PROTAC induced-BET protein degradation exhibits potent anti-osteosarcoma activity by triggering apoptosis

Experimental Characterization of the Binding Affinities between Proapoptotic BH3 Peptides and Antiapoptotic Bcl-2 Proteins

(2018) Wenna Kong et al.   ChemMedChem

Inhibition of Mcl-1 enhances Pevonedistat-triggered apoptosis in osteosarcoma cells

(2017) Yi Zhang et al.   EXPERIMENTAL CELL RESEARCH

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

Novel BET protein proteolysis-targeting chimera exerts superior lethal activity than bromodomain inhibitor (BETi) against post-myeloproliferative neoplasm secondary (s) AML cells

(2017) D T Saenz et al.   LEUKEMIA

Targeting BET proteins improves the therapeutic efficacy of BCL-2 inhibition in T-cell acute lymphoblastic leukemia

(2017) S Peirs et al.   LEUKEMIA

PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer

(2016) Kanak Raina et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Broad targeting of resistance to apoptosis in cancer

(2015) Ramzi M. Mohammad et al.   SEMINARS IN CANCER BIOLOGY

BET inhibitors induce apoptosis through a MYC independent mechanism and synergise with CDK inhibitors to kill osteosarcoma cells

(2015) Emma K Baker et al.   Scientific Reports

BET bromodomain protein inhibition is a therapeutic option for medulloblastoma

(2015) Anton George Henssen et al.   Oncotarget

Synergistic effect of JQ1 and rapamycin for treatment of human osteosarcoma

(2014) Dhong Hyun Lee et al.   INTERNATIONAL JOURNAL OF CANCER

BET Protein Antagonist JQ1 Is Synergistically Lethal with FLT3 Tyrosine Kinase Inhibitor (TKI) and Overcomes Resistance to FLT3-TKI in AML Cells Expressing FLT-ITD

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

Selective inhibition of BET bromodomain epigenetic signalling interferes with the bone-associated tumour vicious cycle

(2014) François Lamoureux et al.   Nature Communications

Patient-Derived Xenograft Models: An Emerging Platform for Translational Cancer Research

(2014) M. Hidalgo et al.   Cancer Discovery

MicroRNA-133a, downregulated in osteosarcoma, suppresses proliferation and promotes apoptosis by targeting Bcl-xL and Mcl-1

(2013) Fang Ji et al.   BONE

Osteosarcoma treatment – Where do we stand? A state of the art review

(2013) Anja Luetke et al.   CANCER TREATMENT REVIEWS

Selective Inhibition of Tumor Oncogenes by Disruption of Super-Enhancers

(2013) Jakob Lovén et al.   CELL

Rise of the Selective Inhibitors of Anti-Apoptotic Bcl-2 Family Proteins

(2013) Li Han et al.   ChemMedChem

BRD4 associates with p53 in DNMT3A-mutated leukemia cells and is implicated in apoptosis by the bromodomain inhibitor JQ1

(2013) Helen Jayne Susan Stewart et al.   Cancer Medicine

Functional and biological analysis of Bcl-xL expression in human osteosarcoma

(2010) Zhao-Xia Wang et al.   BONE

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE

The ubiquitin pathway: An emerging drug target in cancer therapy

(2009) Sudharsana Rao Ande et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Molecular Details of Bax Activation, Oligomerization, and Membrane Insertion

(2009) Stephanie Bleicken et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Sorafenib blocks tumour growth, angiogenesis and metastatic potential in preclinical models of osteosarcoma through a mechanism potentially involving the inhibition of ERK1/2, MCL-1 and ezrin pathways

(2009) Ymera Pignochino et al.   Molecular Cancer