Optimization of Class I Histone Deacetylase PROTACs Reveals that HDAC1/2 Degradation is Critical to Induce Apoptosis and Cell Arrest in Cancer Cells

Proteolysis-Targeting Chimeras as Therapeutics and Tools for Biological Discovery

(2020) George M. Burslem et al.   CELL

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

Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight

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

Induced protein degradation of histone deacetylases 3 (HDAC3) by proteolysis targeting chimera (PROTAC)

(2020) Fangyuan Cao et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase

(2019) Blake E. Smith et al.   Nature Communications

A comparative safety review of histone deacetylase inhibitors for the treatment of myeloma

(2019) Guldane Cengiz Seval et al.   Expert Opinion On Drug Safety

Decreased DHRS2 expression is associated with HDACi resistance and poor prognosis in ovarian cancer

(2019) Yingyan Han et al.   Epigenetics

Discovery of Highly Potent and Efficient PROTAC Degraders of Androgen Receptor (AR) by Employing Weak Binding Affinity VHL E3 Ligase Ligands

(2019) Xin Han et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

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

The Process and Strategy for Developing Selective Histone Deacetylase 3 Inhibitors

(2018) et al.   MOLECULES

Targeting the CoREST complex with dual histone deacetylase and demethylase inhibitors

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

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

Group-Based Optimization of Potent and Cell-Active Inhibitors of the von Hippel–Lindau (VHL) E3 Ubiquitin Ligase: Structure–Activity Relationships Leading to the Chemical Probe (2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (VH298)

(2017) Pedro Soares et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting Class I Histone Deacetylases in a “Complex” Environment

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

Selective targeting of HDAC1/2 elicits anticancer effects through Gli1 acetylation in preclinical models of SHH Medulloblastoma

(2017) Sonia Coni et al.   Scientific Reports

SwissADME: a free web tool to evaluate pharmacokinetics, drug-likeness and medicinal chemistry friendliness of small molecules

(2017) Antoine Daina et al.   Scientific Reports

Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition

(2016) Julianty Frost et al.   Nature Communications

Why Hydroxamates May Not Be the Best Histone Deacetylase Inhibitors-What Some May Have Forgotten or Would Rather Forget?

(2015) Sida Shen et al.   ChemMedChem

Selective Inhibition of HDAC1 and HDAC2 as a Potential Therapeutic Option for B-ALL

(2015) M. C. Stubbs et al.   CLINICAL CANCER RESEARCH

HDAC inhibitors still need a home run, despite recent approval

(2015) Malini Guha   NATURE REVIEWS DRUG DISCOVERY

Histone deacetylase (HDAC) 1 and 2 are essential for accurate cell division and the pluripotency of embryonic stem cells

(2014) Shereen Jamaladdin et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Selective HDAC1/HDAC2 Inhibitors Induce Neuroblastoma Differentiation

(2013) Stacey M. Frumm et al.   CHEMISTRY & BIOLOGY

Histone deacetylase 3 as a novel therapeutic target in multiple myeloma

(2013) J Minami et al.   LEUKEMIA

Deacetylase-Independent Function of HDAC3 in Transcription and Metabolism Requires Nuclear Receptor Corepressor

(2013) Zheng Sun et al.   MOLECULAR CELL

Inhibition of Histone Deacetylase 3 Causes Replication Stress in Cutaneous T Cell Lymphoma

(2013) Christina E. Wells et al.   PLoS One

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

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

Mitochondrial HEP27 Is a c-Myb Target Gene That Inhibits Mdm2 and Stabilizes p53

(2010) C. Deisenroth et al.   MOLECULAR AND CELLULAR BIOLOGY

Chemical genetic strategy identifies histone deacetylase 1 (HDAC1) and HDAC2 as therapeutic targets in sickle cell disease

(2010) James E. Bradner et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Histone deacetylase 1 (HDAC1), but not HDAC2, controls embryonic stem cell differentiation

(2010) O. M. Dovey et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

A novel domain in histone deacetylase 1 and 2 mediates repression of cartilage-specific genes in human chondrocytes

(2009) Sohee Hong et al.   FASEB JOURNAL

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