Targeting histone deacetylase 8 as a therapeutic approach to cancer and neurodegenerative diseases

Structure-Based Design and Synthesis of Novel Inhibitors Targeting HDAC8 from Schistosoma mansoni for the Treatment of Schistosomiasis

(2016) Tino Heimburg et al.   JOURNAL OF MEDICINAL CHEMISTRY

Alterations in histone deacetylase 8 lead to cell migration and poor prognosis in breast cancer

(2016) Chang-Lin Hsieh et al.   LIFE SCIENCES

Structure-Based Identification of HDAC8 Non-histone Substrates

(2016) Nawsad Alam et al.   STRUCTURE

Isotype-Specific Inhibition of Histone Deacetylases: Identification of Optimal Targets for Radiosensitization

(2016) Jin Ho Kim et al.   Cancer Research and Treatment

Results from a multicenter, open-label, pivotal phase II study of chidamide in relapsed or refractory peripheral T-cell lymphoma

(2015) Y. Shi et al.   ANNALS OF ONCOLOGY

Biochemical and Structural Characterization of HDAC8 Mutants Associated with Cornelia de Lange Syndrome Spectrum Disorders

(2015) Christophe Decroos et al.   BIOCHEMISTRY

Histone Deacetylase HDAC8 Promotes Insulin Resistance and  -Catenin Activation in NAFLD-Associated Hepatocellular Carcinoma

(2015) Y. Tian et al.   CANCER RESEARCH

HDAC8 Inhibition Specifically Targets Inv(16) Acute Myeloid Leukemic Stem Cells by Restoring p53 Acetylation

(2015) Jing Qi et al.   Cell Stem Cell

Synthesis of benzothiophene-based hydroxamic acids as potent and selective HDAC6 inhibitors

(2015) Rob De Vreese et al.   CHEMICAL COMMUNICATIONS

QSAR Studies on Hydroxamic Acids: A Fascinating Family of Chemicals with a Wide Spectrum of Activities

(2015) Satya P. Gupta   CHEMICAL REVIEWS

Histone deacetylases: structural determinants of inhibitor selectivity

(2015) Carmina Micelli et al.   DRUG DISCOVERY TODAY

Mechanism ofN-Acylthiourea-mediated Activation of Human Histone Deacetylase 8 (HDAC8) at Molecular and Cellular Levels

(2015) Raushan K. Singh et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Homology modeling of parasite histone deacetylases to guide the structure-based design of selective inhibitors

(2015) Jelena Melesina et al.   JOURNAL OF MOLECULAR GRAPHICS & MODELLING

Expression of the class 1 histone deacetylases HDAC8 and 3 are associated with improved survival of patients with metastatic melanoma

(2015) James S Wilmott et al.   MODERN PATHOLOGY

Acetylation site specificities of lysine deacetylase inhibitors in human cells

(2015) Christian Schölz et al.   NATURE BIOTECHNOLOGY

A lazy learning-based QSAR classification study for screening potential histone deacetylase 8 (HDAC8) inhibitors

(2015) G.P. Cao et al.   SAR AND QSAR IN ENVIRONMENTAL RESEARCH

RETRACTED ARTICLE: MicroRNA-216b is Down-Regulated in Human Gastric Adenocarcinoma and Inhibits Proliferation and Cell Cycle Progression by Targeting Oncogene HDAC8

(2015) Ying Wang et al.   Targeted Oncology

HDAC8: a multifaceted target for therapeutic interventions

(2015) Alokta Chakrabarti et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Selective inhibition of HDAC8 decreases neuroblastoma growth in vitro and in vivo and enhances retinoic acid-mediated differentiation

(2015) I Rettig et al.   Cell Death & Disease

Mutant cohesin affects RNA polymerase II regulation in Cornelia de Lange syndrome

(2015) Linda Mannini et al.   Scientific Reports

HDAC Family Members Intertwined in the Regulation of Autophagy: A Druggable Vulnerability in Aggressive Tumor Entities

(2015) Emily Koeneke et al.   Cells

HDAC8, A Potential Therapeutic Target for the Treatment of Malignant Peripheral Nerve Sheath Tumors (MPNST)

(2015) Gonzalo Lopez et al.   PLoS One

An Unbiased Approach To Identify Endogenous Substrates of “Histone” Deacetylase 8

(2014) David E. Olson et al.   ACS Chemical Biology

Compromised Structure and Function of HDAC8 Mutants Identified in Cornelia de Lange Syndrome Spectrum Disorders

(2014) Christophe Decroos et al.   ACS Chemical Biology

Histone deacetylase 8 regulates cortactin deacetylation and contraction in smooth muscle tissues

(2014) Jia Li et al.   AMERICAN JOURNAL OF PHYSIOLOGY-CELL PHYSIOLOGY

Design, Synthesis, and Biological Activity of NCC149 Derivatives as Histone Deacetylase 8-Selective Inhibitors

(2014) Takayoshi Suzuki et al.   ChemMedChem

Cornelia de Lange syndrome

(2014) M.I. Boyle et al.   CLINICAL GENETICS

Loss-of-function HDAC8 mutations cause a phenotypic spectrum of Cornelia de Lange syndrome-like features, ocular hypertelorism, large fontanelle and X-linked inheritance

(2014) Frank J. Kaiser et al.   HUMAN MOLECULAR GENETICS

Histone deacetylase 8 suppresses osteogenic differentiation of bone marrow stromal cells by inhibiting histone H3K9 acetylation and RUNX2 activity

(2014) Yu Fu et al.   INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY

Discovery of Inhibitors of Schistosoma mansoni HDAC8 by Combining Homology Modeling, Virtual Screening, and in Vitro Validation

(2014) Srinivasaraghavan Kannan et al.   Journal of Chemical Information and Modeling

Histone deacetylase 8 is deregulated in urothelial cancer but not a target for efficient treatment

(2014) Maria Lehmann et al.   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

HDAC8-Mediated Epigenetic Reprogramming Plays a Key Role in Resistance to Anthrax Lethal Toxin-Induced Pyroptosis in Macrophages

(2014) S.-D. Ha et al.   JOURNAL OF IMMUNOLOGY

Identification of a Novel Aminotetralin Class of HDAC6 and HDAC8 Selective Inhibitors

(2014) Guozhi Tang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Molecular Basis for the Antiparasitic Activity of a Mercaptoacetamide Derivative That Inhibits Histone Deacetylase 8 (HDAC8) from the Human Pathogen Schistosoma mansoni

(2014) Diana A. Stolfa et al.   JOURNAL OF MOLECULAR BIOLOGY

DEC1 Coordinates with HDAC8 to Differentially Regulate TAp73 and ΔNp73 Expression

(2014) Yingjuan Qian et al.   PLoS One

Closing the cohesin ring: Structure and function of its Smc3-kleisin interface

(2014) T. G. Gligoris et al.   SCIENCE

Histone deacetylase 4 promotes ubiquitin-dependent proteasomal degradation of Sp3 in SH-SY5Y cells treated with di(2-ethylhexyl)phthalate (DEHP), determining neuronal death

(2014) Natascia Guida et al.   TOXICOLOGY AND APPLIED PHARMACOLOGY

Erasers of Histone Acetylation: The Histone Deacetylase Enzymes

(2014) E. Seto et al.   Cold Spring Harbor Perspectives in Biology

HDAC8 and STAT3 repress BMF gene activity in colon cancer cells

(2014) Y Kang et al.   Cell Death & Disease

Synthesis and biological evaluation of a targeted DNA-binding transcriptional activator with HDAC8 inhibitory activity

(2013) Abhijit Saha et al.   BIOORGANIC & MEDICINAL CHEMISTRY

SOX4 is a direct target gene of FRA-2 and induces expression of HDAC8 in adult T-cell leukemia/lymphoma

(2013) T. Higuchi et al.   BLOOD

The Up-Regulation of Histone Deacetylase 8 Promotes Proliferation and Inhibits Apoptosis in Hepatocellular Carcinoma

(2013) Jian Wu et al.   DIGESTIVE DISEASES AND SCIENCES

Azetidinone–retinoid hybrids: Synthesis and differentiative effects

(2013) Matteo Pori et al.   EUROPEAN 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

Discovery of the First Histone Deacetylase 6/8 Dual Inhibitors

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

Investigating the Selectivity of Metalloenzyme Inhibitors

(2013) Joshua A. Day et al.   JOURNAL OF MEDICINAL CHEMISTRY

Loop Interactions and Dynamics Tune the Enzymatic Activity of the Human Histone Deacetylase 8

(2013) Micha B. A. Kunze et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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

(2013) Mercedes Lobera et al.   Nature Chemical Biology

MYCN and HDAC2 cooperate to repress miR-183 signaling in neuroblastoma

(2013) Marco Lodrini et al.   NUCLEIC ACIDS RESEARCH

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

Structural Basis for the Inhibition of Histone Deacetylase 8 (HDAC8), a Key Epigenetic Player in the Blood Fluke Schistosoma mansoni

(2013) Martin Marek et al.   PLoS Pathogens

HDAC8 substrates: Histones and beyond

(2012) Noah A. Wolfson et al.   BIOPOLYMERS

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

(2012) Wei-Jan Huang et al.   ChemMedChem

Histone deacetylases inhibitor sodium butyrate inhibits JAK2/STAT signaling through upregulation of SOCS1 and SOCS3 mediated by HDAC8 inhibition in myeloproliferative neoplasms

(2012) Shen-meng Gao et al.   EXPERIMENTAL HEMATOLOGY

X-exome sequencing identifies aHDAC8variant in a large pedigree with X-linked intellectual disability, truncal obesity, gynaecomastia, hypogonadism and unusual face

(2012) Magdalena Harakalova et al.   JOURNAL OF MEDICAL GENETICS

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

MOLECULAR MODELING OF THE INTERACTIONS BETWEEN HISTONE DEACETYLASE 8 AND INHIBITORS

(2012) DAWEI HUANG et al.   JOURNAL OF THEORETICAL & COMPUTATIONAL CHEMISTRY

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

(2012) Matthew A. Deardorff et al.   NATURE

Histone deacetylase inhibitors suppress mutant p53 transcription via histone deacetylase 8

(2012) W Yan et al.   ONCOGENE

NMR Profiling of Histone Deacetylase and Acetyl-transferase Activities in Real Time

(2011) Alexander Dose et al.   ACS Chemical Biology

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

Corrigendum to “Synthesis and evaluation of indole-based new scaffolds for antimicrobial activities—Identification of promising candidates” [Bioorg. Med. Chem. Lett. 21 (2011) 3367–3372]

(2011) Palwinder Singh et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of histone deacetylase 8 selective inhibitors

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

Acetylation of Heat Shock Protein 20 (Hsp20) Regulates Human Myometrial Activity

(2011) Magdalena Karolczak-Bayatti et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Zinc Chelation with Hydroxamate in Histone Deacetylases Modulated by Water Access to the Linker Binding Channel

(2011) Ruibo Wu et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

p73: A Multifunctional Protein in Neurobiology

(2011) Richard Killick et al.   MOLECULAR NEUROBIOLOGY

Synthesis and Biological Evaluation of JAHAs: Ferrocene-Based Histone Deacetylase Inhibitors

(2011) John Spencer et al.   ACS Medicinal Chemistry Letters

Histone Deacetylase 8 Is Required for Centrosome Cohesion and Influenza A Virus Entry

(2011) Yohei Yamauchi et al.   PLoS Pathogens

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

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

Sequential requirement of Sox4 and Sox11 during development of the sympathetic nervous system

(2010) M. R. Potzner et al.   DEVELOPMENT

A Proton-Shuttle Reaction Mechanism for Histone Deacetylase 8 and the Catalytic Role of Metal Ions

(2010) Ruibo Wu et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Hos1 Deacetylates Smc3 to Close the Cohesin Acetylation Cycle

(2010) Vanessa Borges et al.   MOLECULAR CELL

An Acetylation Switch Modulates the Transcriptional Activity of Estrogen-Related Receptor α

(2010) Brian J. Wilson et al.   MOLECULAR ENDOCRINOLOGY

N-Hydroxy-(4-oxime)-cinnamide: A versatile scaffold for the synthesis of novel histone deacetilase (HDAC) inhibitors

(2009) Giuseppe Giannini et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Development of the pan-DAC inhibitor panobinostat (LBH589): Successes and challenges

(2009) Peter Atadja   CANCER LETTERS

 -Keto acid metabolites of organoselenium compounds inhibit histone deacetylase activity in human colon cancer cells

(2009) H. Nian et al.   CARCINOGENESIS

Azetidinones as Zinc-Binding Groups to Design Selective HDAC8 Inhibitors

(2009) Paola Galletti et al.   ChemMedChem

Targeting Histone Deacetylases in Neuroblastoma

(2009) O. Witt et al.   CURRENT PHARMACEUTICAL DESIGN

Targeting of HDAC8 and investigational inhibitors in neuroblastoma

(2009) Ina Oehme et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Epigenetic control of skull morphogenesis by histone deacetylase 8

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

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

(2009) C. Choudhary et al.   SCIENCE

Inactivation of CREB mediated gene transcription by HDAC8 bound protein phosphatase

(2008) Jingxia Gao et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

The Activity of HDAC8 Depends on Local and Distal Sequences of Its Peptide Substrates†

(2008) Zachary A. Gurard-Levin et al.   BIOCHEMISTRY

Differential expression of 12 histone deacetylase (HDAC) genes in astrocytomas and normal brain tissue: class II and IV are hypoexpressed in glioblastomas

(2008) Agda KB Lucio-Eterovic et al.   BMC CANCER

HDAC family: What are the cancer relevant targets?

(2008) Olaf Witt et al.   CANCER LETTERS

Histone Deacetylase 8 in Neuroblastoma Tumorigenesis

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

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

(2008) S Balasubramanian et al.   LEUKEMIA

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

(2008) Michael Haberland et al.   NATURE REVIEWS GENETICS