Bifunctional HDAC Therapeutics: One Drug to Rule Them All?

Proteolysis-Targeting Chimeras as Therapeutics and Tools for Biological Discovery

(2020) George M. Burslem et al.   CELL

Discovery of novel cyclin-dependent kinase (CDK) and histone deacetylase (HDAC) dual inhibitors with potent in vitro and in vivo anticancer activity

(2020) Chunhui Cheng et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Mechanism of Crosstalk between the LSD1 Demethylase and HDAC1 Deacetylase in the CoREST Complex

(2020) Yun Song et al.   Cell Reports

Development of Selective Histone Deacetylase 6 (HDAC6) Degraders Recruiting Von Hippel–Lindau (VHL) E3 Ubiquitin Ligase

(2020) Ka Yang et al.   ACS Medicinal Chemistry Letters

Analysis of Dual Class I Histone Deacetylase and Lysine Demethylase Inhibitor Domatinostat (4SC-202) on Growth and Cellular and Genomic Landscape of Atypical Teratoid/Rhabdoid

(2020) Mariah M. Hoffman et al.   Cancers

Epigenetic Chemical Biology: Opportunities Beyond the Advances and Opportunities in Epigenetic Chemical Biology

(2020) Jenna N Beyer et al.   CHEMBIOCHEM

Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight

(2020) Terence C. S. Ho et al.   JOURNAL OF MEDICINAL CHEMISTRY

Developing potent PROTACs tools for selective degradation of HDAC6 protein

(2019) Zixuan An et al.   Protein & Cell

Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies

(2019) Xuewu Liang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of novel phenoxybenzamide analogues as Raf/HDAC dual inhibitors

(2019) Aixin Geng et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Development of Multifunctional Histone Deacetylase 6 Degraders with Potent Antimyeloma Activity

(2019) Hao Wu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structural Basis of Catalysis and Inhibition of HDAC6 CD1, the Enigmatic Catalytic Domain of Histone Deacetylase 6

(2019) Jeremy D. Osko et al.   BIOCHEMISTRY

Evodiamine-inspired dual inhibitors of histone deacetylase 1 (HDAC1) and topoisomerase 2 (TOP2) with potent antitumor activity

(2019) Yahui Huang et al.   Acta Pharmaceutica Sinica B

Design, synthesis and anticancer evaluation of acridine hydroxamic acid derivatives as dual Topo and HDAC inhibitors

(2018) Jiwei Chen et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Development of the first small molecule histone deacetylase 6 (HDAC6) degraders

(2018) Ka Yang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Small molecules as tools to study the chemical epigenetics of lysine acetylation

(2018) Matthias Schiedel et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

1-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC

(2018) Ritu Ojha et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease

(2018) Obdulia Rabal et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections

(2018) Yahui Huang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously

(2018) Jie Zang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on isocombretastatin A-4

(2018) Diana Lamaa et al.   JOURNAL OF MEDICINAL CHEMISTRY

Chimeric HDAC inhibitors: Comprehensive review on the HDAC-based strategies developed to combat cancer

(2018) Heba M. Hesham et al.   MEDICINAL RESEARCH REVIEWS

Targeting the CoREST complex with dual histone deacetylase and demethylase inhibitors

(2018) Jay H. Kalin et al.   Nature Communications

Combination Therapy With Histone Deacetylase Inhibitors (HDACi) for the Treatment of Cancer: Achieving the Full Therapeutic Potential of HDACi

(2018) Amila Suraweera et al.   Frontiers in Oncology

HDAC3 is a potential validated target for cancer: An overview on the benzamide-based selective HDAC3 inhibitors through comparative SAR/QSAR/QAAR approaches

(2018) Nilanjan Adhikari et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design and synthesis of potent dual inhibitors of JAK2 and HDAC based on fusing the pharmacophores of XL019 and vorinostat

(2018) Yu-yi Chu-Farseeva et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents

(2018) Shipeng He et al.   JOURNAL OF MEDICINAL CHEMISTRY

Histone Deacetylase 6-Selective Inhibitors and the Influence of Capping Groups on Hydroxamate-Zinc Denticity

(2018) Nicholas J. Porter et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of in Vivo Chemical Probes for Treating Alzheimer’s Disease: Dual Phosphodiesterase 5 (PDE5) and Class I Histone Deacetylase Selective Inhibitors

(2018) Obdulia Rabal et al.   ACS Chemical Neuroscience

CoREST Complex-Selective Histone Deacetylase Inhibitors Show Prosynaptic Effects and an Improved Safety Profile To Enable Treatment of Synaptopathies

(2018) Nathan O. Fuller et al.   ACS Chemical Neuroscience

Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy

(2018) Yepeng Luan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design and synthesis of tranylcypromine derivatives as novel LSD1/HDACs dual inhibitors for cancer treatment

(2017) Ying-Chao Duan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Designing multi-targeted agents: An emerging anticancer drug discovery paradigm

(2017) Rong-geng Fu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

CUDC-907 in relapsed/refractory diffuse large B-cell lymphoma, including patients with MYC-alterations: results from an expanded phase I trial

(2017) Yasuhiro Oki et al.   HAEMATOLOGICA

Small Molecule Inhibitors Simultaneously Targeting Cancer Metabolism and Epigenetics: Discovery of Novel Nicotinamide Phosphoribosyltransferase (NAMPT) and Histone Deacetylase (HDAC) Dual Inhibitors

(2017) Guoqiang Dong et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat

(2017) Lianbin Yao et al.   JOURNAL OF MEDICINAL CHEMISTRY

Chemically Induced Degradation of Sirtuin 2 (Sirt2) by a Proteolysis Targeting Chimera (PROTAC) Based on Sirtuin Rearranging Ligands (SirReals)

(2017) Matthias Schiedel et al.   JOURNAL OF MEDICINAL CHEMISTRY

Is dual inhibition of metalloenzymes HDAC-8 and MMP-2 a potential pharmacological target to combat hematological malignancies?

(2017) Sk. Abdul Amin et al.   PHARMACOLOGICAL RESEARCH

Stepwise assembly of functional C-terminal REST/NRSF transcriptional repressor complexes as a drug target

(2017) Ken Inui et al.   PROTEIN SCIENCE

Targeting Class I Histone Deacetylases in a “Complex” Environment

(2017) Christopher J. Millard et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Design, Synthesis, and Biological Evaluation of the First c-Met/HDAC Inhibitors Based on Pyridazinone Derivatives

(2017) Dong Lu et al.   ACS Medicinal Chemistry Letters

The HDAC inhibitor AR42 interacts with pazopanib to kill trametinib/dabrafenib-resistant melanoma cells in vitro and in vivo

(2017) Laurence Booth et al.   Oncotarget

CUDC-907 in relapsed/refractory diffuse large B-cell lymphoma, including patients with MYC-alterations: results from an expanded phase I trial

(2017) Yasuhiro Oki et al.   HAEMATOLOGICA

Differential HDAC1 and 2 Recruitment by Members of the MIER Family

(2017) Roya Derwish et al.   PLoS One

Structure-Based Development of an Affinity Probe for Sirtuin 2

(2016) Matthias Schiedel et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

General Base–General Acid Catalysis in Human Histone Deacetylase 8

(2016) Sister M. Lucy Gantt et al.   BIOCHEMISTRY

Epigenetic Treatment of Neurodegenerative Disorders: Alzheimer and Parkinson Diseases

(2016) Michael H. Irwin et al.   DRUG DEVELOPMENT RESEARCH

Inside HDACs with more selective HDAC inhibitors

(2016) Joëlle Roche et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines

(2016) Eugene Guorong Yang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Histone deacetylase 6 structure and molecular basis of catalysis and inhibition

(2016) Yang Hai et al.   Nature Chemical Biology

Structural insights into HDAC6 tubulin deacetylation and its selective inhibition

(2016) Yasuyuki Miyake et al.   Nature Chemical Biology

Pre-clinical characterization of 4SC-202, a novel class I HDAC inhibitor, against colorectal cancer cells

