Towards Selective Inhibition of Histone Deacetylase Isoforms: What Has Been Achieved, Where We Are and What Will Be Next

Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2)

(2013) Taotao Feng et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Dosage-dependent tumor suppression by histone deacetylases 1 and 2 through regulation of c-Myc collaborating genes and p53 function

(2013) M. R. Heideman et al.   BLOOD

Histone deacetylase 1 and 2 are essential for normal T-cell development and genomic stability in mice

(2013) O. M. Dovey et al.   BLOOD

A dual role for Hdac1: oncosuppressor in tumorigenesis, oncogene in tumor maintenance

(2013) F. Santoro et al.   BLOOD

Potent and selective HDAC6 inhibitory activity of N-(4-hydroxycarbamoylbenzyl)-1,2,4,9-tetrahydro-3-thia-9-azafluorenes as novel sulfur analogues of Tubastatin A

(2013) Rob De Vreese et al.   CHEMICAL COMMUNICATIONS

Histone Deacetylase (HDAC) 10 Suppresses Cervical Cancer Metastasis through Inhibition of Matrix Metalloproteinase (MMP) 2 and 9 Expression

(2013) Chenlin Song et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Potent Histone Deacetylase Inhibitors Derived from 4-(Aminomethyl)-N-hydroxybenzamide with High Selectivity for the HDAC6 Isoform

(2013) Christopher Blackburn et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Potent, Isoform-Selective Inhibitors of Histone Deacetylase Containing Chiral Heterocyclic Capping Groups and a N-(2-Aminophenyl)benzamide Binding Unit

(2013) Charles M. Marson et al.   JOURNAL OF MEDICINAL CHEMISTRY

3-Hydroxypyridin-2-thione as Novel Zinc Binding Group for Selective Histone Deacetylase Inhibition

(2013) Vishal Patil et al.   JOURNAL OF MEDICINAL CHEMISTRY

Potent and Selective Inhibition of Histone Deacetylase 6 (HDAC6) Does Not Require a Surface-Binding Motif

(2013) Florence F. Wagner et al.   JOURNAL OF MEDICINAL CHEMISTRY

Development and Therapeutic Implications of Selective Histone Deacetylase 6 Inhibitors

(2013) Jay H. Kalin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of the First Histone Deacetylase 6/8 Dual Inhibitors

(2013) David E. Olson et al.   JOURNAL OF MEDICINAL CHEMISTRY

Class I HDACs Share a Common Mechanism of Regulation by Inositol Phosphates

(2013) Christopher J. Millard et al.   MOLECULAR CELL

HDAC6 as a target for neurodegenerative diseases: what makes it different from the other HDACs?

(2013) Claudia Simões-Pires et al.   Molecular Neurodegeneration

Selective class IIa histone deacetylase inhibition via a nonchelating zinc-binding group

(2013) Mercedes Lobera et al.   Nature Chemical Biology

Development of Frataxin Gene Expression Measures for the Evaluation of Experimental Treatments in Friedreich’s Ataxia

(2013) Heather L. Plasterer et al.   PLoS One

Identification of Highly Selective and Potent Histone Deacetylase 3 Inhibitors Using Click Chemistry-Based Combinatorial Fragment Assembly

(2013) Takayoshi Suzuki et al.   PLoS One

HDAC3-selective inhibitor enhances extinction of cocaine-seeking behavior in a persistent manner

(2013) M. Malvaez et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Histone deacetylase 10 promotes autophagy-mediated cell survival

(2013) I. Oehme et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Role of Hydroxamate-Based Histone Deacetylase Inhibitors (Hb-HDACIs) in the Treatment of Solid Malignancies

(2013) Antonino Grassadonia et al.   Cancers

Profiling of Substrates for Zinc-dependent Lysine Deacylase Enzymes: HDAC3 Exhibits Decrotonylase Activity In Vitro

(2012) Andreas S. Madsen et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Novel histone deacetylase 8 ligands without a zinc chelating group: Exploring an ‘upside-down’ binding pose

(2012) Aditya Sudheer Vaidya et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Preclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with bortezomib in multiple myeloma

(2012) L. Santo et al.   BLOOD

Histone deacetylase 3 is required for maintenance of bone mass during aging

(2012) Meghan E. McGee-Lawrence et al.   BONE

QT interval prolongation and torsades de pointes in a patient undergoing treatment with vorinostat: A case report and review of the literature

(2012) Donald R. Lynch Jr et al.   Cardiology Journal

HDAC4 Governs a Transcriptional Program Essential for Synaptic Plasticity and Memory

(2012) Richard Sando et al.   CELL

HDAC5 is required for maintenance of pericentric heterochromatin and controls cell-cycle progression and survival of human cancer cells

(2012) P Peixoto et al.   CELL DEATH AND DIFFERENTIATION

Multiple roles of class I HDACs in proliferation, differentiation, and development

(2012) Nina Reichert et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Synthesis and Biological Evaluation ofortho-ArylN-Hydroxycinnamides as Potent Histone Deacetylase (HDAC) 8 Isoform-Selective Inhibitors

(2012) Wei-Jan Huang et al.   ChemMedChem

Molecular Pathways: Old Drugs Define New Pathways: Non-Histone Acetylation at the Crossroads of the DNA Damage Response and Autophagy

(2012) O. A. Botrugno et al.   CLINICAL CANCER RESEARCH

Targeting class I histone deacetylases in cancer therapy

(2012) Geneviève P Delcuve et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Histone deacetylase inhibitors in the treatment of cancer: overview and perspectives

(2012) Giuseppe Giannini et al.   Future Medicinal Chemistry

Targeted cancer therapy: giving histone deacetylase inhibitors all they need to succeed

(2012) Berkley E Gryder et al.   Future Medicinal Chemistry

HDAC11 is a novel drug target in carcinomas

(2012) Hedwig E. Deubzer et al.   INTERNATIONAL JOURNAL OF CANCER

Rapid Discovery of Highly Potent and Selective Inhibitors of Histone Deacetylase 8 Using Click Chemistry to Generate Candidate Libraries

(2012) Takayoshi Suzuki et al.   JOURNAL OF MEDICINAL CHEMISTRY

Selective Histone Deacetylase 6 Inhibitors Bearing Substituted Urea Linkers Inhibit Melanoma Cell Growth

(2012) Joel A. Bergman et al.   JOURNAL OF MEDICINAL CHEMISTRY

Histone Deacetylase (HDAC) Inhibitors with a Novel Connecting Unit Linker Region Reveal a Selectivity Profile for HDAC4 and HDAC5 with Improved Activity against Chemoresistant Cancer Cells

(2012) Linda Marek et al.   JOURNAL OF MEDICINAL CHEMISTRY

Histone deacetylases and cancer

(2012) Bruna Barneda-Zahonero et al.   Molecular Oncology

HDAC8 mutations in Cornelia de Lange syndrome affect the cohesin acetylation cycle

(2012) Matthew A. Deardorff et al.   NATURE

Histone deacetylase (HDAC) inhibitors targeting HDAC3 and HDAC1 ameliorate polyglutamine-elicited phenotypes in model systems of Huntington's disease

(2012) Haiqun Jia et al.   NEUROBIOLOGY OF DISEASE

Molecular Modeling Study on Tunnel Behavior in Different Histone Deacetylase Isoforms

(2012) Sundarapandian Thangapandian et al.   PLoS One

Roles of histone deacetylases in epigenetic regulation: emerging paradigms from studies with inhibitors

(2012) Geneviève P Delcuve et al.   Clinical Epigenetics

Human HDAC isoform selectivity achieved via exploitation of the acetate release channel with structurally unique small molecule inhibitors

(2011) Lewis Whitehead et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Discovery of histone deacetylase 8 selective inhibitors

(2011) Weiping Tang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Histone Deacetylase 6 (HDAC6) Is an Essential Modifier of Glucocorticoid-Induced Hepatic Gluconeogenesis

(2011) R. Winkler et al.   DIABETES

Class IIb HDAC6 regulates endothelial cell migration and angiogenesis by deacetylation of cortactin

(2011) David Kaluza et al.   EMBO JOURNAL

Next generation histone deacetylase inhibitors: the answer to the search for optimized epigenetic therapies?

