BET proteins as targets for anticancer treatment
A Stathis, F Bertoni - Cancer discovery, 2018 - AACR
Bromodomain and extraterminal domain (BET) proteins are epigenetic readers that regulate
gene expression and are involved in cancer pathogenesis. Over the last years, several BET …
gene expression and are involved in cancer pathogenesis. Over the last years, several BET …
Bromodomain inhibitors and cancer therapy: From structures to applications
M Pérez-Salvia, M Esteller - Epigenetics, 2017 - Taylor & Francis
Aberrations in the epigenetic landscape are a hallmark of cancer. Alterations in enzymes
that are “writers,”“erasers,” or “readers” of histone modification marks are common …
that are “writers,”“erasers,” or “readers” of histone modification marks are common …
Bromodomains: Structure, function and pharmacology of inhibition
E Ferri, C Petosa, CE McKenna - Biochemical pharmacology, 2016 - Elsevier
Bromodomains are epigenetic readers of histone acetylation involved in chromatin
remodeling and transcriptional regulation. The human proteome comprises 46 …
remodeling and transcriptional regulation. The human proteome comprises 46 …
BET proteins as attractive targets for cancer therapeutics
J Sarnik, T Popławski, P Tokarz - International journal of molecular …, 2021 - mdpi.com
Transcriptional dysregulation is a hallmark of cancer and can be an essential driver of
cancer initiation and progression. Loss of transcriptional control can cause cancer cells to …
cancer initiation and progression. Loss of transcriptional control can cause cancer cells to …
Targeting BET bromodomain proteins in cancer: The example of lymphomas
Abstract The Bromo-and Extra-Terminal domain (BET) family proteins act as “readers” of
acetylated histones and they are important transcription regulators. BRD2, BRD3, BRD4 and …
acetylated histones and they are important transcription regulators. BRD2, BRD3, BRD4 and …
Epigenetics in multiple myeloma: From mechanisms to therapy
M Alzrigat, AA Párraga, H Jernberg-Wiklund - Seminars in cancer biology, 2018 - Elsevier
Multiple myeloma (MM) is a tumor of antibody producing plasmablasts/plasma cells that
resides within the bone marrow (BM). In addition to the well-established role of genetic …
resides within the bone marrow (BM). In addition to the well-established role of genetic …
The BET bromodomain inhibitor CPI203 overcomes resistance to ABT-199 (venetoclax) by downregulation of BFL-1/A1 in in vitro and in vivo models of MYC+/BCL2+ …
High-grade B-cell lymphoma with MYC and BCL2 and/or BCL6 rearrangements, mostly
known as double-hit lymphoma (DHL), is a rare entity characterized by morphologic and …
known as double-hit lymphoma (DHL), is a rare entity characterized by morphologic and …
The novel BET bromodomain inhibitor BI 894999 represses super-enhancer-associated transcription and synergizes with CDK9 inhibition in AML
D Gerlach, U Tontsch-Grunt, A Baum, J Popow… - Oncogene, 2018 - nature.com
Bromodomain and extra-terminal (BET) protein inhibitors have been reported as treatment
options for acute myeloid leukemia (AML) in preclinical models and are currently being …
options for acute myeloid leukemia (AML) in preclinical models and are currently being …
IRF4 in multiple myeloma—Biology, disease and therapeutic target
A Agnarelli, T Chevassut, EJ Mancini - Leukemia research, 2018 - Elsevier
Multiple Myeloma (MM) is an incurable hematologic malignancy characterized by abnormal
proliferation of plasma cells. Interferon Regulatory Factor 4 (IRF4), a member of the …
proliferation of plasma cells. Interferon Regulatory Factor 4 (IRF4), a member of the …
BET inhibitors in the treatment of hematologic malignancies: current insights and future prospects
SM Abedin, CS Boddy, HG Munshi - OncoTargets and therapy, 2016 - Taylor & Francis
The bromodomain and extra-terminal (BET) family of proteins are important epigenetic
regulators involved in promoting gene expression of critical oncogenes. BET inhibitors have …
regulators involved in promoting gene expression of critical oncogenes. BET inhibitors have …