From discovery to the coming generation of histone deacetylase inhibitors.

No abstract is available for this paper.

• Publication year

  2003

• Venue

  Current Medicinal Chemistry

• Publication date

  2003-10-31

• Fields of study

  Biology, Medicine, Chemistry

• Identifiers
  DOI 10.2174/0929867033456602PMID 14529478
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• HDAC6 is a microtubule-associated deacetylase

  2002cited by this paper
• FK228 (depsipeptide) as a natural prodrug that inhibits class I histone deacetylases.

  2002cited by this paper
• In vivo destabilization of dynamic microtubules by HDAC6‐mediated deacetylation

  2002cited by this paper
• Molecular Cloning and Characterization of a Novel Histone Deacetylase HDAC10*

  2002cited by this paper
• Enzymatic activities of Sir2 and chromatin silencing.

  2001cited by this paper
• Potent histone deacetylase inhibitors built from trichostatin A and cyclic tetrapeptide antibiotics including trapoxin.

  2001cited by this paper
• Functional significance of histone deacetylase diversity.

  2001cited by this paper
• Negative control of p53 by Sir2alpha promotes cell survival under stress.

  2001cited by this paper
• Valproic acid defines a novel class of HDAC inhibitors inducing differentiation of transformed cells

  2001cited by this paper
• Inhibition of histone deacetylase activity enhances Fas receptor-mediated apoptosis in leukemic lymphoblasts

  2001cited by this paper
• 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

  2001cited by this paper
• The emerging role of class II histone deacetylases.

  2001cited by this paper
• Cloning and characterization of a histone deacetylase, HDAC9

  2001cited by this paper
• Trichostatin A is a histone deacetylase inhibitor with potent antitumor activity against breast cancer in vivo.

  2001cited by this paper
• Identification of a Class of Small Molecule Inhibitors of the Sirtuin Family of NAD-dependent Deacetylases by Phenotypic Screening*

  2001cited by this paper
• Identification of Components of the Murine Histone Deacetylase 6 Complex: Link between Acetylation and Ubiquitination Signaling Pathways

  2001cited by this paper
• hSIR2(SIRT1) functions as an NAD-dependent p53 deacetylase.

  2001cited by this paper
• Crystal structure of a SIR2 homolog-NAD complex.

  2001cited by this paper
• Site-Specific Acetylation by p300 or CREB Binding Protein Regulates Erythroid Krüppel-Like Factor Transcriptional Activity via Its Interaction with the SWI-SNF Complex

  2001cited by this paper
• The histone deacetylase inhibitor suberoylanilide hydroxamic acid induces differentiation of human breast cancer cells.

  2001cited by this paper
• Inhibitor of histone deacetylation, depsipeptide (FR901228), in the treatment of peripheral and cutaneous T-cell lymphoma: a case report.

  2001cited by this paper
• Butyrate suppression of colonocyte NF-kappa B activation and cellular proteasome activity.

  2001cited by this paper
• Active maintenance of mHDA2/mHDAC6 histone-deacetylase in the cytoplasm.

  2000cited by this paper
• Transcriptional silencing and longevity protein Sir2 is an NAD-dependent histone deacetylase

  2000cited by this paper
• Deacetylation of p53 modulates its effect on cell growth and apoptosis

  2000cited by this paper
• Acetylation regulates transcription factor activity at multiple levels.

  2000cited by this paper
• Acetylation of importin-alpha nuclear import factors by CBP/p300.

  2000cited by this paper
• Mechanism of cell cycle arrest caused by histone deacetylase inhibitors in human carcinoma cells.

  2000cited by this paper
• Silent information regulator 2 family of NAD- dependent histone/protein deacetylases generates a unique product, 1-O-acetyl-ADP-ribose.

  2000cited by this paper
• Histone deacetylase inhibitors: inducers of differentiation or apoptosis of transformed cells.

  2000cited by this paper
• Isolation of a novel histone deacetylase reveals that class I and class II deacetylases promote SMRT-mediated repression.

  2000cited by this paper
• Cloning and Characterization of a Novel Human Class I Histone Deacetylase That Functions as a Transcription Repressor*

  2000cited by this paper
• Acetylation of Histones and Transcription-Related Factors

  2000cited by this paper
• Acetylation: a regulatory modification to rival phosphorylation?

  2000cited by this paper
• The silencing protein SIR2 and its homologs are NAD-dependent protein deacetylases.

  2000cited by this paper
• Role of NAD(+) in the deacetylase activity of the SIR2-like proteins.

  2000cited by this paper
• Regulation of E2F1 activity by acetylation

  2000cited by this paper
• Chemoprevention of carcinogen-induced mammary tumorigenesis by the hybrid polar cytodifferentiation agent, suberanilohydroxamic acid (SAHA).

  1999cited by this paper
• Three proteins define a class of human histone deacetylases related to yeast Hda1p.

  1999cited by this paper
• Structures of a histone deacetylase homologue bound to the TSA and SAHA inhibitors

  1999cited by this paper
• Histone acetylases and deacetylases in cell proliferation.

  1999cited by this paper
• Identification of a New Family of Higher Eukaryotic Histone Deacetylases

  1999cited by this paper
• Sin meets NuRD and other tails of repression.

  1999cited by this paper
• Amide analogues of trichostatin A as inhibitors of histone deacetylase and inducers of terminal cell differentiation.

  1999cited by this paper
• HDAC4, a Human Histone Deacetylase Related to Yeast HDA1, Is a Transcriptional Corepressor

  1999cited by this paper
• Regulation of hormone-induced histone hyperacetylation and gene activation via acetylation of an acetylase.

  1999cited by this paper
• Neuronal differentiation of neuro 2a cells by inhibitors of cell cycle progression, trichostatin A and butyrolactone I.

  1999cited by this paper
• A synthetic inhibitor of histone deacetylase, MS-27-275, with marked in vivo antitumor activity against human tumors.

  1999cited by this paper
• Oxamflatin is a novel antitumor compound that inhibits mammalian histone deacetylase

  1999cited by this paper
• p53 Sites Acetylated In Vitro by PCAF and p300 Are Acetylated In Vivo in Response to DNA Damage

  1999cited by this paper
• Histone deacetylases: transcriptional repression with SINers and NuRDs.

  1999cited by this paper
• p21(WAF1) is required for butyrate-mediated growth inhibition of human colon cancer cells.

  1998cited by this paper
• DNA damage activates p53 through a phosphorylation-acetylation cascade.

  1998cited by this paper
• Histone acetylation and transcriptional regulatory mechanisms.

  1998cited by this paper
• FR901228, a potent antitumor antibiotic, is a novel histone deacetylase inhibitor.

  1998cited by this paper
• Co-activators and co-repressors in the integration of transcriptional responses.

  1998cited by this paper
• Fusion proteins of the retinoic acid receptor-α recruit histone deacetylase in promyelocytic leukaemia

  1998cited by this paper
• A class of hybrid polar inducers of transformed cell differentiation inhibits histone deacetylases.

  1998cited by this paper
• Roles of histone acetyltransferases and deacetylases in gene regulation

  1998cited by this paper
• Regulation of activity of the transcription factor GATA-1 by acetylation

  1998cited by this paper
• Distinct interactions of PML-RARalpha and PLZF-RARalpha with co-repressors determine differential responses to RA in APL.

  1998cited by this paper
• Role of the histone deacetylase complex in acute promyelocytic leukaemia

  1998cited by this paper
• Characterization of a human RPD3 ortholog, HDAC3.

  1998cited by this paper
• Drosophila CBP represses the transcription factor TCF to antagonize Wingless signalling

  1998cited by this paper
• Steroid receptor coactivator-1 is a histone acetyltransferase

  1997cited by this paper
• Activation of p53 sequence-specific DNA binding by acetylation of the p53 C-terminal domain.

  1997cited by this paper
• Fiber-derived butyrate and the prevention of colon cancer.

  1997cited by this paper
• Histone acetylation in chromatin structure and transcription

  1997cited by this paper
• Histone deacetylases associated with the mSin3 corepressor mediate mad transcriptional repression.

  1997cited by this paper
• A histone deacetylase inhibitor potentiates retinoid receptor action in embryonal carcinoma cells.

  1997cited by this paper
• A p300/CBP-associated factor that competes with the adenoviral oncoprotein E1A

  1996cited by this paper
• Tetrahymena histone acetyltransferase A: a homolog to yeast Gcn5p linking histone acetylation to gene activation.

  1996cited by this paper
• Apicidin: a novel antiprotozoal agent that inhibits parasite histone deacetylase.

  1996cited by this paper
• The transcriptional coactivators p300 and CBP are histone acetyltransferases.

  1996cited by this paper
• The TAF(II)250 subunit of TFIID has histone acetyltransferase activity.

  1996cited by this paper
• A Mammalian Histone Deacetylase Related to the Yeast Transcriptional Regulator Rpd3p

  1996cited by this paper
• The expression of a small fraction of cellular genes is changed in response to histone hyperacetylation.

  1996cited by this paper
• HDA1 and RPD3 are members of distinct yeast histone deacetylase complexes that regulate silencing and transcription.

  1996cited by this paper
• Trichostatin A and trapoxin: Novel chemical probes for the role of histone acetylation in chromatin structure and function

  1995cited by this paper
• Inhibition of maize histone deacetylases by HC toxin, the host-selective toxin of Cochliobolus carbonum.

  1995cited by this paper
• Trichostatin A induces morphological changes and gelsolin expression by inhibiting histone deacetylase in human carcinoma cell lines.

  1994cited by this paper
• Suppression of heat-shock protein synthesis by short-chain fatty acids and alcohols.

  1994cited by this paper
• Trapoxin, an antitumor cyclic tetrapeptide, is an irreversible inhibitor of mammalian histone deacetylase.

  1993cited by this paper
• Isolation and structural elucidation of new cyclotetrapeptides, trapoxins A and B, having detransformation activities as antitumor agents.

  1990cited by this paper
• Potent and specific inhibition of mammalian histone deacetylase both in vivo and in vitro by trichostatin A.

  1990cited by this paper
• Structural specificity for biological activity of trichostatin A, a specific inhibitor of mammalian cell cycle with potent differentiation-inducing activity in Friend leukemia cells.

  1990cited by this paper
• Reversible arrest of proliferation of rat 3Y1 fibroblasts in both the G1 and G2 phases by trichostatin A.

  1988cited by this paper
• Effects of trichostatins on differentiation of murine erythroleukemia cells.

  1987cited by this paper
• Studies on WF-3161, a new antitumor antibiotic.

  1983cited by this paper
• Different accessibilities in chromatin to histone acetylase.

  1979cited by this paper
• A new antifungal antibiotic, trichostatin.

  1976cited by this paper
• [Isolation and structural clarification of chlamydocin].

  1974cited by this paper
• Cytostatic activity of chlamydocin, a rapidly inactivated cyclic tetrapeptide.

  1974cited by this paper

• Natural Derivatives of Selective HDAC8 Inhibitors with Potent in Vivo Antitumor Efficacy against Breast Cancer.

  2024cites this paper
• Histone deacetylase 8 in focus: Decoding structural prerequisites for innovative epigenetic intervention beyond hydroxamates.

  2024cites this paper
• Cellular senescence with SASP in periodontal ligament cells triggers inflammation in aging periodontal tissue

  2023cites this paper
• Discovery of New Uracil and Thiouracil Derivatives as Potential HDAC Inhibitors

  2023cites this paper
• Loss of heterochromatin and retrotransposon silencing as determinants in oocyte aging

  2022influential citation
• Epigenetic underpinnings of inflammation: Connecting the dots between pulmonary diseases, lung cancer and COVID-19

  2021cites this paper
• 25th ANNIVERSARY OF CLONING BY SOMATIC-CELL NUCLEAR TRANSFER Epigenetic abnormalities associated with somatic cell nuclear transfer

  2021cites this paper
• The Selective Histone Deacetylase Inhibitor MI192 Enhances the Osteogenic Differentiation Efficacy of Human Dental Pulp Stromal Cells

  2021cites this paper
• Improved development of mouse somatic cell nuclear transfer embryos by chlamydocin analogues, class I and IIa histone deacetylase inhibitors†

  2021cites this paper
• In silico structure-based discovery of a SARS-CoV-2 main protease inhibitor

  2021cites this paper
• Histone Modifier Differentially Regulates Gene Expression and Unravels Survival Role of MicroRNA-494 in Jurkat Leukemia.

  2021cites this paper
• Epigenetic abnormalities associated with somatic cell nuclear transfer.

  2021cites this paper
• Loss of heterochromatin and retrotransposon silencing constitute an early phase in oocyte aging

  2020cites this paper
• Occurrence of the d-Proline Chemotype in Enzyme Inhibitors

  2019cites this paper
• Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.

  2019cites this paper
• Histone Deacetylase Inhibitors in Cancer Therapy.

  2019cites this paper
• N-(2′-Hydroxyphenyl)-2-propylpentanamide (OH-VPA), a histone deacetylase inhibitor, induces the release of nuclear HMGB1 and modifies ROS levels in HeLa cells

  2018cites this paper
• CHM-1, a novel microtubule-destabilizing agent exhibits antitumor activity via inducing the expression of SIRT2 in human breast cancer cells.

  2018cites this paper
• Medicinal Chemistry Insights into Novel HDAC Inhibitors: An Updated Patent Review (2012-2016).

  2017cites this paper
• Chemical and structural biology of protein lysine deacetylases

  2017cites this paper
• Living long and ageing well: is epigenomics the missing link between nature and nurture?

  2016cites this paper
• Histone deacetylase 3 indirectly modulates tubulin acetylation

  2015cites this paper
• Neuroprotective capabilities of TSA against cerebral ischemia/reperfusion injury via PI3K/Akt signaling pathway in rats

  2015influential citation
• Effect of histone deacetylase on prostate carcinoma.

  2015cites this paper
• The Histone Deacetylase Inhibitor Trichostatin A Sensitizes Human Renal Carcinoma Cells to TRAIL-Induced Apoptosis through Down-Regulation of c-FLIPL

  2015cites this paper
• Attenuated Airway Epithelial Cell Interleukin-22R1 Expression in the Infant Nonhuman Primate Lung.

  2015cites this paper
• Design, synthesis and evaluation of antiestrogen and histone deacetylase inhibitor molecular hybrids.

  2015cites this paper
• Bicyclic tetrapeptides as potent HDAC inhibitors: effect of aliphatic loop position and hydrophobicity on inhibitory activity.

  2014cites this paper
• Design and synthesis of mono and bicyclic tetrapeptides thioester as potent inhibitor of histone deacetylases

  2014cites this paper
• Prostaglandins, Leukotrienes and Essential Fatty Acids

  2013cites this paper
• The development and potential clinical utility of biomarkers for HDAC inhibitors.

  2013cites this paper
• Acetylation and deacetylation--novel factors in muscle wasting.

  2013cites this paper
• Microbial natural products: molecular blueprints for antitumor drugs

  2013cites this paper
• Induction of differentiation and apoptosis in leukaemic cell lines by the novel benzamide family histone deacetylase 2 and 3 inhibitor MI-192.

  2012cites this paper
• Cyclic tetrapeptides with thioacetate tails or intramolecular disulfide bridge as potent inhibitors of histone deacetylases.

  2012cites this paper
• Histone deacetylases activate hepatocyte growth factor signaling by repressing microRNA-449 in hepatocellular carcinoma cells.

  2012cites this paper
• Prostaglandin E2 induces growth inhibition, apoptosis and differentiation in T and B cell-derived acute lymphoblastic leukemia cell lines (CCRF-CEM and Nalm-6).

  2012cites this paper
• HDAC inhibitors in kidney development and disease

  2012cites this paper
• Modulation of apoptosis and signalling in cancer cells after treatment with epigenetic modulators

  2012cites this paper
• Histone deacetylase inhibitors (HDACIs). Structure—activity relationships: history and new QSAR perspectives

  2012cites this paper
• Histone Deacetylase Inhibitors in Cell Pluripotency, Differentiation, and Reprogramming

  2012cites this paper
• Evaluation of functional groups on amino acids in cyclic tetrapeptides in histone deacetylase inhibition

  2012cites this paper
• Influence of Natural and Synthetic Histone Deacetylase Inhibitors on Chromatin

  2012cites this paper
• Cutting-Edge Issues in Primary Biliary Cirrhosis

  2012cites this paper
• Discovery of histone deacetylase 8 selective inhibitors.

  2011cites this paper
• Probing the role of HDACs and mechanisms of chromatin-mediated neuroplasticity.

  2011cites this paper
• Metabolism as a key to histone deacetylase inhibition

  2011cites this paper
• The epigenetics of autoimmunity

  2011cites this paper
• Histone deacetylase inhibitors.

  2011cites this paper
• Novel histone deacetylase inhibitors in clinical trials as anti-cancer agents

  2010cites this paper
• Bicyclic peptides as potent inhibitors of histone deacetylases: optimization of alkyl loop length.

  2010cites this paper
• Sepsis and glucocorticoids upregulate p300 and downregulate HDAC6 expression and activity in skeletal muscle.

  2010cites this paper
• Histone H1 subtype preferences of DFF40 and possible nuclear localization of DFF40/45 in normal and trichostatin A-treated NB4 leukemic cells

  2010cites this paper
• Macrocyclic histone deacetylase inhibitors.

  2010cites this paper
• Nature as Source of Medicines; Novel Drugs from Nature; Screening for Antitumor Activity

  2010cites this paper
• Differential sensitivity of human leukemic cell lines to the histone deacetylase inhibitor, trichostatin A.

  2010cites this paper
• An aldol-based build/couple/pair strategy for the synthesis of medium- and large-sized rings: discovery of macrocyclic histone deacetylase inhibitors.

  2010cites this paper
• Impact of natural products on developing new anti-cancer agents.

  2009cites this paper
• Cell‐surface expression of Hsp70 on hematopoietic cancer cells after inhibition of HDAC activity

  2009cites this paper
• Acetylation of FoxO1 activates Bim expression to induce apoptosis in response to histone deacetylase inhibitor depsipeptide treatment.

  2009cites this paper
• High class I HDAC activity and expression are associated with RelA/p65 activation in pancreatic cancer in vitro and in vivo

  2009cites this paper
• Untersuchungen zur Lokalisation und Funktion der cAMP-induzierten Proteine IFR1 und TOB bei der terminalen Erythrozytendifferenzierung

  2009cites this paper
• Microbial antitumor drugs: natural products of microbial origin as anticancer agents.

  2009cites this paper
• Histone deacetylase inhibitors: apoptotic effects and clinical implications (Review).

  2008cites this paper
• Evaluating epigenetic landmarks in the brain of multiple sclerosis patients: a contribution to the current debate on disease pathogenesis.

  2008cites this paper
• Interaction of aliphatic cap group in inhibition of histone deacetylases by cyclic tetrapeptides.

  2008cites this paper
• Comparative molecular dynamics simulations of histone deacetylase‐like protein: Binding modes and free energy analysis to hydroxamic acid inhibitors

  2008cites this paper
• Anticancer drug discovery targeting DNA hypermethylation.

  2008cites this paper
• Diminishing HDACs by drugs or mutations promotes normal or abnormal sister chromatid separation by affecting APC/C and adherin

  2008cites this paper
• Targeted therapies in T-cell malignancies

  2007cites this paper
• Histone deacetylase inhibitors for epigenetic therapy of cancer

  2007cites this paper
• High-Frequency Epigenetic Repression and Silencing of Retroviruses Can Be Antagonized by Histone Deacetylase Inhibitors and Transcriptional Activators, but Uniform Reactivation in Cell Clones Is Restricted by Additional Mechanisms

  2007cites this paper
• Gene profile analysis of osteoblast genes differentially regulated by histone deacetylase inhibitors

  2007influential citation
• Design, synthesis, structure--selectivity relationship, and effect on human cancer cells of a novel series of histone deacetylase 6-selective inhibitors.

  2007cites this paper
• 1.08 – Natural Product Sources of Drugs: Plants, Microbes, Marine Organisms, and Animals

  2007cites this paper
• Drug evaluation: MGCD-0103, a histone deacetylase inhibitor for the treatment of cancer.

  2007cites this paper
• Molecular design of histone deacetylase inhibitors by aromatic ring shifting in chlamydocin framework.

  2007cites this paper
• Inhibition of histone deacetylation promotes abnormal epidermal differentiation and specifically suppresses the expression of the late differentiation marker profilaggrin.

  2007cites this paper
• Pharmacological modulation of stem cell function.

  2007cites this paper
• An SMA Project Report: Neural Cell-Based Assays Derived from Human Embryonic Stem Cells

  2007cites this paper
• Zinc binding in HDAC inhibitors: a DFT study.

  2007cites this paper
• Microsporins A and B: new histone deacetylase inhibitors from the marine-derived fungus Microsporum cf. gypseum and the solid-phase synthesis of microsporin A

  2007cites this paper
• Recent Development in Novel Anticancer Therapies

  2007cites this paper
• Dexamethasone-induced protein degradation in cultured myotubes is p300/HAT dependent.

  2007influential citation
• Impact of protein acetylation in inflammatory lung diseases.

  2007cites this paper
• Silencer Runx-Mediated Activation of the CD 4 CD 4 Expression by Antagonizing The Transcription Factor Zbtb 7 b Promotes

  2007cites this paper
• Histone deacetylase inhibitors: molecular mechanisms of action

  2007cites this paper
• The Transcription Factor Zbtb7b Promotes CD4 Expression by Antagonizing Runx-Mediated Activation of the CD4 Silencer1

  2007cites this paper
• The pharmaceutical potential of histone deacetylase inhibitors.

  2007cites this paper
• A proteomic analysis of protein variations during differentiation of v-myb-transformed monoblasts.

  2007cites this paper
• Histone deacetylases in control of skeletogenesis

  2007cites this paper
• Natural products from marine invertebrates and microbes as modulators of antitumor targets.

  2006cites this paper
• The Paradox of Histone Deacetylase Inhibitor-Mediated Modulation of Cellular Responses to Radiation

  2006cites this paper
• Neuron Restrictive Silencer Factor NRSF/REST Is a Transcriptional Repressor of Neuropilin-1 and Diminishes the Ability of Semaphorin 3A to Inhibit Keratinocyte Migration*

  2006cites this paper
• Rational design of non-hydroxamate histone deacetylase inhibitors.

  2006cites this paper
• Natural product-based inhibitors of hypoxia-inducible factor-1 (HIF-1).

  2006cites this paper
• Highly potent and selective histone deacetylase 6 inhibitors designed based on a small-molecular substrate.

  2006cites this paper
• A phase II study of depsipeptide in refractory metastatic renal cell cancer.

  2006cites this paper
• Thioredoxin in cancer--role of histone deacetylase inhibitors.

  2006cites this paper
• Epigenetic control using natural products and synthetic molecules.

  2006cites this paper