(2011) Florian Thaler et al.   Expert Opinion on Drug Discovery

Romidepsin (Istodax, NSC 630176, FR901228, FK228, depsipeptide): a natural product recently approved for cutaneous T-cell lymphoma

(2011) Karen M VanderMolen et al.   JOURNAL OF ANTIBIOTICS

Histone Deacetylases 9 and 10 Are Required for Homologous Recombination

(2011) Shweta Kotian et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Class IIa HDACs: from important roles in differentiation to possible implications in tumourigenesis

(2011) Andrea Clocchiatti et al.   JOURNAL OF CELLULAR AND MOLECULAR MEDICINE

Second-Generation Histone Deacetylase 6 Inhibitors Enhance the Immunosuppressive Effects of Foxp3+ T-Regulatory Cells

(2011) Jay H. Kalin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Suppression of Histone Deacetylase 11 Promotes Expression of IL-10 in Kupffer Cells and Induces Tolerance Following Orthotopic Liver Transplantation in Rats

(2011) Zheng-rong Lian et al.   JOURNAL OF SURGICAL RESEARCH

HDAC6 α-tubulin deacetylase: A potential therapeutic target in neurodegenerative diseases

(2011) Guoyi Li et al.   JOURNAL OF THE NEUROLOGICAL SCIENCES

Mocetinostat for relapsed classical Hodgkin's lymphoma: an open-label, single-arm, phase 2 trial

(2011) Anas Younes et al.   LANCET ONCOLOGY

HDACs link the DNA damage response, processing of double-strand breaks and autophagy

(2011) Thomas Robert et al.   NATURE

Chemoproteomics profiling of HDAC inhibitors reveals selective targeting of HDAC complexes

(2011) Marcus Bantscheff et al.   NATURE BIOTECHNOLOGY

Interplay between oncogene-induced DNA damage response and heterochromatin in senescence and cancer

(2011) Raffaella Di Micco et al.   NATURE CELL BIOLOGY

Advantages of Promoting Interleukin-10 by Silence of Histone Deacetylase 11 in Inducing Tolerance in Orthotopic Liver Transplantation in Rats

(2011) X. Lai et al.   TRANSPLANTATION PROCEEDINGS

On the inhibition of histone deacetylase 8

(2010) Guillermina Estiu et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Exploration of the HDAC2 foot pocket: Synthesis and SAR of substituted N-(2-aminophenyl)benzamides

(2010) Jerome C. Bressi et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Hdac3 Is Essential for the Maintenance of Chromatin Structure and Genome Stability

(2010) Srividya Bhaskara et al.   CANCER CELL

HDAC5 and HDAC9 in Medulloblastoma: Novel Markers for Risk Stratification and Role in Tumor Cell Growth

(2010) T. Milde et al.   CLINICAL CANCER RESEARCH

The Role of Histone Deacetylase Inhibitors in the Treatment of Patients With Cutaneous T-Cell Lymphoma

(2010) Kenneth B. Hymes   Clinical Lymphoma Myeloma & Leukemia

Hdac1 and Hdac2 Act Redundantly to Control p63 and p53 Functions in Epidermal Progenitor Cells

(2010) Matthew LeBoeuf et al.   DEVELOPMENTAL CELL

Overlapping functions of Hdac1 and Hdac2 in cell cycle regulation and haematopoiesis

(2010) Roel H Wilting et al.   EMBO JOURNAL

A work in progress: The clinical development of histone deacetylase inhibitor

(2010) Silvia Marsoni et al.   Epigenetics

Histone deacetylases in skeletal development and bone mass maintenance

(2010) Meghan E. McGee-Lawrence et al.   GENE

Histone deacetylases 1 and 2 act in concert to promote the G1-to-S progression

(2010) T. Yamaguchi et al.   GENES & DEVELOPMENT

Redundant Control of Adipogenesis by Histone Deacetylases 1 and 2

(2010) Michael Haberland et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The Role of HDAC6 in Cancer

(2010) Grace I. Aldana-Masangkay et al.   JOURNAL OF BIOMEDICINE AND BIOTECHNOLOGY

Regulating the Regulators: The Post-Translational Code of Class I HDAC1 and HDAC2

(2010) Chiara V. Segré et al.   JOURNAL OF BIOMEDICINE AND BIOTECHNOLOGY

Disease-causing mutations in Parkin impair mitochondrial ubiquitination, aggregation, and HDAC6-dependent mitophagy

(2010) Joo-Yong Lee et al.   JOURNAL OF CELL BIOLOGY

Novel histone deacetylase inhibitors in clinical trials as anti-cancer agents

(2010) Jiahuai Tan et al.   Journal of Hematology & Oncology

Non-Natural Macrocyclic Inhibitors of Histone Deacetylases: Design, Synthesis, and Activity

(2010) Luciana Auzzas et al.   JOURNAL OF MEDICINAL CHEMISTRY

The role of histone deacetylase 7 (HDAC7) in cancer cell proliferation: regulation on c-Myc

(2010) Caihua Zhu et al.   JOURNAL OF MOLECULAR MEDICINE-JMM

Rational Design and Simple Chemistry Yield a Superior, Neuroprotective HDAC6 Inhibitor, Tubastatin A

(2010) Kyle V. Butler et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Inhibition of histone deacetylase 10 induces thioredoxin-interacting protein and causes accumulation of reactive oxygen species in SNU-620 human gastric cancer cells

(2010) Ju-Hee Lee et al.   MOLECULES AND CELLS

Chemical phylogenetics of histone deacetylases

(2010) James E Bradner et al.   Nature Chemical Biology

Histone deacetylases and epigenetic therapies of hematological malignancies

(2010) Ciro Mercurio et al.   PHARMACOLOGICAL RESEARCH

Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors

(2009) Pierre Tessier et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Isoform-specific histone deacetylase inhibitors: The next step?

(2009) Sriram Balasubramanian et al.   CANCER LETTERS

Loss of Histone Deacetylase 4 Causes Segregation Defects during Mitosis of p53-Deficient Human Tumor Cells

(2009) B. Cadot et al.   CANCER RESEARCH

Azetidinones as Zinc-Binding Groups to Design Selective HDAC8 Inhibitors

(2009) Paola Galletti et al.   ChemMedChem

JNJ-26481585, a Novel "Second-Generation" Oral Histone Deacetylase Inhibitor, Shows Broad-Spectrum Preclinical Antitumoral Activity

(2009) J. Arts et al.   CLINICAL CANCER RESEARCH

Non-Cancer Uses of Histone Deacetylase Inhibitors: Effects on Infectious Diseases and β-Hemoglobinopathies+

(2009) Dante Rotili et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Assays for Histone Deacetylases

(2009) Alexander-Thomas Hauser et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Epigenetic control of skull morphogenesis by histone deacetylase 8

(2009) M. Haberland et al.   GENES & DEVELOPMENT

Class IIa histone deacetylases: conducting development and differentiation

(2009) Maud Martin et al.   INTERNATIONAL JOURNAL OF DEVELOPMENTAL BIOLOGY

Histone Deacetylase 10 Relieves Repression on the Melanogenic Program by Maintaining the Deacetylation Status of Repressors

(2009) I-Lu Lai et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Trans-regulation of Histone Deacetylase Activities through Acetylation

(2009) Yi Luo et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Histone Deacetylase Inhibitors in Cancer Therapy

(2009) Andrew A. Lane et al.   JOURNAL OF CLINICAL ONCOLOGY

Phase II Multi-Institutional Trial of the Histone Deacetylase Inhibitor Romidepsin As Monotherapy for Patients With Cutaneous T-Cell Lymphoma

(2009) Richard L. Piekarz et al.   JOURNAL OF CLINICAL ONCOLOGY

Synthesis and Biological Evaluation ofN-Hydroxyphenylacrylamides andN-Hydroxypyridin-2-ylacrylamides as Novel Histone Deacetylase Inhibitors

(2009) Florian Thaler et al.   JOURNAL OF MEDICINAL CHEMISTRY

Lysine Acetylation Targets Protein Complexes and Co-Regulates Major Cellular Functions

(2009) C. Choudhary et al.   SCIENCE

Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors

(2008) Nagma Khan et al.   BIOCHEMICAL JOURNAL

Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases

(2008) Philip Jones et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Phase 1 study of the oral isotype specific histone deacetylase inhibitor MGCD0103 in leukemia

(2008) G. Garcia-Manero et al.   BLOOD

Isoform-selective histone deacetylase inhibitors

(2008) Anton V. Bieliauskas et al.   CHEMICAL SOCIETY REVIEWS

Histone Deacetylase 8 in Neuroblastoma Tumorigenesis

(2008) I. Oehme et al.   CLINICAL CANCER RESEARCH

Isoform-Selective Histone Deacetylase Inhibitors

(2008) Takayoshi Suzuki et al.   CURRENT PHARMACEUTICAL DESIGN

Chemical Origins of Isoform Selectivity in Histone Deacetylase Inhibitors

(2008) Alan Kozikowski et al.   CURRENT PHARMACEUTICAL DESIGN

Structural and Functional Analysis of the Human HDAC4 Catalytic Domain Reveals a Regulatory Structural Zinc-binding Domain

(2008) Matthew J. Bottomley et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Human HDAC7 Harbors a Class IIa Histone Deacetylase-specific Zinc Binding Motif and Cryptic Deacetylase Activity

(2008) Anja Schuetz et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Maintenance of cardiac energy metabolism by histone deacetylase 3 in mice

(2008) Rusty L. Montgomery et al.   JOURNAL OF CLINICAL INVESTIGATION

Residues in the 11 Å Channel of Histone Deacetylase 1 Promote Catalytic Activity: Implications for Designing Isoform-Selective Histone Deacetylase Inhibitors†

(2008) Sujith V. W. Weerasinghe et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery ofN-(2-Aminophenyl)-4-[(4-pyridin-3-ylpyrimidin-2-ylamino)methyl]benzamide (MGCD0103), an Orally Active Histone Deacetylase Inhibitor

(2008) Nancy Zhou et al.   JOURNAL OF MEDICINAL CHEMISTRY

A novel histone deacetylase 8 (HDAC8)-specific inhibitor PCI-34051 induces apoptosis in T-cell lymphomas

(2008) S Balasubramanian et al.   LEUKEMIA

HDAC4 Promotes Growth of Colon Cancer Cells via Repression of p21

(2008) Andrew J. Wilson et al.   MOLECULAR BIOLOGY OF THE CELL

MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity in vitro and in vivo

(2008) M. Fournel et al.   MOLECULAR CANCER THERAPEUTICS

Deletion of Histone Deacetylase 3 Reveals Critical Roles in S Phase Progression and DNA Damage Control

(2008) Srividya Bhaskara et al.   MOLECULAR CELL

Nanog and Oct4 associate with unique transcriptional repression complexes in embryonic stem cells

(2008) Jiancong Liang et al.   NATURE CELL BIOLOGY

The histone deacetylase HDAC11 regulates the expression of interleukin 10 and immune tolerance

(2008) Alejandro Villagra et al.   NATURE IMMUNOLOGY

Therapeutic application of histone deacetylase inhibitors for central nervous system disorders

(2008) Aleksey G. Kazantsev et al.   NATURE REVIEWS DRUG DISCOVERY

The many roles of histone deacetylases in development and physiology: implications for disease and therapy

(2008) Michael Haberland et al.   NATURE REVIEWS GENETICS

The Rpd3/Hda1 family of lysine deacetylases: from bacteria and yeast to mice and men

(2008) Xiang-Jiao Yang et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

HDAC4 represses p21WAF1/Cip1 expression in human cancer cells through a Sp1-dependent, p53-independent mechanism

(2008) D Mottet et al.   ONCOGENE

HDAC6: a key regulator of cytoskeleton, cell migration and cell–cell interactions

(2008) Agustín Valenzuela-Fernández et al.   TRENDS IN CELL BIOLOGY