A 7-methoxybicoumarin derivative selectively inhibits BRD4 BD2 for anti-melanoma therapy

Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer

(2020) Emily J. Faivre et al.   NATURE

Targeted chemotherapy overcomes drug resistance in melanoma

(2020) Jingyin Yue et al.   GENES & DEVELOPMENT

Discovery of N-Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain

(2020) George S. Sheppard et al.   JOURNAL OF MEDICINAL CHEMISTRY

Selective targeting of BD1 and BD2 of the BET proteins in cancer and immuno-inflammation

(2020) Omer Gilan et al.   SCIENCE

Structure-Based Discovery of a Selective KDM5A Inhibitor that Exhibits Anti-Cancer Activity via Inducing Cell Cycle Arrest and Senescence in Breast Cancer Cell Lines

(2019) Guan-Jun Yang et al.   Cancers

Emerging roles of and therapeutic strategies targeting BRD4 in cancer

(2019) Mary E. White et al.   CELLULAR IMMUNOLOGY

Bromodomain-Containing Protein 4: A Druggable Target

(2019) Yingying Shi et al.   CURRENT DRUG TARGETS

BET inhibitor JQ1 suppresses cell proliferation via inducing autophagy and activating LKB1/AMPK in bladder cancer cells

(2019) Feng Li et al.   Cancer Medicine

The Hippo pathway modulates resistance to BET proteins inhibitors in lung cancer cells

(2019) Giulia Gobbi et al.   ONCOGENE

Selective Inhibition of Lysine-Specific Demethylase 5A (KDM5A) Using a Rhodium(III) Complex for Triple-Negative Breast Cancer Therapy

(2018) Guan-Jun Yang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Identification of a rhodium(iii) complex as a Wee1 inhibitor against TP53-mutated triple-negative breast cancer cells

(2018) Guan-Jun Yang et al.   CHEMICAL COMMUNICATIONS

Small Molecule Pin1 Inhibitor Blocking NF-κB Signaling in Prostate Cancer Cells

(2018) Ke-Jia Wu et al.   Chemistry-An Asian Journal

Co‐targeting BET and MEK as salvage therapy for MAPK and checkpoint inhibitor‐resistant melanoma

(2018) Ileabett M Echevarría‐Vargas et al.   EMBO Molecular Medicine

Plk1 Inhibition Enhances the Efficacy of BET Epigenetic Reader Blockade in Castration-Resistant Prostate Cancer

(2018) Fengyi Mao et al.   MOLECULAR CANCER THERAPEUTICS

Toosendanin, a natural product, inhibited TGF-β1-induced epithelial-mesenchymal transition through ERK/Snail pathway

(2018) Weiwei Luo et al.   PHYTOTHERAPY RESEARCH

TIP60-dependent acetylation of the SPZ1-TWIST complex promotes epithelial–mesenchymal transition and metastasis in liver cancer

(2018) Li-Ting Wang et al.   ONCOGENE

Bromodomain Drug Discovery – the Past, the Present, and the Future

(2018) Mehrosh Pervaiz et al.   CHEMICAL RECORD

WNT5A supports viability of senescent human dental follicle cells

(2018) Christian Morsczeck et al.   MOLECULAR AND CELLULAR BIOCHEMISTRY

Combination therapy targeting the elevated interleukin-6 level reduces invasive migration of BRAF inhibitor-resistant melanoma cells

(2018) Purusottam Mohapatra et al.   Molecular Oncology

Targeting the BRD4/FOXO3a/CDK6 axis sensitizes AKT inhibition in luminal breast cancer

(2018) Jingyi Liu et al.   Nature Communications

The Development of Target-Specific Pose Filter Ensembles To Boost Ligand Enrichment for Structure-Based Virtual Screening

(2017) Jie Xia et al.   Journal of Chemical Information and Modeling

MiR-200a Regulates CDK4/6 Inhibitor Effect by Targeting CDK6 in Metastatic Melanoma

(2017) Matias A. Bustos et al.   JOURNAL OF INVESTIGATIVE DERMATOLOGY

Structure-Based Discovery of 4-(6-Methoxy-2-methyl-4-(quinolin-4-yl)-9H-pyrimido[4,5-b]indol-7-yl)-3,5-dimethylisoxazole (CD161) as a Potent and Orally Bioavailable BET Bromodomain Inhibitor

(2017) Yujun Zhao et al.   JOURNAL OF MEDICINAL CHEMISTRY

Harnessing BET Inhibitor Sensitivity Reveals AMIGO2 as a Melanoma Survival Gene

(2017) Barbara Fontanals-Cirera et al.   MOLECULAR CELL

Discovery of a VHL and HIF1α interaction inhibitor with in vivo angiogenic activity via structure-based virtual screening

(2016) Chao Yang et al.   CHEMICAL COMMUNICATIONS

Discovery and Optimization of a Selective Ligand for the Switch/Sucrose Nonfermenting-Related Bromodomains of Polybromo Protein-1 by the Use of Virtual Screening and Hydration Analysis

(2016) Vassilios Myrianthopoulos et al.   JOURNAL OF MEDICINAL CHEMISTRY

Scientists in the dark after French clinical trial proves fatal

(2016) Declan Butler et al.   NATURE

MiR-29b suppresses the proliferation and migration of osteosarcoma cells by targeting CDK6

(2016) Kegan Zhu et al.   Protein & Cell

Anticancer Gold(III) Porphyrins Target Mitochondrial Chaperone Hsp60

(2015) Di Hu et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Discovery of Natural Product-Derived 5-HT1A Receptor Binders by Cheminfomatics Modeling of Known Binders, High Throughput Screening and Experimental Validation

(2015) Man Luo et al.   COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING

Twist-BRD4 Complex: Potential Drug Target for Basal-like Breast Cancer

(2015) Jian Shi et al.   CURRENT PHARMACEUTICAL DESIGN

Molecular characterization and functional analysis of a novel C-type lectin receptor-like gene from a teleost fish, Plecoglossus altivelis

(2015) Guan-Jun Yang et al.   FISH & SHELLFISH IMMUNOLOGY

Virtual screening in small molecule discovery for epigenetic targets

(2015) Guo-Bo Li et al.   METHODS

The TNFα converting enzyme (TACE) from ayu (Plecoglossus altivelis) exhibits TNFα shedding activity

(2015) Xin-Jiang Lu et al.   MOLECULAR IMMUNOLOGY

An iridium(iii)-based irreversible protein–protein interaction inhibitor of BRD4 as a potent anticancer agent

(2015) Hai-Jing Zhong et al.   Chemical Science

Inhibition of BET bromodomain proteins as a therapeutic approach in prostate cancer.

(2015) Anastasia Wyce et al.   Oncotarget

A novel BET bromodomain inhibitor, RVX-208, shows reduction of atherosclerosis in hyperlipidemic ApoE deficient mice

(2014) Ravi Jahagirdar et al.   ATHEROSCLEROSIS

Structure-based repurposing of FDA-approved drugs as inhibitors of NEDD8-activating enzyme

(2014) Hai-Jing Zhong et al.   BIOCHIMIE

Disrupting the Interaction of BRD4 with Diacetylated Twist Suppresses Tumorigenesis in Basal-like Breast Cancer

(2014) Jian Shi et al.   CANCER CELL

The Epigenetic Regulator I-BET151 Induces BIM-Dependent Apoptosis and Cell Cycle Arrest of Human Melanoma Cells

(2014) Stuart J. Gallagher et al.   JOURNAL OF INVESTIGATIVE DERMATOLOGY

Acidic and Basic Drugs in Medicinal Chemistry: A Perspective

(2014) Paul S. Charifson et al.   JOURNAL OF MEDICINAL CHEMISTRY

WNT5A induces release of exosomes containing pro-angiogenic and immunosuppressive factors from malignant melanoma cells

(2014) Elin J Ekström et al.   Molecular Cancer

The Mechanisms behind the Therapeutic Activity of BET Bromodomain Inhibition

(2014) Junwei Shi et al.   MOLECULAR CELL

Therapeutic targeting of BET bromodomain proteins in castration-resistant prostate cancer

(2014) Irfan A. Asangani et al.   NATURE

Targeting bromodomains: epigenetic readers of lysine acetylation

(2014) Panagis Filippakopoulos et al.   NATURE REVIEWS DRUG DISCOVERY

Wnt5A promotes an adaptive, senescent-like stress response, while continuing to drive invasion in melanoma cells

(2014) Marie R. Webster et al.   Pigment Cell & Melanoma Research

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

Novel ferrocenyl derivatives exert anti-cancer effect in human lung cancer cells in vitro via inducing G1-phase arrest and senescence

(2013) Ying Li et al.   ACTA PHARMACOLOGICA SINICA

Structure–activity relationship studies of thalidomide analogs with a taxol-like mode of action

(2013) Bulbul Pandit et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762

(2013) A. Chaidos et al.   BLOOD

BRD4 Sustains Melanoma Proliferation and Represents a New Target for Epigenetic Therapy

(2013) M. F. Segura et al.   CANCER RESEARCH

FoxO3a Is an Antimelanogenic Factor that Mediates Antioxidant-Induced Depigmentation

(2013) Juewon Kim et al.   JOURNAL OF INVESTIGATIVE DERMATOLOGY

Discovery of Epigenetic Regulator I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains

(2013) Olivier Mirguet et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Making of I-BET762, a BET Bromodomain Inhibitor Now in Clinical Development

(2013) Yujun Zhao et al.   JOURNAL OF MEDICINAL CHEMISTRY

A small compound targeting TACC3 revealed its different spatiotemporal contributions for spindle assembly in cancer cells

(2013) R Yao 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

Monitoring Drug Target Engagement in Cells and Tissues Using the Cellular Thermal Shift Assay

(2013) D. M. Molina et al.   SCIENCE

A Systematic Screen for CDK4/6 Substrates Links FOXM1 Phosphorylation to Senescence Suppression in Cancer Cells

(2011) Lars Anders et al.   CANCER CELL

Normal and disease-related biological functions of Twist1 and underlying molecular mechanisms

(2011) Qian Qin et al.   CELL RESEARCH

Computational chemistry in 25 years

(2011) Ruben Abagyan   JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE

Combined Integrin Phosphoproteomic Analyses and Small Interfering RNA-Based Functional Screening Identify Key Regulators for Cancer Cell Adhesion and Migration

(2009) Y. Chen et al.   CANCER RESEARCH

Wnt5A Activates the Calpain-Mediated Cleavage of Filamin A

(2009) Michael P. O'Connell et al.   JOURNAL OF INVESTIGATIVE DERMATOLOGY

The orphan tyrosine kinase receptor, ROR2, mediates Wnt5A signaling in metastatic melanoma

(2009) M P O’Connell et al.   ONCOGENE

A t-butyloxycarbonyl-modified Wnt5a-derived hexapeptide functions as a potent antagonist of Wnt5a-dependent melanoma cell invasion

(2009) V. Jenei et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Generation of a Set of Simple, Interpretable ADMET Rules of Thumb

(2008) M. Paul Gleeson   JOURNAL OF MEDICINAL CHEMISTRY