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

Inhibitory selectivity among class I HDACs has a major impact on inflammatory gene expression in macrophages

(2019) Fangyuan Cao et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Targeted protein degradation: elements of PROTAC design

(2019) Stacey-Lynn Paiva et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Development of Multifunctional Histone Deacetylase 6 Degraders with Potent Antimyeloma Activity

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

Development of selective small molecule MDM2 degraders based on nutlin

(2019) Bo Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

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

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

Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK)

(2018) Chelsea E. Powell et al.   JOURNAL OF MEDICINAL CHEMISTRY

Pomalidomide promotes chemosensitization of pancreatic cancer by inhibition of NF-κB

(2018) Yoshihiro Shirai et al.   Oncotarget

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

Modulating PCAF/GCN5 Immune Cell Function through a PROTAC Approach

(2018) Zuni I. Bassi et al.   ACS Chemical Biology

β-adrenergic Receptor Stimulation Revealed a Novel Regulatory Pathway via Suppressing Histone Deacetylase 3 to Induce Uncoupling Protein 1 Expression in Mice Beige Adipocyte

(2018) Ana Yuliana et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Targeting breast cancer stem cells by novel HDAC3-selective inhibitors

(2017) Hao-Yu Hsieh et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Protac-Induced Protein Degradation in Drug Discovery: Breaking the Rules or Just Making New Ones?

(2017) Ian Churcher   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

Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression

(2017) Bing Zhou et al.   JOURNAL OF MEDICINAL CHEMISTRY

HDAC1-3 inhibitor MS-275 enhances IL10 expression in RAW264.7 macrophages and reduces cigarette smoke-induced airway inflammation in mice

(2017) Niek G. J. Leus et al.   Scientific Reports

HDAC 3-selective inhibitor RGFP966 demonstrates anti-inflammatory properties in RAW 264.7 macrophages and mouse precision-cut lung slices by attenuating NF-κB p65 transcriptional activity

(2016) Niek G.J. Leus et al.   BIOCHEMICAL PHARMACOLOGY

Histone deacetylase 3 (HDAC 3) as emerging drug target in NF-κB-mediated inflammation

(2016) Niek GJ Leus et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Inside HDACs with more selective HDAC inhibitors

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

Induced protein degradation: an emerging drug discovery paradigm

(2016) Ashton C. Lai et al.   NATURE REVIEWS DRUG DISCOVERY

An Isochemogenic Set of Inhibitors To Define the Therapeutic Potential of Histone Deacetylases in β-Cell Protection

(2015) Florence F. Wagner et al.   ACS Chemical Biology

Erasers of Histone Acetylation: The Histone Deacetylase Enzymes

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

Histone deacetylase inhibitors as potential treatment for spinal muscular atrophy

(2013) Jafar Mohseni et al.   GENETICS AND MOLECULAR BIOLOGY

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

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

(2012) Geneviève P Delcuve et al.   Clinical Epigenetics

Histone deacetylases and the immunological network: implications in cancer and inflammation

(2009) A Villagra et al.   ONCOGENE

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

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