Current status in the discovery of dual BET/HDAC inhibitors

Potent Dual BET/HDAC Inhibitors for Efficient Treatment of Pancreatic Cancer

(2020) Shipeng He et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

The novel dual BET/HDAC inhibitor TW09 mediates cell death by mitochondrial apoptosis in rhabdomyosarcoma cells

(2020) Stephanie Laszig et al.   CANCER LETTERS

Novel strategies targeting bromodomain-containing protein 4 (BRD4) for cancer drug discovery

(2020) Dailin Liang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Thieno[2,3-d]pyrimidine-Based Hydroxamic Acid Derivatives as Bromodomain-Containing Protein 4/Histone Deacetylase Dual Inhibitors Induce Autophagic Cell Death in Colorectal Carcinoma Cells

(2020) Zhaoping Pan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Dual-Target Inhibitors Based on HDACs: Novel Antitumor Agents for Cancer Therapy

(2020) Tingting Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Combination BET Family Protein and HDAC Inhibition Synergistically Elicits Chondrosarcoma Cell Apoptosis Through RAD51-Related DNA Damage Repair

(2020) Songwei Huan et al.   Cancer Management and Research

Inhibition of BET Proteins and Histone Deacetylase (HDACs): Crossing Roads in Cancer Therapy

(2019) Gloria Manzotti et al.   Cancers

Identification and Characterization of AES-135, a Hydroxamic Acid-Based HDAC Inhibitor That Prolongs Survival in an Orthotopic Mouse Model of Pancreatic Cancer

(2019) Andrew E. Shouksmith et al.   JOURNAL OF MEDICINAL CHEMISTRY

Ferritinophagy is required for the induction of ferroptosis by the bromodomain protein BRD4 inhibitor (+)-JQ1 in cancer cells

(2019) Shiyao Sui et al.   Cell Death & Disease

BRD4 inhibitor and histone deacetylase inhibitor synergistically inhibit the proliferation of gallbladder cancer in vitro and in vivo

(2019) Shilei Liu et al.   CANCER SCIENCE

Apabetalone (RVX-208) reduces vascular inflammation in vitro and in CVD patients by a BET-dependent epigenetic mechanism

(2019) Laura M. Tsujikawa et al.   Clinical Epigenetics

Suppression of BCL6 function by HDAC inhibitor mediated acetylation and chromatin modification enhances BET inhibitor effects in B-cell lymphoma cells

(2019) María G. Cortiguera et al.   Scientific Reports

Co-targeting of BET proteins and HDACs as a novel approach to trigger apoptosis in rhabdomyosarcoma cells

(2018) Julius C. Enßle et al.   CANCER LETTERS

Dual or multi-targeting inhibitors: The next generation anticancer agents

(2018) Nulgumnalli Manjunathaiah Raghavendra et al.   EUROPEAN 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

BET inhibition in advanced cutaneous T cell lymphoma is synergistically potentiated by BCL2 inhibition or HDAC inhibition

(2018) Sa Rang Kim et al.   Oncotarget

Combined inhibition of BET proteins and class I HDACs synergistically induces apoptosis in urothelial carcinoma cell lines

(2018) Alexander S. Hölscher et al.   Clinical Epigenetics

Combined HDAC and BET Inhibition Enhances Melanoma Vaccine Immunogenicity and Efficacy

(2018) Alexander Badamchi-Zadeh et al.   JOURNAL OF IMMUNOLOGY

HDAC stimulates gene expression through BRD4 availability in response to IFN and in interferonopathies

(2018) Isabelle J. Marié et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy

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

NF-κB signaling activation via increases in BRD2 and BRD4 confers resistance to the bromodomain inhibitor I-BET151 in U937 cells

(2018) Kotaro Hishiki et al.   LEUKEMIA RESEARCH

BRD4 and Cancer: going beyond transcriptional regulation

(2018) Benedetta Donati et al.   Molecular Cancer

Preclinical Studies Support Combined Inhibition of BET Family Proteins and Histone Deacetylases as Epigenetic Therapy for Cutaneous T-Cell Lymphoma

(2018) Lei Zhao et al.   NEOPLASIA

Design, synthesis and biological evaluation of novel indole derivatives as potential HDAC/BRD4 dual inhibitors and anti-leukemia agents

(2018) Gaoliang Cheng et al.   BIOORGANIC CHEMISTRY

Pendant HDAC inhibitor SAHA derivatised polymer as a novel prodrug micellar carrier for anticancer drugs

(2017) Jieni Xu et al.   JOURNAL OF DRUG TARGETING

Design, Multicomponent Synthesis, and Anticancer Activity of a Focused Histone Deacetylase (HDAC) Inhibitor Library with Peptoid-Based Cap Groups

(2017) Viktoria Krieger et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Alkoxyurea-Based Histone Deacetylase Inhibitors Increase Cisplatin Potency in Chemoresistant Cancer Cell Lines

(2017) Katharina Stenzel et al.   JOURNAL OF MEDICINAL CHEMISTRY

Drug Discovery Targeting Bromodomain-Containing Protein 4

(2017) Zhiqing Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives

(2017) Gebremedhin S. Hailu 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

Histone deacetylase class-I inhibition promotes epithelial gene expression in pancreatic cancer cells in a BRD4- and MYC-dependent manner

(2017) Vivek Kumar Mishra et al.   NUCLEIC ACIDS RESEARCH

Selective BET bromodomain inhibition as an antifungal therapeutic strategy

(2017) Flore Mietton et al.   Nature Communications

Combination therapy in combating cancer

(2017) Reza Bayat Mokhtari et al.   Oncotarget

Targeting epigenetic reader and eraser: Rational design, synthesis and in vitro evaluation of dimethylisoxazoles derivatives as BRD4/HDAC dual inhibitors

(2016) Zhimin Zhang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Histone Deacetylase Inhibitors Repress Tumoral Expression of the Proinvasive Factor RUNX2

(2015) V. Sancisi et al.   CANCER RESEARCH

Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors

(2015) F. Anthony Romero et al.   JOURNAL OF MEDICINAL CHEMISTRY

BET inhibitor resistance emerges from leukaemia stem cells

(2015) Chun Yew Fong et al.   NATURE

Combined inhibition of BET family proteins and histone deacetylases as a potential epigenetics-based therapy for pancreatic ductal adenocarcinoma

(2015) Pawel K Mazur et al.   NATURE MEDICINE

Induction of USP17 by combining BET and HDAC inhibitors in breast cancer cells

(2015) Gabor Borbely et al.   Oncotarget

Highly Active Combination of BRD4 Antagonist and Histone Deacetylase Inhibitor against Human Acute Myelogenous Leukemia Cells

(2014) W. Fiskus et al.   MOLECULAR CANCER THERAPEUTICS

The Mechanisms behind the Therapeutic Activity of BET Bromodomain Inhibition

(2014) Junwei Shi et al.   MOLECULAR CELL

BET and HDAC inhibitors induce similar genes and biological effects and synergize to kill in Myc-induced murine lymphoma

(2014) Joydeep Bhadury et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The structure based design of dual HDAC/BET inhibitors as novel epigenetic probes

(2014) Stephen J. Atkinson et al.   MedChemComm

Histone deacetylases inhibitors: conjugation to other anti-tumour pharmacophores provides novel tools for cancer treatment

(2013) Konstantinos A Papavassiliou et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands

(2013) David S. Hewings et al.   JOURNAL OF MEDICINAL CHEMISTRY

HDAC inhibitors induce transcriptional repression of high copy number genes in breast cancer through elongation blockade

(2013) Y J Kim et al.   ONCOGENE

RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain

(2013) S. Picaud et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

CUDC-101, a Multitargeted Inhibitor of Histone Deacetylase, Epidermal Growth Factor Receptor, and Human Epidermal Growth Factor Receptor 2, Exerts Potent Anticancer Activity

(2010) Cheng-Jung Lai et al.   CANCER RESEARCH

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE