Targeting both BET and CBP/EP300 proteins with the novel dual inhibitors NEO2734 and NEO1132 leads to anti‐tumor activity in multiple myeloma

Combined targeting of the BRD4-NUT-p300 axis in NUT midline carcinoma by dual selective bromodomain inhibitor, NEO2734

(2020) Chevaun D Morrison-Smith et al.   MOLECULAR CANCER THERAPEUTICS

Antitumor activity of the dual BET and CBP/EP300 inhibitor NEO2734

(2020) Filippo Spriano et al.   Blood Advances

Identification of lenalidomide resistance pathways in myeloma and targeted resensitization using cereblon replacement, inhibition of STAT3 or targeting of IRF4

(2019) Yuan Xiao Zhu et al.   Blood Cancer Journal

Y08197 is a novel and selective CBP/EP300 bromodomain inhibitor for the treatment of prostate cancer

(2019) Ling-jiao Zou et al.   ACTA PHARMACOLOGICA SINICA

Bromodomain inhibition of the coactivators CBP/EP300 facilitate cellular reprogramming

(2019) Ayyub Ebrahimi et al.   Nature Chemical Biology

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

The BET bromodomain inhibitor CPI203 improves lenalidomide and dexamethasone activity in in vitro and in vivo models of multiple myeloma by blockade of Ikaros and MYC signaling

(2017) Tania Díaz et al.   HAEMATOLOGICA

BET Proteins as Targets for Anticancer Treatment

(2017) Anastasios Stathis et al.   Cancer Discovery

The BET bromodomain inhibitor CPI203 improves lenalidomide and dexamethasone activity in in vitro and in vivo models of multiple myeloma by blockade of Ikaros and MYC signaling

(2017) Tania Díaz et al.   HAEMATOLOGICA

Antimyeloma activity of bromodomain inhibitors on the human myeloma cell line U266 by downregulation of MYCL

(2016) Kazuhito Suzuki et al.   ANTI-CANCER DRUGS

Novel agents in the treatment of multiple myeloma: a review about the future

(2016) Leonard Naymagon et al.   Journal of Hematology & Oncology

CBP/p300 acetyltransferase activity in hematologic malignancies

(2016) Ritika Dutta et al.   MOLECULAR GENETICS AND METABOLISM

Genomic complexity of multiple myeloma and its clinical implications

(2016) Salomon Manier et al.   Nature Reviews Clinical Oncology

Nonselective inhibition of the epigenetic transcriptional regulator BET induces marked lymphoid and hematopoietic toxicity in mice

(2016) Dong U. Lee et al.   TOXICOLOGY AND APPLIED PHARMACOLOGY

Bromodomain inhibition of the transcriptional coactivators CBP/EP300 as a therapeutic strategy to target the IRF4 network in multiple myeloma

(2016) Andrew R Conery et al.   eLife

Small molecule inhibitor screen identifies synergistic activity of the bromodomain inhibitor CPI203 and bortezomib in drug resistant myeloma

(2015) Matthew B. Siegel et al.   Oncotarget

Synergistic antitumor activity of lenalidomide with the BET bromodomain inhibitor CPI203 in bortezomib-resistant mantle cell lymphoma

(2014) A Moros et al.   LEUKEMIA

Targeting bromodomains: epigenetic readers of lysine acetylation

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

The role of epigenetics in the biology of multiple myeloma

(2014) K Dimopoulos et al.   Blood Cancer Journal

Translocations at 8q24 juxtapose MYC with genes that harbor superenhancers resulting in overexpression and poor prognosis in myeloma patients

(2014) B A Walker et al.   Blood Cancer Journal

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

(2013) A. Chaidos et al.   BLOOD

Transcriptional/epigenetic regulator CBP/p300 in tumorigenesis: structural and functional versatility in target recognition

(2013) Feng Wang et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

MYC addiction: a potential therapeutic target in MM

(2012) W. M. Kuehl et al.   BLOOD

Integrative genome analyses identify key somatic driver mutations of small-cell lung cancer

(2012) Martin Peifer et al.   NATURE GENETICS

BET Bromodomain Inhibition as a Therapeutic Strategy to Target c-Myc

(2011) Jake E. Delmore et al.   CELL

Clinical and biological implications of MYC activation: a common difference between MGUS and newly diagnosed multiple myeloma

(2011) W-J Chng et al.   LEUKEMIA

Inactivating mutations of acetyltransferase genes in B-cell lymphoma

(2011) Laura Pasqualucci et al.   NATURE

RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia

(2011) Johannes Zuber et al.   NATURE

Multiple Myeloma

(2011) Antonio Palumbo et al.   NEW ENGLAND JOURNAL OF MEDICINE

Targeting MYC dependence in cancer by inhibiting BET bromodomains

(2011) J. A. Mertz et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Survival and Years of Life Lost in Different Age Cohorts of Patients With Multiple Myeloma

(2010) Heinz Ludwig et al.   JOURNAL OF CLINICAL ONCOLOGY

Suppression of inflammation by a synthetic histone mimic

(2010) Edwige Nicodeme et al.   NATURE

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE

Gene Expression Profiles of Tumor Biology Provide a Novel Approach to Prognosis and May Guide the Selection of Therapeutic Targets in Multiple Myeloma

(2009) Ariel Anguiano et al.   JOURNAL OF CLINICAL ONCOLOGY

The Bromodomain Protein Brd4 Stimulates G1Gene Transcription and Promotes Progression to S Phase

(2008) Kazuki Mochizuki et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

IRF4 addiction in multiple myeloma

(2008) Arthur L. Shaffer et al.   NATURE