(2016) Huang Zhijun et al.   TUMOR BIOLOGY

Epigenetic polypharmacology: from combination therapy to multitargeted drugs

(2016) Angel R. de Lera et al.   Clinical Epigenetics

Identification of Histone Deacetylase Inhibitors with Benzoylhydrazide Scaffold that Selectively Inhibit Class I Histone Deacetylases

(2015) Yunfei Wang et al.   CHEMISTRY & BIOLOGY

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

(2015) Jing Lu et al.   CHEMISTRY & BIOLOGY

A Phase I Study of CUDC-101, a Multitarget Inhibitor of HDACs, EGFR, and HER2, in Combination with Chemoradiation in Patients with Head and Neck Squamous Cell Carcinoma

(2015) T. J. Galloway et al.   CLINICAL CANCER RESEARCH

Panobinostat for the Treatment of Multiple Myeloma

(2015) J. P. Laubach et al.   CLINICAL CANCER RESEARCH

Enhancing the cellular anti-proliferation activity of pyridazinones as c-met inhibitors using docking analysis

(2015) Weiqiang Xing et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis and biological evaluation of colchicine derivatives as novel tubulin and histone deacetylase dual inhibitors

(2015) Xuan Zhang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Catalytic in vivo protein knockdown by small-molecule PROTACs

(2015) Daniel P Bondeson et al.   Nature Chemical Biology

Structural and functional characterization of a cell cycle associated HDAC1/2 complex reveals the structural basis for complex assembly and nucleosome targeting

(2015) Toshimasa Itoh et al.   NUCLEIC ACIDS RESEARCH

Inhibition of nicotinamide phosphoribosyltransferase (NAMPT) as a therapeutic strategy in cancer

(2015) Deepak Sampath et al.   PHARMACOLOGY & THERAPEUTICS

Phthalimide conjugation as a strategy for in vivo target protein degradation

(2015) G. E. Winter et al.   SCIENCE

A Selective Phenelzine Analogue Inhibitor of Histone Demethylase LSD1

(2014) Polina Prusevich et al.   ACS Chemical Biology

Pazopanib and HDAC inhibitors interact to kill sarcoma cells

(2014) Seyedmehrad Tavallai et al.   CANCER BIOLOGY & THERAPY

Phase I First-in-Human Study of CUDC-101, a Multitargeted Inhibitor of HDACs, EGFR, and HER2 in Patients with Advanced Solid Tumors

(2014) T. Shimizu et al.   CLINICAL CANCER RESEARCH

Belinostat: First Global Approval

(2014) Raewyn M. Poole   DRUGS

Rational approaches, design strategies, structure activity relationship and mechanistic insights for anticancer hybrids

(2014) Kunal Nepali et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

New and emerging HDAC inhibitors for cancer treatment

(2014) Alison C. West et al.   JOURNAL OF CLINICAL INVESTIGATION

Structure-Guided Design and Optimization of Small Molecules Targeting the Protein–Protein Interaction between the von Hippel–Lindau (VHL) E3 Ubiquitin Ligase and the Hypoxia Inducible Factor (HIF) Alpha Subunit with in Vitro Nanomolar Affinities

(2014) Carles Galdeano et al.   JOURNAL OF MEDICINAL CHEMISTRY

Polypharmacology: Challenges and Opportunities in Drug Discovery

(2014) Andrew Anighoro et al.   JOURNAL OF MEDICINAL CHEMISTRY

Inhibition and Mechanism of HDAC8 Revisited

(2014) Kai Chen et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Highly effective combination of LSD1 (KDM1A) antagonist and pan-histone deacetylase inhibitor against human AML cells

(2014) W Fiskus et al.   LEUKEMIA

Targeting Microtubules by Natural Agents for Cancer Therapy

(2014) E. Mukhtar et al.   MOLECULAR CANCER THERAPEUTICS

Histone deacetylases and their inhibitors in cancer, neurological diseases and immune disorders

(2014) Katrina J. Falkenberg et al.   NATURE REVIEWS DRUG DISCOVERY

Histone Deacetylase Inhibitor Trichostatin A Enhances Antitumor Effects of Docetaxel or Erlotinib in A549 Cell Line

(2013) Qun-Cheng Zhang et al.   Asian Pacific Journal of Cancer Prevention

The physiological roles of histone deacetylase (HDAC) 1 and 2: complex co-stars with multiple leading parts

(2013) Richard D.W. Kelly et al.   BIOCHEMICAL SOCIETY TRANSACTIONS

The discovery of colchicine-SAHA hybrids as a new class of antitumor agents

(2013) Xuan Zhang et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Dual-acting histone deacetylase-topoisomerase I inhibitors

(2013) William Guerrant et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Phase II trial of panobinostat, an oral pan-deacetylase inhibitor in patients with primary myelofibrosis, post-essential thrombocythaemia, and post-polycythaemia vera myelofibrosis

(2013) Daniel J. DeAngelo et al.   BRITISH JOURNAL OF HAEMATOLOGY

JAK1/2 and Pan-Deacetylase Inhibitor Combination Therapy Yields Improved Efficacy in Preclinical Mouse Models of JAK2V617F-Driven Disease

(2013) E. Evrot et al.   CLINICAL CANCER RESEARCH

Histone Deacetylase (HDAC) Inhibitor Kinetic Rate Constants Correlate with Cellular Histone Acetylation but Not Transcription and Cell Viability

(2013) Benjamin E. L. Lauffer et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Development and Therapeutic Implications of Selective Histone Deacetylase 6 Inhibitors

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

Structure-Based Identification of Ureas as Novel Nicotinamide Phosphoribosyltransferase (Nampt) Inhibitors

(2013) Xiaozhang Zheng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Polypharmacology – Foe or Friend?

(2013) Jens-Uwe Peters   JOURNAL OF MEDICINAL CHEMISTRY

Exploring QSAR and pharmacophore mapping of structurally diverse selective matrix metalloproteinase-2 inhibitors

(2013) Amit Kumar Halder et al.   JOURNAL OF PHARMACY AND PHARMACOLOGY

Targeted treatment for advanced soft tissue sarcoma: profile of pazopanib

(2013) Seth Pollack et al.   OncoTargets and Therapy

Phosphodiesterases as Therapeutic Targets for Alzheimer's Disease

(2012) Ana García-Osta et al.   ACS Chemical Neuroscience

Ruxolitinib: The First FDA Approved Therapy for the Treatment of Myelofibrosis

(2012) J. Mascarenhas et al.   CLINICAL CANCER RESEARCH

Phase I Trial of Combretastatin A4 Phosphate (CA4P) in Combination with Bevacizumab in Patients with Advanced Cancer

(2012) P. Nathan et al.   CLINICAL CANCER RESEARCH

Cancer Network Disruption by a Single Molecule Inhibitor Targeting Both Histone Deacetylase Activity and Phosphatidylinositol 3-Kinase Signaling

(2012) C. Qian et al.   CLINICAL CANCER RESEARCH

Jakinibs: a new class of kinase inhibitors in cancer and autoimmune disease

(2012) Apostolos Kontzias et al.   CURRENT OPINION IN PHARMACOLOGY

The HDAC inhibitor Givinostat modulates the hematopoietic transcription factors NFE2 and C-MYB in JAK2V617F myeloproliferative neoplasm cells

(2012) Ariel Amaru Calzada et al.   EXPERIMENTAL HEMATOLOGY

Biology and significance of the JAK/STAT signalling pathways

(2012) Hiu Kiu et al.   GROWTH FACTORS

JAK and STAT Signaling Molecules in Immunoregulation and Immune-Mediated Disease

(2012) John J. O'Shea et al.   IMMUNITY

Combination therapy for hepatocellular carcinoma: Additive preclinical efficacy of the HDAC inhibitor panobinostat with sorafenib

(2012) Anja Lachenmayer et al.   JOURNAL OF HEPATOLOGY

Dual Targeting of Histone Deacetylase and Topoisomerase II with Novel Bifunctional Inhibitors

(2012) William Guerrant et al.   JOURNAL OF MEDICINAL CHEMISTRY

Pazopanib for metastatic soft-tissue sarcoma (PALETTE): a randomised, double-blind, placebo-controlled phase 3 trial

(2012) Winette TA van der Graaf et al.   LANCET

Chimerically designed HDAC- and tyrosine kinase inhibitors. A series of erlotinib hybrids as dual-selective inhibitors of EGFR, HER2 and histone deacetylases

(2012) Thomas Beckers et al.   MedChemComm

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

Inhibitors of histone demethylation and histone deacetylation cooperate in regulating gene expression and inhibiting growth in human breast cancer cells

(2011) Yi Huang et al.   BREAST CANCER RESEARCH AND TREATMENT

A phase II study of the histone deacetylase inhibitor vorinostat combined with tamoxifen for the treatment of patients with hormone therapy-resistant breast cancer

(2011) P N Munster et al.   BRITISH JOURNAL OF CANCER

A Phase II Trial of Panobinostat, a Histone Deacetylase Inhibitor, in the Treatment of Patients with Refractory Metastatic Renal Cell Carcinoma

(2011) John D. Hainsworth et al.   CANCER INVESTIGATION

Hallmarks of Cancer: The Next Generation

(2011) Douglas Hanahan et al.   CELL

p53 regulation by ubiquitin

(2011) Christopher L. Brooks et al.   FEBS LETTERS

Rational therapeutic combinations with histone deacetylase inhibitors for the treatment of cancer

(2011) K Ted Thurn et al.   Future Oncology

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

The JAK2/STAT3 signaling pathway is required for growth of CD44+CD24– stem cell–like breast cancer cells in human tumors

(2011) Lauren L.C. Marotta et al.   JOURNAL OF CLINICAL INVESTIGATION

Synergistic induction of p53 mediated apoptosis by valproic acid and nutlin-3 in acute myeloid leukemia

(2011) E McCormack et al.   LEUKEMIA

Recent advances in the multitarget-directed ligands approach for the treatment of Alzheimer's disease

(2011) Rafael León et al.   MEDICINAL RESEARCH REVIEWS

Unknown

(2011) Dan Christensen et al.   MOLECULAR MEDICINE

Chemoproteomics profiling of HDAC inhibitors reveals selective targeting of HDAC complexes

(2011) Marcus Bantscheff et al.   NATURE BIOTECHNOLOGY

Inhibition of LSD1 sensitizes glioblastoma cells to histone deacetylase inhibitors

(2011) M. M. Singh et al.   NEURO-ONCOLOGY

Synergistic Antitumor Effects of Novel HDAC Inhibitors and Paclitaxel In Vitro and In Vivo

(2011) Valentina Zuco et al.   PLoS One

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

Cell Signaling by Receptor Tyrosine Kinases

(2010) Mark A. Lemmon et al.   CELL

Combretastatin A4 phosphate: a novel vascular disrupting agent

(2010) Govardhanan Nagaiah et al.   Future Oncology

Histone deacetylase inhibitors enhance the anticancer activity of nutlin-3 and induce p53 hyperacetylation and downregulation of MDM2 and MDM4 gene expression

(2010) Chithra D. Palani et al.   INVESTIGATIONAL NEW DRUGS

Phase I study of vorinostat (suberoylanilide hydroxamic acid, NSC 701852) in combination with docetaxel in patients with advanced and relapsed solid malignancies

(2010) Bryan J. Schneider et al.   INVESTIGATIONAL NEW DRUGS

The Role of HDAC6 in Cancer

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

Pazopanib in Locally Advanced or Metastatic Renal Cell Carcinoma: Results of a Randomized Phase III Trial

(2010) Cora N. Sternberg et al.   JOURNAL OF CLINICAL ONCOLOGY

Discovery of 7-(4-(3-Ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDC-101) as a Potent Multi-Acting HDAC, EGFR, and HER2 Inhibitor for the Treatment of Cancer

(2010) Xiong Cai et al.   JOURNAL OF MEDICINAL CHEMISTRY

Isoform-selective HDAC inhibitors: Closing in on translational medicine for the heart

(2010) Timothy A. McKinsey   JOURNAL OF MOLECULAR AND CELLULAR CARDIOLOGY

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

Vorinostat (NSC# 701852) in Patients with Relapsed Non-small Cell Lung Cancer: A Wisconsin Oncology Network Phase II Study

(2010) Anne M. Traynor et al.   Journal of Thoracic Oncology

Regulation of Cellular Metabolism by Protein Lysine Acetylation

(2010) S. Zhao et al.   SCIENCE

Safety and efficacy of NAD depleting cancer drugs: results of a phase I clinical trial of CHS 828 and overview of published data

(2009) Anne von Heideman et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Histone Deacetylase Inhibitors in Cancer Therapy

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

Design of Chimeric Histone Deacetylase- and Tyrosine Kinase-Inhibitors: A Series of Imatinib Hybrides as Potent Inhibitors of Wild-Type and Mutant BCR-ABL, PDGF-Rβ, and Histone Deacetylases†

(2009) Siavosh Mahboobi et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Novel Potent Nicotinamide Phosphoribosyltransferase Inhibitor Synthesized via Click Chemistry

(2009) Giampiero Colombano et al.   JOURNAL OF MEDICINAL CHEMISTRY

Phosphodiesterase 5 Inhibition Improves Synaptic Function, Memory, and Amyloid-  Load in an Alzheimer's Disease Mouse Model

(2009) D. Puzzo et al.   JOURNAL OF NEUROSCIENCE

Histone Deacetylase Inhibitor Romidepsin Enhances Anti-Tumor Effect of Erlotinib in Non-small Cell Lung Cancer (NSCLC) Cell Lines

(2009) Wei Zhang et al.   Journal of Thoracic Oncology

Synergistic drug combinations tend to improve therapeutically relevant selectivity

(2009) Joseph Lehár et al.   NATURE BIOTECHNOLOGY

Inhibitors of Class 1 Histone Deacetylases Reverse Contextual Memory Deficits in a Mouse Model of Alzheimer's Disease

(2009) Mark Kilgore et al.   NEUROPSYCHOPHARMACOLOGY

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

(2009) C. Choudhary et al.   SCIENCE

Multiple roles of HDAC inhibition in neurodegenerative conditions

(2009) De-Maw Chuang et al.   TRENDS IN NEUROSCIENCES

Targeted intracellular protein degradation induced by a small molecule: En route to chemical proteomics

(2008) Ashley R. Schneekloth et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

HDAC family: What are the cancer relevant targets?

(2008) Olaf Witt et al.   CANCER LETTERS

Zinc-Binding Groups Modulate Selective Inhibition of MMPs

(2008) Arpita Agrawal et al.   ChemMedChem

A Phase II Trial of Vorinostat (Suberoylanilide Hydroxamic Acid) in Metastatic Breast Cancer: A California Cancer Consortium Study

(2008) T. H. Luu et al.   CLINICAL CANCER RESEARCH

Phase II trial of romidepsin (NSC-630176) in previously treated colorectal cancer patients with advanced disease: a Southwest Oncology Group study (S0336)

(2008) Robert P. Whitehead et al.   INVESTIGATIONAL NEW DRUGS

Early phase II trial of oral vorinostat in relapsed or refractory breast, colorectal, or non-small cell lung cancer

(2008) Johan Vansteenkiste et al.   INVESTIGATIONAL NEW DRUGS

Pimelic Diphenylamide 106 Is a Slow, Tight-binding Inhibitor of Class I Histone Deacetylases

(2008) C. James Chou et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Lack of Therapeutic Effect of the Histone Deacetylase Inhibitor Vorinostat in Patients with Metastatic Radioiodine-Refractory Thyroid Carcinoma

(2008) Jennifer A. Woyach et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

The HDAC inhibitor 4b ameliorates the disease phenotype and transcriptional abnormalities in Huntington's disease transgenic mice

(2008) E. A. Thomas et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2)

(2007) David J. Witter et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Exploration of the internal cavity of histone deacetylase (HDAC) with selective HDAC1/HDAC2 inhibitors (SHI-1:2)

(2007) Joey L. Methot et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS