHENYL) 4 (3 PYRIDINYLMETHOXYCARBONYLAMINOMETHYL)BENZAMIDE; OXAMFLATIN; PHENYLACETIC ACID DERIVATIVE; PIVALOYLOXYMETHYL BUTYRATE; RETINOIC ACID; SULFONAMIDE; TRAPOXIN; TRICHOSTATIN A; UNCLASSIFIED DRUG; UNINDEXED DRUG; VALPROIC ACID; VORINOSTAT; ANTINEOPLASTIC AGENT; CYCLOPEPTIDE; ENZYME INHIBITOR; HYDROXAMIC ACID;

ACETYLATION; ANIMAL EXPERIMENT; ANIMAL MODEL; APOPTOSIS; CANCER CELL CULTURE; CANCER GROWTH; CELL DIFFERENTIATION; CELL PROLIFERATION; CELL TRANSFORMATION; CHROMATIN STRUCTURE; CLINICAL TRIAL; CONFUSION; DRUG ACTIVITY; DRUG BIOAVAILABILITY; DRUG HALF LIFE; DRUG STRUCTURE; DRUG TARGETING; DRUG TOLERABILITY; DYSPEPSIA; EDEMA; ENZYME ACTIVITY; ENZYME INHIBITION; FATIGUE; GENE EXPRESSION REGULATION; GENETIC ANALYSIS; GLIOBLASTOMA; GROWTH INHIBITION; HEMATOLOGIC MALIGNANCY; HUMAN; IN VITRO STUDY; IN VIVO STUDY; LUNG NON SMALL CELL CANCER; MALIGNANT NEOPLASTIC DISEASE; MITOSIS INHIBITION; NAUSEA AND VOMITING; NEUROLOGIC DISEASE; NONHUMAN; PROTEIN METHYLATION; PROTEIN PHOSPHORYLATION; PROTEIN PROCESSING; REVIEW; SOLID TUMOR; STIMULUS RESPONSE; DRUG ANTAGONISM; NEOPLASM;

ANTINEOPLASTIC AGENTS; BENZAMIDES; CLINICAL TRIALS; ENZYME INHIBITORS; HISTONE DEACETYLASES; HUMANS; HYDROXAMIC ACIDS; NEOPLASMS; PEPTIDES, CYCLIC;

EID: 0036906832     PISSN: 13543784     EISSN: None     Source Type: Journal    
DOI: 10.1517/13543784.11.12.1695     Document Type: Review

References (134)

1. MARKS PA, RIFKIND RA: Erythroleukemic differentiation. Ann. Rev. Biochem. (1978) 47:419-478.
2. MARKS PA, RIFKIND RA, RICHON VM et al.: Histone deacetylases and cancer: causes and therapies. Nat. Rev. Cancer (2001) 1:194-202.
3. JENUWEIN T, ALLIS CD: Translating the histone code. Science (2001) 293:1074-1080.
4. CHEUNG P, ALLIS CD, SASSONE-CORSI P: Signaling to chromatin through histone modifications. Cell (2000) 103:263-271.
5. WOLFFE AP, PRUSS D: Deviant nucleosomes: the functional specialization of chromatin. Trends Genet. (1996) 12:58-62.
6. STRAHL BD, ALLIS CD: The language of covalent histone modifications. Nature (2000) 403:41-45.
7. TURNER BM: Histone acetylation and an epigenetic code. Bioessays (2000) 22: 836-845.
8. REA SF, EISENHABER F, O'CARROLL BD et al.: Regulation of chromatin structure by site-specific histone H3 methyltransferase. Nature (2000) 406:593-599.
9. KHOCHBIN S, VERDEL A, LEMERCIER C, SEIGNEURIN-BERNY D: Functional significance of histone deacetylase diversity. Curr. Opin. Genet. Dev. (2001) 11:162-166.
10. NG HH, BIRD A: Histone deacetylases: silencers for hire. Trends Biochem. Sci. (2000) 25:121-126.
11. URNOV FD, WOLFFE A: Chromatin organization and human disease. Emerg. Ther. Targets (2000) 4: 665-685.
12. MAHIKNECHT U, HOELZER D: Histone acetylation modifiers in the pathogenesis of malignant disease. Mol. Med. (2000) 6:623-644.
13. TIMMERMANN S, LEHRMANN H, POLESSKAYA A, HAREL-BELLAN A: Histone acetylation and disease. Cell. Mol. Life Sci. (2001) 58:728-736.
14. CRESS WD, SETO E: Histone deacetylases, transcriptional control and cancer. J. Cell. Physiol. (2000) 184:1-16.
15. CAMERON EE, BACHMAN KE, MYOHANEN S et al.: Synergy of demethylation and histone deacetylase inhibition in the re-expression of genes silenced in cancer. Nat. Genet. (1999) 21:103-107.
16. WANG C, FU M, MANI S et al.: Histone acetylation and the cell-cycle in cancer. Front. Biosci. (2001) 6:610-629.
17. VIGUSHIN DM, COOMBES RC: Histone deacetylase inhibitors in cancer treatment. Anti-Cancer Drugs (2002) 13:1-13.
18. JONES PA, BAYLIN SB: The fundamental role of epigenetic events in cancer. Nature Rev. Genet. (2002) 3:415-428.
19. SPECK NA, GILLILAND DG: Core-binding factors in haematopoiesis and leukaemia. Nat. Rev. Cancer (2002) 2:502-513.
20. MARKS PA, RICHON VM, RIFKIND RA: Histone deacetylase inhibitors: inducers of differentiation or apoptosis of transformed cells. J. Natl. Cancer Inst. (2000) 92:1210-1216.
21. VAN LINT C, EMILIANI S, VERDIN E: The expression of a small fraction of cellular gene is changed in response to histone hyperacetylation. Gene Expr. (1996) 5:245-254.
22. BUTLER LM, ZHOU X., XU W-S et al.: The histone deacetylase inhibitor SAHA arrests cancer cell growth, up-regulates thioredoxin-binding protein-2, and down-regulates thioredoxin. Proc. Natl. Acad. Sci. USA (2002) 99:11700-11705.
23. SUZUKI H, GABRIELSON E, CHEN W et al.: A genomic screen for genes upregulated by demethylation and histone deacetylase inhibitors in human colorectal cancer. Nat. Genet. (2002) 31:141-149.
24. ROGIONE FD, CRINITE V, DELLA-PIETRA V et al.: Genes modulated by histone acetylation as new effectors of butyrate activity. FEBS (2001) 499:199-204.
25. LUGER K, MADER AW, RICHMOND RK et al.: Crystal structure of the nucleosome core particle at 2.8 A resolution. Nature (1997) 389:231-233.
26. GREGORY PD, WAGNER K, HORZ W: Histone acetylation and chromatin remodeling. Exp. Cell Res. (2001) 265:195-202.
27. DAVIE JR: Covalent modifications of histones: expression from chromatin templates. Curr. Opin. Genet. Dev. (1998) 8:173-174.
28. KOUZARIDES T. Acetylation: a regulatory modification to rival phosphorylation? EMBO J. (2000) 19:1176-1179.
29. TURNER BM: Histone acetylation and an epigenic code. BioEssays (2000) 22:836-845.
30. BIRD A: Methylation talk between histones and DNA. Science (2001) 294:2113-2115.
31. BANNISTER AJ, ZEGERMAN P, PARTRIDGE JF et al.: Selective recognition of methylated lysine 9 on histone H3 by the HP1 chromo domain. Nature (2001) 410:120-124.
32. NAKAYAMA J-I, RICE JC, STRAHL BD et al.: Role of histone H3 lysine 9 methylation in epigenetic control of heterochromatin assembly. Science (2001) 292:110-113.
33. STERNER DE, BERGER SL: Acetylation of histones and transcription-related factors. Microbiol. Mol. Biol. Rev. (2000) 64:435-459.
34. YANG X-J, OGRYZKO VV, NISHIKAWA J-I: A P300/CBP-associated factor that competes with the adenoviral oncoprotein E1A. Nature (1996) 382:319-324.
35. ROTH SY, DENU JM, ALLIS CD: Histone acetyltransferases. Ann. Rev. Biochem. (2001) 70:81-120.
36. DECKERT J, STRUHL K: Histone acetylation at promoters is differentially affected by specific activators and repressors. Mol. Cell Biol. (2001) 8:2726-2735.
37. GREGORY PD: Histone acetylation and chromatin remodeling. Exp. Cell Res. (2001) 265:195-202.
38. GRAY GG, EKSTROM TJ: The human histone deacetylase family. Exp. Cell Res. (2001) 262:75-83.
39. ZHOU X, MARKS PA, RIFKIND RA et al.: Cloning and characterization of a histone deacetylase, HDAC9. Proc. Natl. Acad. Sci. USA (2001) 98:10572-10577.
40. GROZINGER CM, HASSIG CA, SCHREIBER SL: Three proteins define a class of human histone deacetylases related to yeast Hda1p. Proc. Natl. Acad. Sci. USA (1999) 96:4868-4873.
41. GAO L, CUETO MA, ASSELBERGS F, ATAOJA P: Cloning and functional characterization of HDAC II, a novel member of the human histone deacetylase family. J. Biol. Chem. (2002) 277:25748-25755.
42. KAO H-Y, LEE C-H, KOMAROV A et al.: Isolation and characterization of mammalian HDAC10, a novel histone deacetylase. J. Biol. Chem. (2002) 277:187-193.
43. FISCHER DD, CAI R, BHATIA U et al.: Isolation and characterization of a novel class II histone deacetylase, HDAC10. J. Biol. Chem. (2002) 277:6656-6666.
44. GUARDIOLA AR, YAO TP: Molecular cloning and characterization of a novel histone deacetylase HDAC10. J. Biol. Chem. (2002) 277:3350-3356.
45. LANDRY J, SUTTON A, STEFAN T, TAFROV RC, STEBINS J: The silencing protein SIR2 and its homologs are NAD-dependent protein deacetylases. Proc. Natl. Acad. Sci. USA (2000) 97:5807-5811.
46. FRYE RA: Phylogenetic classification of prokaryotic and eukaryotic Sir2-like proteins. Biochem. Biophys. Res. Commun. (2000) 273:793-798.
47. ALLAND L, MUHLE R, HOU JR et al.: Role for N-CoR and histone deacetylase in Sin3-mediated transcriptional repression. Nature (1997) 387:49-55.
48. HEINZEL T, LAVINSKY RM, MULLEN TM et al.: A complex containing N-CoR, mSin3 and histone deacetylase mediates transcriptional repression. Nature (1997) 387:43-48.
49. JOHNSON CA, WHITE DA, LAVENDER JS et al.: Human class I histone deacetylase complexes show enhanced catalytic activity in the presence of ATP and co-immunoprecipate with the ATP-dependent chaperone protein HSP70. J. Biol. Chem. (2002) 277:9590-9597.
50. LU J, McKINSEY TA, ZHANG C-L et al.: Regulation of skeletal myogenesis by association of the MEF2 transcription factor with class II histone deacetylases. Mol. Cell (2000) 6:233-244.
51. BERNSTEIN BE, TONG JK, SCHREIBER SL: Genome wide studies of histone deacetylase in yeast. Proc. Natl. Acad. Sci. USA (2000) 97:13708-13713.
52. CHAN HM, KASTIC-DEMONACOS M, SMITH L et al.: Acetylation control of the retinoblastoma tumor-suppressor protein. Mol. Cell Biol. (2001) 3:667-674.
53. NAGY L, KAO HY, CHATERAVATI D et al.: Nuclear receptor repression mediated by a complex containing SMRT, mSin3A and histone deacetylase. Cell (1997) 89:373-380.
54. ITO K, BARNES PJ, ADCOCK IM: Glucocorticoid receptor recruitment of histone deacetylase 2 inhibits interleukin-1-β induced histone H4 acetylation on lysines 8 and 12. Mol. Cell Biol. (2000) 20:6891-6903.
55. 2/M checkpoint Rad proteins. J. Biol. Chem. (2000) 275:27909-27916.
56. ROBERTSON KD, AIT-SI-ALI S, YOKOCHI T, WADE PA, JONES PL, WOLFFE AP: DNMT1 forms a complex with Rb, E2F1 and HDAC1 and represses transcription from E2F-responsive promoters. Nat. Genet. (2000) 25:338-342.
57. SMIRNOV DA, HOU S, RICCIARDI RP: Association of histone deacetylase with COUP-TF in tumorigenic Ad12-transformed cells and its potential role in shut-off of MHC class 1 transcription. Virology (2000) 268:319-328.
58. GILES RH, PETERS DJ, BREUNING MH: Conjunction dysfunction: CBP/p300 in human disease. Trends Genet. (1998) 14:178-183.
59. GAYTHER SA, BATLEY SJ, LINGER L, BANNISTER A et al.: Mutations truncating the EP300 acetylase in human cancers. Nature Genet. (2000) 24:300-303.
60. MURATA T, KUROKAWA R, KRONES A et al: Defect of histone acetyltransferase activity of the nuclear transcriptional coactivator CBP in Rubinstein-Taybi syndrome. Hum. Mol. Genet. (2001) 10:1071-1076.
61. MAGNAGHI-JAULIN L, GROISMAN R, NAGUIBNEVA I et al.: Retinoblastoma protein represses transcription by recruiting a histone deacetylase. Nature (London) (1998) 391:601-605.
62. MURPHY M, AHN J, WALKER KK et al.: Transcriptional repression by wild-type p53 utilizes histone deacetylases, mediated by interaction with mSin3a. Genes Dev. (1999) 13:2490-2501.
63. YARDEN RI, BRODY LC: BRCA1 interacts with components of the histone deacetylase complex. Proc. Natl. Acad. Sci. USA (1999) 96:4983-4988.
64. FENICK R, HIEBERT SW: Role of histone deacetylase in acute leukemia. J. Cell. Biochem. (1998) 31:194-202.
65. HE L-Z, TOLENTINO T, GRAYSON P et al.: Histone deacetylase inhibitors induce remission in transgenic models of therapy-resistant acute promyleocytic leukemia. J. Clin. Invest. (2001) 108:1321-1330.
66. WANG J, HOSHINO T, REDNER RL et al.: ETO, fusion partner in t(8;21) acute myeloid leukemia, represses transcription by interaction with the human N-Co-R/mSin3/HDAC1 complex. Proc. Natl. Acad. Sci. USA (1998) 95:10860-10865.
67. KRAMER OH, GOTTLICHER M, HEINZEL T: Histone deacetylase as a therapeutic target. Trends Endocrinol. Metab. (2001) 12:294-300.
68. MARKS PA, RICHON VM, BRESLOW R et al.: Histone deacetylase inhibitors as new cancer drugs. Curr. Opin. Oncol. (2001) 13:477-485.
69. GLASER KB, LI J, AAKRE ME et al.: Transforming growth factor β mimetics: discovery of 7-[4-(4-cyanophenyl) phenoxy]-heptanohydroxamic acid, a biaryl hydroxamate inhibitor of histone deacetylase. Mol. Cancer Ther. (2002) 1:759-768.
70. UESATO S, KITAGAWA M, NAGAOKA Y et al.: Novel histone deacetylase inhibitors: N-hydroxycarboxamides possessing a terminal bicyclic aryl group. Bioorg. Med. Chem. Lett. (2002) 12:1347-1349.
71. LAVOIE R, BOUCHAIN G, FRECHETTE S: Design and synthesis of a novel class of histone deacetylase inhibitors. Bioorg. Med. Chem. Lett. (2001) 11:2847-2850.
72. NEWMARK HL, LUPTON JR, YOUNG CW: Butyrate as a differentiating agent: pharmacokinetics analogues and current status. Cancer Lett. (1994) 78:1-5.
73. CARDUCCI MA, BOWLING MK, EISENBERGER M et al.: Phenylbutyrate (PB) for refractory solid tumors: Phase I clinical and pharmacologic evaluation of intravenous and oral PB. Anticancer Res. (1997) 17:3972-3973.
74. THIBAUDT A, COOPER MR, FIGG WD et al.: A Phase I and pharmacokinetic study of intravenous phenylacetate in patients with cancer. Cancer Res. (1994) 54:1690.
75. CONLEY BA, EGORIN MJ, TAIT H et al.: Phase I study of orally administered butyrate prodrug tubutepin, in patients with solid tumors. Clin. Cancer Res. (1998) 4:629-634.
76. GORE SD, CARDUCCI MA: Modifying histones to tame cancer: clinical development of sodium phenylbutyrate and other histone deacetylase inhibitors. Expert Opin. Investig. Drugs (2000) 9:2923-2934.
77. GILBERT J, BAKER SD, BOWLING MK et al.: A Phase I dose escalation and bioavailability study of oral sodium phenylbutyrate in patients with refractory solid tumor malignancies. Clin. Cancer Res. (2001) 7:2292-2300.
