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Review

Interpreting clinical assays for histone deacetylase inhibitors

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Pages 117-141 | Published online: 30 Sep 2022

References

  • ChoudhuriSCuiYKlaassenCDMolecular targets of epigenetic regulation and effectors of environmental influencesToxicol Appl Pharmacol2010245337839320381512
  • Santos-RosaHCaldasCChromatin modifier enzymes, the histone code and cancerEur J Cancer200541162381240216226460
  • OliverSSDenuJMDynamic interplay between histone H3 modifications and protein interpreters: emerging evidence for a “histone language”Chembiochem201112229930721243717
  • ZeeBMLevinRSDimaggioPAGlobal turnover of histone post-translational modifications and variants in human cellsEpigenetics Chromatin20103223321134274
  • DekkerFHaismaHJHistone acetyl transferases as emerging drug targetsDrug Discovery Today20091419/2094294819577000
  • LimSMetzgerESchüleREpigenetic regulation of cancer growth by histone demethylasesInt J Cancer201012791991199820607829
  • NicholsonTBChenTRichardSThe physiological and pathophysiological role of PRMT1-mediated protein arginine methylationPharmacol Res200960646647419643181
  • FackelmayerFOProtein arginine methyltransferases: guardians of the Arg?Trends Biochem Sci2005301266667116257219
  • TiniMNaeemHTorchiaJBiochemical analysis of arginine methylation in transcriptionMethods Mol Biol200952323524719381935
  • SpannhoffATHauserRHeinkeWThe emerging therapeutic potential of histone methyltransferase and demethylase inhibitorsChemMedChem20094101568158219739196
  • ZhangYXuKNiMNucleosome dynamics define transcriptional enhancersNature Genetics201042434334720208536
  • CopelandRAOlhavaEJScottMPTargeting epigenetic enzymes for drug discoveryCurr Opin Chem Biol201014450551020621549
  • JonesPABaylinSBThe fundamental role of epigenetic events in cancerNat Rev Genet20023641542812042769
  • KriaucionisSHeintzNThe nuclear DNA base 5-hydroxymethylcytosine is present in purkinje neurons and the brainScience2009324592992993019372393
  • Abdel-WahabOMullallyAHedvatCGenetic characterization of TET1, TET2, and TET3 alterations in myeloid malignanciesBlood2009114114414719420352
  • FabbriMCalinGAEpigenetics and miRNAs in human cancerAdv Genet201070879920920746
  • ZainJKaminetzkiDO’ConnorOAEmerging role of epigenetic therapies in cutaneous T-cell lymphomasExpert Rev Hematol20103218720321083462
  • GrahamJSKayeSBBrownRThe promises and pitfalls of epigenetic therapies in solid tumorsEur J Cancer20094571129113619211243
  • BoldenJEPeartMJJohnstoneRWAnticancer activities of histone deacetylase inhibitorsNat Rev Drug Discov20065957695784
  • HaberlandMMontgomeryRLOlsonENThe many roles of histone deacetylases in development and physiology: implications for disease and therapyNat Rev Genet2009101324219065135
  • RazidloDFWhitneyTJCasperMEHistone deacetylase 3 depletion in osteo/chondroprogenitor cells decreases bone density and increases marrow fatPLoS One201057e1149220628553
  • BhaskaraSChylaBJAmannJMDeletion of histone deacetylase 3 reveals critical roles in S phase progression and DNA damage controlMol Cell2008301617218406327
  • De ZoetenEFWangLSaiHInhibition of HDAC9 increases T regulatory cell function and prevents colitis in miceGastroenterology2010138258359419879272
  • KotianSLiyanarachchiSZelentAHistone deacetylases 9 and 10 are required for homologous recombinationJ Biol Chem. Epub 2011 Jan 18.
  • KellyGA review of the sirtuin system, its clinical implications, and the potential role of dietary activators like resveratrol: part 1Altern Med Rev201015324526321155626
  • ZhangYKwonSYamaguchiTMice lacking histone deacetylase 6 have hyperacetylated tubulin but are viable and develop normallyMol Cell Biol20082851688170118180281
  • MaiAAltucciLEpi-drugs to fight cancer: from chemistry to cancer treatment, the road aheadInt J Biochem Cell Biol200941119921318790076
  • MarksPADokmanovicMHistone deacetylase inhibitors: discovery and development as anticancer agentsExpert Opin Investig Drugs2005141214971511
  • BertrandPInside HDAC with HDAC inhibitorsEur J Med Chem20104562095211620223566
  • Yurek-GeorgeACecilARMoAHThe first biologically active synthetic analogues of FK228, the depsipeptide histone deacetylase inhibitorJ Med Chem200750235720572617958342
  • KhanNJeffersMKumarSDetermination of the class and isoform selectivity of small-molecule histone deacetylase inhibitorsBiochem J2008409258158917868033
  • KrennHrubecKMarshallBLHedglinMDesign and evaluation of ‘linkerless’ hydroxamic acids as selective HDAC8 inhibitorsBioorg Med Chem Lett200717102874287817346959
  • EstiuGGreenbergEHarrisonCBStructural origin of selectivity in class II-selective histone deacetylase inhibitorsJ Med Chem200851102898290618412327
  • TaoriKPaulVJLueschHStructure and activity of largazole, a potent antiproliferative agent from the Floridian marine cyanobacterium Symploca spJ Am Chem Soc200813061806180718205365
  • HuhtiniemiTSuuronenTLahtela-KakkonenMNε-Modified lysine containing inhibitors for SIRT1 and SIRT2Bioorg Med Chem201018155616562520630764
  • HuhtiniemiTWittekindtCLaitinenTComparative and pharmacophore model for deacetylase SIRT1J Comput Aided Mol Des200620958959917103016
  • ElautGTörökGVinkenMMajor phase I biotransformation pathways of Trichostatin A in rat hepatocytes and in rat and human liver microsomesDrug Metab Dispos200230121320132812433798
  • EbbelENLeymarieNSchiavoSIdentification of phenylbutyrate-generated metabolites in Huntington disease patients using parallel liquid chromatography/electrochemical array/mass spectrometry and off-line tandem mass spectrometryAnalytical Biochem20103992152161
  • PariseRAHolleranJLBeunerJHA liquid chromatography–electrospray ionization tandem mass spectrometric assay for quantitation of the histone deacetylase inhibitor, vorinostat (suberoylanilide hydroxamicacid, SAHA), and its metabolites in human serumJ Chrom B20068402108115
  • DuLMussonDGWangAQStability studies of vorinostat and its two metabolites in human plasma, serum and urineJ Pharm Biomed Anal200642555656416824724
  • FurumaiRMatsuyamaAKobashiNFK228 (depsipeptide) as a natural prodrug that inhibits class I histone deacetylasesCancer Res200262174916492112208741
  • XiaoJJByrdJMarcucciGIdentification of thiols and glutathione conjugates of depsipeptide FK228 (FR901228), a novel histone protein deacetylase inhibitor, in the bloodRapid Commun Mass Spectrom200317875776612672127
  • ShiragaTTozukaZIshimuraRIdentification of cytochrome P450 enzymes involved in the metabolism of FK228, a potent histone deacetylase inhibitor, in human liver microsomesBiol Pharm Bull200528112412915635176
  • KimHMOhSJParkSKIn vitro metabolism of KBH-A40, a novel delta-lactam-based histone deacetylase (HDAC) inhibitor, in human liver microsomes and serumXenobiotica200838328129318274957
  • FonsiMFioreFJonesPMetabolism-related liabilities of a potent histone deacetylase (HDAC) inhibitor and relevance of the route of administration on its metabolic fateXenobiotica2009391072273719569735
  • PeartMJSmythGKvan LaarRKIdentification and functional significance of genes regulated by structurally different histone deacetylase inhibitorsPNAS2005102103697370215738394
  • EllisLPanYSmythGKHistone deacetylase inhibitor panobinostat induces clinical responses with associated alterations in gene expression profiles in cutaneous T-cell lymphomaClin Cancer Res200814144500451018628465
  • KatoNTanakaJSugitaJRegulation of the expression of MHC class I-related chain A, B (MICA, MICB) via chromatin remodeling and its impact on the susceptibility of leukemic cells to the cytotoxicity of NKG2D-expressing cellsLeukemia200721102103210817625602
  • VoDDPrinsRMBegleyJLEnhanced antitumor activity induced by adoptive T-cell transfer and adjunctive use of the histone deacetylase inhibitor LAQ824Cancer Res200969228693869919861533
  • CameronEEBachmanKEMyöhänenSSynergy of demethylation and histone deacetylase inhibition in the re-expression of genes silenced in cancerNat Genet19992111031079916800
  • AppelbaumFRBaerMRCarabasiMHNCCN Practice guidelines for acute myelogenous leukemiaOncology20001411A536111195419
  • SnykersSVinkenMRogiersVDifferential role of epigenetic modulators in malignant and normal stem cells: a novel tool in preclinical in vitro toxicology and clinical therapyArch Toxicol200781853354417387455
  • MarksPAMillerTRichonVMHistone deacetylasesCurr Opin Pharmacol20033434435112901942
  • DiGiuseppeJAWengLJYuKHPhenylbutyrate-induced G1 arrest and apoptosis in myeloid leukemia cells: structure-function analysisLeukemia19991381243125310450753
  • CarducciMANelsonJBChan-TackKMPhenylbutyrate induces apoptosis in human prostate cancer and is more potent than phenylacetateClin Cancer Res1996223793879816181
  • ZhangXWeiLYangYYuQSodium 4-phenylbutyrate induces apoptosis of human lung carcinoma cells through activating JNK pathwayJ Cell Biochem200493481982915389886
  • GorospeMShackSGuytonKZUp-regulation and functional role of p21Waf1/Cip1 during growth arrest of human breast carcinoma MCF-7 cells by phenylacetateCell Growth Differ1996712160916158959328
  • LiuLHudginsWRMillerACTranscriptional upregulation of TGF-α by phenylacetate and phenylbuytrate is associated with differentiation of human melanoma cellsCytokine1995754494567578983
  • HanSWadaRKSidellNDifferentiation of human neuroblastoma by phenylacetate is mediated by peroxisome proliferatoractivated receptor gammaCancer Res200161103998400211358817
  • CarducciMANelsonJBChan-TackKMPhenylbutyrate induces apoptosis in human prostate cancer and is more potent than phenylacetateClin Cancer Res1996223793879816181
  • BrusilowSWPhenylacetylglutamine may replace urea as a vehicle for waste nitrogen excretionPediatr Res19912921471502014149
  • PhuphanichSBakerSDGrossmanSAOral sodium phenylbutyrate in patients with recurrent malignant gliomas: a dose escalation and pharmacologic studyNeuro Oncol20057217718215831235
  • CarducciMAGilbertJBowlingMKA phase I clinical and pharmacological evaluation of sodium phenylbutyrate on an 120-h infusion scheduleClin Cancer Res20017103047305511595694
  • GilbertJBakerSDBowlingMKA phase I dose escalation and bioavailability study of oral sodium phenylbutyrate in patients with refractory solid tumor malignanciesClin Cancer Res2001782292230011489804
  • CamachoLHOlsonJTongWPPhase I dose escalation clinical trial of phenylbutyrate sodium administered twice daily to patients with advanced solid tumorsInvest New Drugs200725213113817053987
  • GoreSDWengLJZhaiSImpact of prolonged infusions of the putative differentiating agent sodium phenylbutyrate on myelodysplastic syndromes and acute myeloid leukemiaClin Cancer Res20028496397011948101
  • MaslakPChanelSCamachoLHPilot study of combination transcriptional modulation therapy with sodium phenylbutyrate and 5-azacytidine in patients with acute myeloid leukemia or myelodysplastic syndromeLeukemia200620221221716357841
  • GilbertJBakerSDDonehowerRMethytransferase (MT) activity and gene expression in tumor biopsies from patients enrolled in a Phase I study of the MT inhibitor, 5-azacytidine (5AC), and the histone deacetylase inhibitor, phenylbutyrate (PB), in refractory solid tumorsProc Am Soc Clin Onc.200187a
  • SungMWWaxmanSCombination of cytotoxicdifferentiation therapy with 5-fluorouracil and phenylbutyrate in patients with advanced colorectal cancerAnticancer Res2007272995100117465233
  • RephaeliARabizadehEAviramADerivatives of butyric acid as potential anti-neoplastic agentsInt J Cancer199149166721874573
  • SchwartzBAvivi-GreenCPolak-CharconSSodium butyrate induces retinoblastoma protein dephosphorylation, p16 expression and growth arrest of colon cancer cellsMol Cell Biochem19981881–221309823007
  • MandalMAdamLKumarRRedistribution of activated caspase-3 to the nucleus during butyric acid-induced apoptosisBiochem Biophys Res Commun1999260377578010403841
  • RabizadehEShaklaiMNudelmanARapid alteration of c-myc and c-jun expression in leukemic cells induced to differentiate by a butyric acid prodrugFEBS Lett199332832252298348968
  • RabizadehEBaireyOAviramADoxorubicin and a butyric acid derivative effectively reduce levels of Bcl-2 protein in the cells of chronic lymphocytic leukemia patientEur J Haematol200166426327111380606
  • PatnaikARowinskyEKVillalonaMAA phase I study of pivaloyloxymethyl butyrate, a prodrug of the differentiating agent butyric acid, in patients with advanced solid malignanciesClin Cancer Res2002872142214812114414
  • ReidTValoneFLiperaWPhase II trial of the histone deacetylase inhibitor pivaloyloxymethyl butyrate (Pivanex, AN-9) in advanced non-small cell lung cancerLung Cancer200445338138615301879
  • LoscherWBasic pharmacology of valproate: a review after 35 years of clinical use for the treatment of epilepsyCNS Drugs2002161066969412269861
  • PeruccaEPharmacological and therapeutic properties of valproate: a summary after 35 years of clinical experienceCNS Drugs2002161069571412269862
  • MarchionDCBicakuEDaudAIValproic acid alters chromatin structure by regulation of chromatin modulation proteinsCancer Res20056593815382215867379
  • JungGAYoonJYMoonBSValproic acid induces differentiation and inhibition of proliferation in neural progenitor cells via the beta-catenin-Ras-ERK-p21Cip/WAF1 pathwayBMC Cell Biol20089667819068119
  • GottlicherMMinucciSZhuJValproic acid defines a novel class of HDAC inhibitors inducing differentiation of transformed cellsEMBO J200120246969697811742974
  • GurvichNTsygankovaOMMeinkothJLHistone deacetylase is a target of valproic acid-mediated cellular differentiationCancer Res20046431079108614871841
  • BaconCLGallagherHCHaugheyJCAntiproliferative action of valproate is associated with aberrant expression and nuclear translocation of cyclin D3 during the C6 glioma G1 phaseJ Neurochem2002831121912358724
  • WerlingUSiehlerSLitfinMInduction of differentiation in F9 cells and activation of peroxisome proliferator-activated receptor delta by valproic acid and its teratogenic derivativesMol Pharmacol20015951269127611306712
  • KawagoeRKawagoeHSanoKValproic acid induces apoptosis in human leukemia cells by stimulating both caspase dependent and -independent apoptotic signaling pathwaysLeuk Res200226549550211916526
  • TangRFaussatAMMajdakPValproic acid inhibits proliferation and induces apoptosis in acute myeloid leukemia cells expressing P-gp and MRP1Leukemia20041871246125115116123
  • IchiyamaTOkadaKLiptonJMSodium valproate inhibits production of TNF-α and IL-6 and activation of NF-κBBrain Res20008571–224625110700573
  • SiitonenTKoistinenPSavolainenERIncrease in Ara-C cytotoxicity in the presence of valproate, a histone deacetylase inhibitor, is associated with the concurrent expression of cyclin D1 and p27(Kip 1) in acute myeloblastic leukemia cellsLeuk Res200529111335134215936818
  • CiminoGLo-CocoFFenuSSequential valproic acid/Alltrans retinoic acid treatment reprograms differentiation in refractory and highrisk acute myeloid leukemiaCancer Res200666178903891116951208
  • ValentiniAGravinaPFedericiGValproic acid induces apoptosis, p16INK4A upregulation and sensitization to chemotherapy in human melanoma cellsCancer Biol Ther20076218519117218782
  • AtmacaAAl-BatranSEMaurerAValproic acid (VPA) in patients with refractory advanced cancer: a dose escalating Phase I clinical trialBritish J Cancer2007972177182
  • BugGRitterMWassmannBClinical trial of valproic acid and all-trans retinoic acid in patients with poor-risk acute myeloid leukemiaCancer2005104122717272516294345
  • KuendgenAKnippSFoxFResults of a Phase 2 study of valproic acid alone or in combination with alltrans retinoic acid in 75 patients with myelodysplastic syndrome and relapsed or refractory acute myeloid leukemiaAnn Hematol200584Suppl 1616616270213
  • PilatrinoCCilloniDMessaEIncrease in platelet count in older, poor-risk patients with acute myeloid leukemia or myelodysplastic syndrome treated with valproic acid and all-trans retinoic acidCancer2005104110110915895376
  • RaffouxEChaibiPDombretHValproic acid and all-trans retinoic acid for the treatment of elderly patients with acute myeloid leukemiaHaematologica200590798698815996941
  • DuprezELillehaugJRNaoeTcAMP signalling is decisive for recovery of nuclear bodies (PODs) during maturation of RA-resistant t(15;17) promyelocytic leukemia NB4 cells expressing PML-RAR alphaOncogene19961211245124598649787
  • KuendgenASchmidMSchlenkRThe histone deacetylase (HDAC) inhibitor valproic acid as monotherapy or in combination with all-trans retinoic acid in patients with acute myeloid leukemiaCancer2006106111211916323176
  • HuangSBrandtSJmSin3A regulates murine erythroleukemia cell differentiation through association with the TAL1 (or SCL) transcription factorMol Cell Biol20002062248225910688671
  • WatamotoKTowatariMOzawaYAltered interaction of HDAC5 with GATA-1 during MEL cell differentiationOncogene200322579176918414668799
  • SiitonenTTimonenTJuvonenEValproic acid combined with 13-cis retinoic acid and 1,25-dihydroxyvitamin D3 in the treatment of patients with myelodysplastic syndromesHaematologica20079281119112217650442
  • SantiniVFerriniPRDifferentiation therapy of myelodysplastic syndromes: fact or fiction?Br J Heamatol1998102511241138
  • Garcia-ManeroGKantarjianHMSanchez-GonzalezBPhase 1/2 study of the combination of 5-aza-2′-deoxycytidine with valproic acid in patients with leukemiaBlood2006108103271327916882711
  • BlumWKlisovicRBHackansonBPhase I study of decitabine alone or in combination with valproic acid in acute myeloid leukemiaJ Clin Oncol200725253884389117679729
  • BraitehFSorianoAOGarcia-ManeroGPhase I study of epigenetic modulation with 5-azacytidine and valproic acid in patients with advanced cancersClin Cancer Res200814196296630118829512
  • SorianoAOYangHFaderlSSafety and clinical activity of the combination of 5-azacytidine, valproic acid, and all-trans retinoic acid in acute myeloid leukemia and myelodysplastic syndromeBlood200711072302230817596541
  • MünsterPMarchionDBicakuEClinical and biological effects of valproic acid as a histone deacetylase inhibitor on tumor and surrogate tissues: Phase I/II trial of valproic acid and epirubicin/FECClin Cancer Res20091572488249619318486
  • MünsterPMarchionDBicakuEPhase I trial of histone deacetylase inhibition by valproic acid followed by the topoisomerase II inhibitor epirubicin in advanced solid tumors: a clinical and translational studyJ Clin Oncology2007251519791985
  • DaudAIDawsonJDeContiRCPotentiation of a topoisomerase I inhibitor, karenitecin, by the histone deacetylase inhibitor valproic acid in melanoma: translational and Phase I/II clinical trialClin Cancer Res20091572479248919318485
  • RoccaAMinucciSTostiGA Phase I–II study of the histone deacetylase inhibitor valproic acid plus chemoimmunotherapy in patients with advanced melanomaBritish J Cancer200910012836
  • FachettiFPrevidiSBallariniMModulation of pro- and anti-apoptotic factors in human melanoma cells exposed to histone deacetylase inhibitorsApoptosis20049557358215314285
  • Chavez-BlancoASegura-PachecoBPerez-CardenasEHistone acetylation and histone deacetylase activity of magnesium valproate in tumor and peripheral blood of patients with cervical cancer. A Phase I studyMol Cancer2005412216001982
  • CandelariaMGallardo-RinconDArceCA Phase II study of epigenetic therapy with hydralazine and magnesium valproate to overcome chemotherapy resistance in refractory solid tumorsAnn Oncol20071891529153817761710
  • ParulekarWREinsenhauerEANovel endpoints and design of early clinical trialsAnnal Oncol200213Suppl 4139143
  • HunsbergerSRubinsteinLVDanceyJDose escalation trial designs based on a molecularly targeted endpointStat Med200524142171218115909289
  • Segura-PachecoBPerez-CardenasETaja-ChayebLGlobal DNA hypermethylation-associated cancer chemotherapy resistance and its reversion with the demethylating agent hydralazineJ Transl Med200643216893460
  • RichonVMWebbYMergerRSecond generation hybrid polar compounds are potent inducers of transformed cell differentiationProc Natl Acad Sci U S A19969312570557088650156
  • ButlerLMAgusDBScherHLSuberoylanilide hydroxamic acid, an inhibitor of histone deacetylase, suppresses the growth of prostate cancer cells in vitro and in vivoCancer Res200060785165517011016644
  • FinninMSDonigianJRCohenAStructures of a histone deacetylase homologue bound to the TSA and SAHA inhibitorsNature1999401674918819310490031
  • YinDOngJMHuJSuberoylanilide hydroxamic acid, a histone deacetylase inhibitor: effects on gene expression and growth of glioma cells in vitro and in vivoClin Cancer Res20071331045105217289901
  • MitsiadesCSPoulakiVMcMullanCNovel histone deacetylase inhibitors in the treatment of thyroid cancerClin Cancer Res200511103958396515897598
  • MunsterPNTroso-SandovalTRosenNThe histone deacetylase inhibitor suberoylanilide hydroxamic acid induces differentiation of human breast cancer cellsCancer Res200161238492849711731433
  • BaliPPranpatMSwabyRActivity of suberoylanilide hydroxamic acid against human breast cancer cells with amplification of her-2Clin Cancer Res200511176382638916144943
  • KomatsuNKawamataNTakeuchiSSAHA, a HDAC inhibitor, has profound anti-growth activity against non-small cell lung cancer cellsOncol Rep200615118719116328054
  • ButlerLMAgusDBScherHISuberoylanilide hydroxamic acid, an inhibitor of histone deacetylase, suppresses the growth of prostate cancer cells in vitro and in vivoCancer Res200060185165517011016644
  • DietrichCGreenbergVLDesimoneCPSuberoylanilide hydroxamic acid potentiates paclitaxel-induced apoptosis in ovarian cancer cell linesGynecol Oncol2006116112613019875160
  • KellyWKRichonVMO’ConnorOPhase I clinical trial of histone deacetylase inhibitor: suberoylanilide hydroxamic acid administered intravenouslyClin Cancer Res.2003910 Pt 13578358814506144
  • KrugLMCurleyTSchwartzLPotential role of histone deacetylase inhibitors in mesothelioma: clinical experience with suberoylanilide hydroxamic acidClin Lung Cancer20067425726116512979
  • KellyWKO’ConnorOAKrugLMPhase I study of an oral histone deacetylase inhibitor, suberoylanilide hydroxamic acid, in patients with advanced cancerJ Clin Oncol200523173923393115897550
  • Garcia-ManeroGYangnHBueso-RamosCPhase 1 study of the histone deacetylase inhibitor vorinostat (suberoylanilide hydroxamic acid [SAHA]) in patients with advanced leukemias andmyelodysplastic syndromesBlood200811131060106617962510
  • ModesittSCSillMHoffmanJSA Phase II study of vorinostat in the treatment of persistent or recurrent epithelial ovarian or primary peritoneal carcinoma: a Gynecologic Oncology Group studyGynecol Oncol2008109218218618295319
  • VansteenkisteJVan CutsemEDumezHEarly Phase II trial of oral vorinostat in relapsed or refractory breast, colorectal, or nonsmall cell lung cancerInvest New Drugs200826548348818425418
  • BlumenscheinGRJrKiesMSPapadimitrakopoulouVAPhase II trial of the histone deacetylase inhibitor vorinostat (Zolinza, suberoylanilide hydroxamic acid, SAHA) in patients with recurrent and/or metastatic head and neck cancerInvest New Drugs2008261818717960324
  • LuuTHMorganRJLeongLA phase II trial of vorinostat (suberoylanilide hydroxamic acid) in metastatic breast cancer: a California Cancer Consortium studyClin Cancer Res200814217138714218981013
  • GalanisEJaeckleKAMaurerMJPhase II trial of vorinostat in recurrent glioblastoma multiforme: a north central cancer treatment group studyJ Clin Oncol200927122052205819307505
  • WoyachJAKloosRTRingelMDLack of therapeutic effect of the histone deacetylase inhibitor vorinostat in patients with metastatic radioiodine-refractory thyroid carcinomaJ Clin Endocrinol Metab200994116417018854394
  • RamalingamSSPariseRARamanathanRKPhase I and pharmacokinetic study of vorinostat, a histone deacetylase inhibitor, in combination with carboplatin and paclitaxel for advanced solid malignanciesClin Cancer Res200713123605361017510206
  • PlumbJAFinnPWWilliamsRJPharmacodynamic response and inhibition of growth of human tumor xenografts by the novel histone deacetylase inhibitor PXD101Mol Cancer Ther20032872172812939461
  • GimsingPBelinostat: a new broad acting antineoplastic histone deacetylase inhibitorExpert Opin Investig Drugs2009184501508
  • GianXLaRochelleWJAraGActivity of PXD101, a histone deacetylase inhibitor, in preclinical ovarian cancer studiesMol Cancer Ther2006582086209516928830
  • MonksAHoseCDPezzoliPGene expression-signature of belinostat in cell lines is specific for histone deacetylase inhibitor treatment, with a corresponding signature in xenograftsAnticancer Drugs200920868269219606018
  • WarrenKEMcCullyCDvingeHPlasma and cerebrospinal fluid pharmacokinetics of the histone deacetylase inhibitor, belinostat (PXD101), in non-human primatesCancer Chemother Pharmacol200862343343717960383
  • TumberACollinsLSPetersenKThe histone deacetylase inhibitor PXD101 synergises with 5-Xuorouracil to inhibit colon cancer cell growth in vitro and in vivoCancer Chemother Pharmacol20076027528317124594
  • SteeleNLPlumbJAVidalLA Phase 1 pharmacokinetic and pharmacodynamic study of the histone deacetylase inhibitor belinostat in patients with advanced solid tumorsClin Cancer Res200814380481018245542
  • TakadaMKataokaAToiMA close association between alteration in growth kinetics by neoadjuvant chemotherapy and survival outcome in primary breast cancerInt J Oncol200425239740515254737
  • GimsingPHansenMKnudsenLMA phase I clinical trial of the histone deacetylase inhibitor belinostat in patients with advanced hematological neoplasiaEur J Hematol2008813170176
  • RamalingamSSBelaniCPRuelCPhase II study of belinostat (PXD101), a histone deacetylase inhibitor, for second line therapy of advanced malignant pleural mesotheliomaJ Thorac Oncol2009419710119096314
  • MackayHJHirteHColganTPhase II trial of the histone deacetylase inhibitor belinostat in women with platinum resistant epithelial ovarian cancer and micropapillary (LMP) ovarian tumoursEur J Cancer20104691573157920304628
  • GolayJCuppiniLLeoniFThe histone deacetylase inhibitor ITF2357 has anti-leukemic activity in vitro and in vivo and inhibits IL-6 and VEGF production by stromal cellsLeukemia20072191892190017637810
  • VivianiSBonfanteVFasolaCPhase II study of the histonedeacetylase inhibitor ITF2357 in relapsed/refractory Hodgkin’s lymphoma patientsJ Clin Oncol.200826 abstract 8532.
  • GalliMSalmoiraghiSGolayJA Phase II multiple dose clinical trial of histone deacetylase inhibitor ITF2357 in patients with relapsed or progressive multiple myelomaAnn Hematol201089218519019633847
  • Carlo-StellaCGuidettiAVivianiSSafety and clinical activity of the histone deacetylase inhibitor givinostat in combination with meclorethamine in relapsed/refractory Hodgkin lymphoma (HL)J Clin Oncol.201028 abstract 3068.
  • QianDZKatoYShabbeerSTargeting tumor angiogenesis with histone deacetylase inhibitors: the hydroxamic acid derivative LBH589Clin Cancer Res200612263464216428510
  • PrinceHMBishtonMJJohnstoneRWPanobinostat (LBH589): a potent pan-deacetylase inhibitor with promising activity against hematologic and solid tumorsFuture Oncol20095560161219519200
  • GilesFFischerTCortesJPhase I Study of Intravenous LBH589, a novel cinnamic hydroxamic acid analogue histone deacetylase inhibitor, in patients with refractory hematologic malignanciesClin Cancer Res200612154628463516899611
  • RathkopfDWongBYRossRWA Phase I study of oral panobinostat alone and in combination with docetaxel in patients with castration-resistant prostate cancerCancer Chemother Pharmacol201066118118920217089
  • RemiszewskiSWThe discovery of NVPLAQ824: from concept to clinicCurr Med Chem200310222393240214529481
  • HurtubiseAMomparlerRLEffect of histone deacetylase inhibitor LAQ824 on antineoplastic action of 5-Aza-2-deoxycytidine (decitabine) on human breast carcinoma cellsCancer Chemother Pharmacol200658561862516783580
  • De BonoJSKristeleitRTolcherAPhase I pharmacokinetic and pharmacodynamic study of LAQ824, a hydroxamate histone deacetylase inhibitor with a heat shock protein-90 inhibitory profile, in patients with advanced solid tumorsClin Cancer Res200814206663667318927309
  • KristeleitRSTandyDAtadjaPEffects of the histone deacetylase inhibitor (HDACI) LAQ824 on histone acetylation, Hsp70 and c-Raf in peripheral blood lymphocytes from patients with advanced solid tumours enrolled in a phase I clinical trialJ Clin Oncol.200422 abstract 3023.
  • OttmannOGDeangeloDJStoneRMA Phase I, pharmacokinetic (PK) and pharmacodynamic (PD) study of a novel histone deacetylase inhibitor LAQ824 in patients with hematologic malignanciesJ Clin Oncol.200422 abstract 3024.
  • ChoyECaoYHornicekFEffect of histone deacetylase inhibitor (HDACI) PCI-24781 on chemotherapy-induced apoptosis in multidrug-resistant sarcoma cell linesJ Clin Oncol.201028 abstract 10089.
  • UndeviaSDJanischLSchilskyRLPhase I study of the safety, pharmacokinetics (PK) and pharmacodynamics (PD) of the histone deacetylase inhibitor (HDACi) PCI-24781J Clin Oncol.200826 abstract 14514.
  • JaboinJWildJHamidiHMS-27-275, an inhibitor of histone deacetylase, has marked in vitro and in vivo antitumor activity against pediatric solid tumorsCancer Res200262216108611512414635
  • LucasDMDavisMEParthunMRThe histone deacetylase inhibitor MS-275 induces caspase-dependent apoptosis in B-cell chronic lymphocytic leukemia cellsLeukemia20041871207121415116122
  • RosatoRRAlmenaraJAGrantSThe 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 1Cancer Res200363133637364512839953
  • LeeBIParkSHKimJWMS-275, a histone deacetylase inhibitor, selectively induces transforming growth factor beta type II receptor expression in human breast cancer cellsCancer Res200161393193411221885
  • AcharyaMRSparreboomASausvilleEAInterspecies differences in plasma protein binding of MS-275, a novel histone deacetylase inhibitorCancer Chemother Pharmacol200657327528116028097
  • RyanQCHeadleeDAcharyaMPhase I and pharmacokinetic study of MS-275, a histone deacetylase inhibitor, in patients with advanced and refractory solid tumors or lymphomaJ Clin Oncol200523173912392215851766
  • KummarSGutierrezMGardnerERPhase I trial of MS-275, a histone deacetylase inhibitor, administered weekly in refractory solid tumors and lymphoid malignanciesClin Cancer Res20071318 Pt 15411541717875771
  • GojoIJiemjitATrepelJBPhase 1 and pharmacologic study of MS-275, a histone deacetylase inhibitor, in adults with refractory and relapsed acute leukemiasBlood200710972781279017179232
  • GoreLRothenbergMLO’BryantCLA phase I and pharmacokinetic study of the oral histone deacetylase inhibitor, MS-275, in patients with refractory solid tumors and lymphomasClin Cancer Res200814144517452518579665
  • HauschildATrefzerUGarbeCMulticenter phase II trial of the histone deacetylase inhibitor pyridylmethyl-N-{4-[(2-aminophenyl)-carbamoyl]-benzyl}-carbamate in pretreated metastatic melanomaMelanoma Res200818427427818626312
  • ZhouNMoradeiORaeppelSDiscovery of N-(2-aminophenyl)-4-[(4-pyridin-3-ylpyrimidin-2-ylamino)methyl]benzamide (MGCD0103), an orally active histone deacethylase inhibitorJ Med Chem200851144072407518570366
  • FournelMBonfilsCHouYMGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity in vitro and in vivoMol Cancer Ther20087475976818413790
  • SiuLLPiliRDuranIPhase I study of MGCD0103 given as a three-times-per-week oral dose in patients with advanced solid tumorsJ Clin Oncol200826121940194718421048
  • Garcia-ManeroGAssoulineSCortesJPhase 1 study of the oral isotype specific histone deacetylase inhibitor MGCD0103 in leukemiaBlood2008112498198918495956
  • LancetJENicholsGAssoulineSA Phase I study of MGCD0103 given as a twice weekly oral dose in patients with advanced leukemias or myelodysplastic syndromes (MDS)J Clin Oncol.200725 abstract 2516.
  • BociekRGKuruvillaGJProBIsotype-selective histone deacetylase (HDAC) inhibitor MGCD0103 demonstrates clinical activity and safety in patients with relapsed/refractory classical Hodgkin Lymphoma (HL)J Clin Oncol.200826 abstract 8507.
  • MartellREYounesAAssoulineSEPhase II study of MGCD0103 in patients with relapsed follicular lymphoma (FL): Study reinitiation and update of clinical efficacy and safetyJ Clin Oncol.201028 abstract 8086.
  • BergerMRBischoffHFritschiESynthesis, toxicity, and therapeutic efficacy of 4-amino-N-(2-aminophenyl) benzamide: a new compound preferentially active in slowly growing tumorsCancer Treat Rep19856912141514243841025
  • KrakerAJMizzenCAHartlBGModulation of histone acetylation by [4-(acetylamino)-N-(2-amino-phenyl) benzamide] in HCT-8 colon carcinomaMol Cancer Ther20032440140812700284
  • PrakashSFosterBJMeyerMChronic oral administration of CI-994: a Phase 1 studyInvest New Drugs200119111111291827
  • UndeviaSDKindlerHLJanischLA Phase I study of the oral combination of CI-994, a putative histone deacetylase inhibitor, and capecitabineAnn Oncol200415111705171115520075
  • RichardsDABoehmKAWaterhouseDMGemcitabine plus CI-994 offers no advantage over gemcitabine alone in the treatment of patients with advanced pancreatic cancer: results of a phase II randomized, double-blind, placebo-controlled, multicenter studyAnn Oncol20061771096110216641168
  • UedaHMandaTMatsumotoSFR901228, a novel antitumor bicyclic depsipeptide produced by Chromobacterium violaceum No. 968, III: antitumor activities on experimental tumors in miceJ Antibiot19944733153238175484
  • UedaHNakajimaHHoriYFR901228, a novel antitumor bicyclic depsipeptide produced by Chromobacterium violaceum No. 968. I. Taxonomy, fermentation, isolation, physicochemical and biological properties, and antitumor activityJ Antibiot19944733013107513682
  • YuXDWangSYChenGAApoptosis induced by depsipeptide FK228 coincides with inhibition of survival signaling in lung cancer cellsCancer J200713210511317476138
  • SandorVRobbinsARRobeyRFR901228 causes mitotic arrest but does not alter microtubule polymerizationAnticancer Drugs2000111144545411001385
  • SandorVSenderowiczAMertinsSP21-dependent G(1) arrest with downregulation of cyclin D1 and upregulation of cyclin E by the histone deacetylase inhibitor FR901228Br J Cancer200083681782510952788
  • WangRBrunnerTZhangLFungal metabolite FR901228 inhibits c-Myc and Fas ligand expressionOncogene19981712150315089794227
  • YuXGuoZSMarcuMGModulation of p53, ErbB1, ErbB2, and Raf-1 expression in lung cancer cells by depsipeptide FR901228J Natl Cancer Inst200294750451311929951
  • RajgolikarGChanKKWangHCEffects of a novel antitumor depsipeptide, FR901228, on human breast cancer cellsBreast Cancer Res Treat199851129389877027
  • KitazonoMRobeyRZhanZLow concentrations of the histone deacetylase inhibitor, depsipeptide (FR901228), increase expression of the Na/I symporter and iodine accumulation in poorly differentiated thyroid carcinoma cellsJ Clin Endocrinol Metab20018673430343511443220
  • AronJLParthunMRMarcucciGDepsipeptide (FR901228) induces histone acetylation and inhibition of histone deacetylase in chronic lymphocytic leukemia cells concurrent with activation of caspase 8-mediated apoptosis and down-regulation of c-FLIP proteinBlood2003102265265812649137
  • WeiserTSGuoZSOhnmachtGASequential 5-aza-2 deoxycytidine-depsipeptide FR901228 treatment induces apoptosis preferentially in cancer cells and facilitates their recognition by cytolytic T lymphocytes specific for NY-ESO-1J Immunother200124215116111265773
  • SteinerFAHongJAFischetteMRSequential 5-Aza 2-deoxycytidine/depsipeptide FK228 treatment induces tissue factor pathway inhibitor 2 (TFPI-2) expression in cancer cellsOncogene200524142386239715735751
  • KlisovicMIMaghrabyEAParthunMRDepsipeptide (FR 901228) promotes histone acetylation, gene transcription, apoptosis and its activity is enhanced by DNA methyltransferase inhibitors in AML1/ETO-positive leukemic cellsLeukemia200317235035812592335
  • SasakawaYNaoeYSogoNMarker genes to predict sensitivityto FK228, a histone deacetylase inhibitorBiochem Pharmacol200569460361615670579
  • PiekarzRLFryeRTurnerMPhase II multi-institutional trial of the histone deacetylase inhibitor romidepsin as monotherapy for patients with cutaneous T-cell lymphomaJ Clin Oncol200927325410541719826128
  • WooSGardnerERChenXPopulation pharmacokinetics of romidepsin in patients with cutaneous T-cell lymphoma and relapsed peripheral T-cell lymphomaClin Cancer Res20091541496150319228751
  • MarshallJLRizviNKauhJA Phase I trial of depsipeptide (FR901228) in patients with advanced cancerJ Exp Ther Oncol20022632533212440223
  • SandorVBakkesSRobeyRWPhase I trial of the histone deacetylase inhibitor, depsipeptide (FR901228, NSC 630176), in patients with refractory neoplasmsClin Cancer Res20028371872811895901
  • ByrdJCMarcucciGParthunMRA phase 1 and pharmacodynamic study of depsipeptide (FK228) in chronic lymphocytic leukemia and acute myeloid leukemiaBlood2005105395996715466934
  • FouladiMFurmanWLChinTPhase I study of depsipeptide in pediatric patients with refractory solid tumors: a Children’s Oncology Group reportJ Clin Oncol200624223678368516877737
  • KlimekVMFircanisSMaslakPTolerability, pharmacodynamics, and pharmacokinetics studies of depsipeptide (romidepsin) in patients with acute myelogenous leukemia or advanced myelodysplastic syndromesClin Cancer Res200814382683218245545
  • StadlerWMMargolinKFerberSA Phase II study of depsipeptide in refractory metastatic renal cell cancerClin Genitourin Cancer200651576016859580
  • ShahMHBinkleyPChanKCardiotoxicity of histone deacetylase inhibitor depsipeptide in patients with metastatic neuroendocrine tumorsClin Cancer Res200612133997400316818698
  • SchrumpDSFischetteMRNguyenDMClinical and molecular responses in lung cancer patients receiving RomidepsinClin Cancer Res200814118819818172270
  • SosmanJAAronsonFRSznolMConcurrent phase I trials of intravenous interleukin 6 in solid tumor patients: reversible dose-limiting neurological toxicityClin Cancer Res19973139469815535
  • MaloneyAWorkmanPHSP90 as a new therapeutic target for cancer therapy: the story unfoldsExpert Opin Biol Ther20022132411772336
  • BantscheffMHopfCSavitskiMMChemoproteomics profiling of HDAC inhibitors reveals selective targeting of HDAC complexes.Nat Biotechnol.2011 In press.