78. WARRELL RP, HE LZ, RICHON VM et al.: Therapeutic targeting of transcription in acute promyelocytic leukemia by use of an inhibitor of histone deacetylase. J. Natl. Cancer Inst. (1998) 90:1621-1625.
79. NOVICH S: Initial clinical evaluation of transcription therapy for cancer: all-trans retinoic acid plus phenylbutyrate. Blood (1999) 94:61A.
80. PHIEL CJ, ZHANG F, HUANG EY et al.: Histone deacetylase is a direct target of valproic acid, a potent anticonvulsant, mood stabilizer, and teratogen. J. Biol. Chem. (2001) 276:36734-36741.
81. GOTTLICHER M, MINUCCI S, ZHU P et al.: Valproic acid defines a novel class of HDAC inhibitors inducing differentiation of transformed cells. EMBO J. (2001) 20:6969-6978.
82. 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) 265:17174-17179.
83. RICHON VM, EMILIANI S, VERDIN E et al.: A class of hybrid polar inducers of transformed cell differentiation inhibits histone deacetylases. Proc. Natl. Acad. Sci. USA (1998) 95:3003-3007.
84. KIM YB, LEE KH, SUGITA K, YOSHIDA M, HORINOUCHI S: Oxamflatin is a novel antitumor compound that inhibits mammalian histone deacetylase. Oncogene (1999) 18:2461-2470.
85. BUTLER LM, AGUS D, SCHER HI et al.: Suberoylanilide hydroxamic acid, an inhibitor of histone deacetylase, suppresses the growth of prostate cancer cells in vitro and in vivo. Cancer Res. (2000) 60:5165-5170.
86. BUTLER LM, WEBB Y, AGUS DB et al.: Inhibition of transformed cell growth and induction of cellular differentiation by pyroxamide, an inhibitor of histone deacetylase. Clin. Cancer Res. (2001) 7:962-970.
87. HUANG L, PARDEE AB: Suberoylanilide hydroxamic acid as a potential therapeutic agent for human breast cancer treatment. Mol. Med. (2000) 6:849-866.
88. RICHON VM, WEBB Y, MERGER R, SHEPPARD T et al.: Second generation hybrid polar compounds are portent inducers of transformed cell differentiation. Proc. Natl. Acad. Sci. USA (1996) 93:5705-5708.
89. SU GH, SOHN TA, RYU BA: A novel histone deacetylase inhibitor identified by high-throughput transcriptional screening of a compound library. Cancer Res. (2000) 60:3137-3142.
90. LAVOIE R, BOUCHAIN G, FRECHETTE S et al.: Design and synthesis of a novel class of histone deacetylase inhibitors. Bioorg. Med. Chem. Lett. (2001) 11:2847-2850.
91. QUI L, KELSO MJ, HANSEN C, WEST ML, FAIRLIE DP, PARSONS PG: Antitumor activity in vitro and in vivo of selective differentiating agents containing hydroxamate. Br. J. Cancer (1999) 80:1252-1258.
92. PARSONS PG, HANSEN C, FAIRLIE DP et al.: Tumor selectivity and transcriptional activation by azelaic bishydroxamic acid in human melanocytic cells. Biochem. Pharmacol. (1997) 53:1719-1724.
93. KIJIMA M, YOSHIDA M, SUGITA K, HORINOUCHI S, BEPPU T: Trapoxin, an antitumor cyclic tetrapeptide, is an irreversible inhibitor of mammalian histone deacetylase. J. Biol. Chem. (1993) 268:22429-22435.
94. NAKAJIMA H, KIM YB, TERANO H, YOSHIDA M, HORINOUCHI S: FR901228, a potent antitumor antibiotic, is a novel histone deacetylase inhibitor. Exp. Cell Res. (1998) 241:126-133.
95. MURRAY PJ, KRANZ M, LADLOW M et al.: The synthesis of cyclic tetrapeptoid analogues of the antiprotozoal natural product apicidin. Bioorg. Med. Chem. Lett. (2001) 11:773-776.
96. MEINKE PT, COLLETTI SL, DOSS G et al.: Synthesis of apicidin-derived quinolone derivatives: parasite-selective histone deacetylase inhibitors and antiproliferative agents. J. Med. Chem. (2000) 43:4919-4922.
97. KOSUGI H, ITO M, YAMAMOTO Y et al.: In vivo effects of a histone deacetylase inhibitor, FK228, on human acute promyeocytic leukemia in NOD/Shi-scid/scid mice. Jpn. J. Cancer Res. (2001) 92:529-536.
98. SUZUKI T, ANDO T, TSUCHIYA K, et al.: Synthesis and histone deacetylase inhibitory activity of new benzamide derivatives. J. Med. Chem. (1999) 42:3001-3003.
99. SAITO A, YAMASHITA T, MARIKO Y et al.: A synthetic inhibitor of histone deacetylase, MS-27-275, with marked in vivo antitumor activity against human tumors. Proc. Natl. Acad. Sci USA (1999) 96:4592-4597.
100. KWON HJ, OWA T, HASSIG CA, SHIMADA J, SCHREIBER SL: Depudecin induces morphological reversion of transformed fibroblasts via the inhibition of histone deacetylase. Proc. Natl. Acad. Sci. USA (1998) 95:3356-3361.
101. FINNIN MS, DONIGIAN JR, COHEN A et al.: Structures of a histone deacetylase homologue bound to TSA and SAHA inhibitors. Nature (1999) 401:188-193.
102. waf1 expression and gene-associated histone acetylation. Proc. Natl. Acad. Sci. USA (2000) 97:10014-10019.
103. SAMBUCETTI LC, FISCHER DD, ZABLUDOFF S et al.: Histone deacetylase inhibition selectively alters the activity and expression of cell cycle proteins leading to specific chromatin acetylation and antiproliferative effects. J. Biol. Chem (1999) 274:34940-34947.
104. YOSHIDA M, HORINOUCHI S, BEPPU T: Trichostatin A and novel chemical probes for the role of histone acetylation in chromatin structure and functioin. Bioessays (1995) 17:423-430.
105. XIAO H, HASEGAWA T, ISOBE K: Both Sp1 and Sp3 are responsible for p21waf1 promoter activity induced by histone deacetylase inhibitor in NIH3T3 cells. J. Cell Biochem. (1999) 73:291-302.
106. JOHNSTONE RW. Histone deacetylase inhibitors: Novel drugs for the treatment of cancer. Nature Rev. Drug Discov. (2002) 1:287-299.
107. VRANA JA, DECKER RH, JOHNSON CR 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-XL, c-Jun, and p211 CIP1, but independent of p53. Oncogene (1999) 18:7016-7025.
108. MACLEOD KF, SHERRY N, HANNON G et al.: p53-dependent and independent expression of p21 during cell growth, differentiation, and DNA damage. Genes Dev. (1995) 9:935-944.
109. TAKAKURA M, KYO S, SOWA Y et al.: Telomerase activation by histone deacetylase inhibitor in normal cells. Nucleic Acids Res. (2001) 29:3006-3011.
110. BRINKMANN H, DAHLER AL, POPA C et al.: Histone hyperacetylation induced by histone deacetylase inhibitors is not sufficient to cause growth inhibition in human dermal fibroblasts. J. Biol. Chem. (2001) 276:22491-22499.
111. KIM MS, KWON HJ, LEE YM et al.: Histone deacetylases induce angiogenesis by negative regulation of tumor suppressor genes. Nat. Med. (2001) 7:437-443.
112. KWON HJ, KIM MS, KIM MJ, NAKAJIMA H, KIM KW: Histone deacetylase inhibitor FK228 inhibits tumor angiogenesis. J. Int. Cancer (2002) 97(3):290-296.
113. DEROANNE CF, BONJEAN K, SERVOTTE S et al.: Histone deacetylases inhibitors as anti-angiogenic agents altering vascular endothelial growth factor signaling. Oncogene (2002) 21:427-436.
114. THIBAULT A, SAMID D, COOPER MR et al.: Phase I study of Phenylacetate administered twice daily to patients with cancer. Cancer (1995) 75:2932-2938.
115. CHANG S, KUHN J, ROBINS I et al.: Phase II study of phenylacetate in patients with recurrent malignant gliomas: a north American brain tumor consortium report. J. Clin. Onc. (1999) 17:984-990.
116. CARDUCCI MA, NELSON JB, CHANTACK KM et al.: Phenylbutyrate induces apoptosis in human prostate cancer and is more potent than phenylacetate. Clin. Cancer Res. (1996) 2:379-387.
117. GORE SD, MILLER CB, WENG LJ et al.: Clinical development of sodium phenylbutyrate as putative differentiating agent in myeloid malignancies. Anticancer Res. (1997) 17:3938.
118. ZHOU D, KIM S, DING W, SCHULTZ C, WARRELL R, GALLAGHER R: Frequent mutations in the ligand-binding domain of PML-RARa after multiple relapses of acute promyelocytic leukemia: analysis for functional relationship to response to all-trans retinoic acid and deacetylase inhibitors in vitro and in vivo. Blood (2002) 99:1356-1363.
119. GILBERT J, BAKER S, DONEHOWER R et al.: Methyltransferase (MT) activity and gene expression in tumor biopsies from patients enrolled in a Phase I study of the MT inhibitor, 5-Azacytidine and histone deacetylase inhibitor, phenylbutyrate in refractory solid tumors. Proc. Am. Soc. Clin. Onc. (2001):87a (Abstract).
120. KEER H, REID T, SREEDHARAN S: Pivanex activity in refractory non-small cell lung cancer, a Phase II study. Proc. Am. Soc. Clin. Onc. (2001):314a (Abstract).
121. GOTTLICHER M, MINUCCI S, ZHU P et al.: Valproic acid defines a novel class of HDAC inhibitors inducing differentiation of transformed cells. EMBO J. (2001) 20:6969-6978.
122. KELLY WK, RICHON VM, TROSO-SANDOVAL T et al.: Suberoylanilide hydroxamic acid (SAHA), a histone deacetylase inhibitor: biologic activity without toxicity. Proc. Am. Soc. Clin. Onc. (2001):87a (Abstract).
123. KELLY WK, O'CONNOR O, RICHON VM ET AL: A Phase I clinical trial of an oral formulation of the histone deacetylase inhibitor of suberoylanilide hydroxamic acid (SAHA). 14th EORTC-NCI-AACR, Frankfurt (2002):286 (Abstract).
124. O'CONNOR OA, KELLY WK, WANG E et al.: Clinical development of the histone deacetylase inhibitor suberoylanilide hydroxamic acid (SAHA) in agressive non-Hodgkin's lymphoma and Hodgkin's disease. Proceedings of the 43rd Annual American Society of Hematology (2001):2562 (Abstract).
125. NAKAJIMA H, KIM YB, TERANO H, YOSHIDA M, HORINOUCHI S: FR901228, a potent antitumor antibiotic, is a novel histone deacetylase inhibitor. Exp. Cell Res. (1998) 241:126-128.
126. SANDOR V, BAKKE S, ROBEY R et al.: Phase I trial of a novel antitumor depsipeptide (FR 901228) in patients with refractory neoplasms. Clin. Cancer Res. (2001) 8:718-728.
127. PIEKARZ R, ROBEY R, BAKKE S, SANDOR V, WILSON W, BATES S: Histone deacetylase inhibitor for the treatment of peripheral or cutaneous T-cell lymphoma. Proc. Am. Soc. Clin. Onc. (2001):232b (Abstract).
128. PIEKARZ RL, ROBEY R, SANDOR V 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.
129. PRAKASH S, FOSTER B, MEYER M et al.: Chronic administration of CI-994: a Phase I study. Invest. New Drugs (2001) 19:1-11.
130. WOZNIAK A, O'SHAUGHNESSY J, FIORICA J, GROVE W: Phase II trial of CI-994 in patients with advanced non-small cell lung cancer. Proc. Am. Soc. Clin. Onc. (1999):487a (Abstract).
131. O'SHAUGHNESSY J, FLAHERTY L, FIORICA J, GROVE W: Phase II trial of CI-994 in patients with metastatic renal cell carcinoma. Proc. Am. Soc. Clin. Onc. (1999):349a (Abstract).
132. KIMMEL KA, KINDLER HL, JANISCH S, OLSON S, GROVE W: Phase I dose-finding study of CI-994 in combination with capecitabine in patients with advanced solid tumors. Proc. Am. Soc. Clin. Onc. (2001):87a (Abstract).
133. OLIVARES J, WILLIAMS A, OLSON S, PAUER LR, GROVE W: Phase I pharmacokinetic study of CI-994 in combination with carboplatin and paclitaxel in patients with advanced solid tumors. Proc. Am. Soc. Clin. Onc. (2001):87a (Abstract).
134. ARDIZZONI A, LOPREVITE M: Histone deacetylation inhibitors. New Drugs in Lung Cancer S52-S54.