Epigenetic regulation in human cancer: the potential role of epi-drug in cancer therapy

Y Lu, YT Chan, HY Tan, S Li, N Wang, Y Feng - Molecular cancer, 2020 - Springer
Epigenetics is dynamic and heritable modifications to the genome that occur independently
of DNA sequence. It requires interactions cohesively with various enzymes and other …

Combining epigenetic drugs with other therapies for solid tumours—past lessons and future promise

D Morel, D Jeffery, S Aspeslagh, G Almouzni… - Nature Reviews …, 2020 - nature.com
Epigenetic dysregulation has long been recognized as a key factor contributing to
tumorigenesis and tumour maintenance that can influence all of the recognized hallmarks of …

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 …

Bromodomain and extra-terminal motif inhibitors: a review of preclinical and clinical advances in cancer therapy

A Alqahtani, K Choucair, M Ashraf… - Future science …, 2019 - Taylor & Francis
Histone lysine acetylation is critical in regulating transcription. Dysregulation of this process
results in aberrant gene expression in various diseases, including cancer. The …

Synthetic lethal combination targeting BET uncovered intrinsic susceptibility of TNBC to ferroptosis

N Verma, Y Vinik, A Saroha, NU Nair, E Ruppin… - Science …, 2020 - science.org
Identification of targeted therapies for TNBC is an urgent medical need. Using a drug
combination screen reliant on synthetic lethal interactions, we identified clinically relevant …

A validation and extended description of the Lund taxonomy for urothelial carcinoma using the TCGA cohort

N Marzouka, P Eriksson, C Rovira, F Liedberg… - Scientific reports, 2018 - nature.com
Global gene expression analysis has been a major tool for urothelial carcinoma subtype
discovery. This approach has revealed extensive complexity both in intrinsic features of the …

A chemical toolbox for the study of bromodomains and epigenetic signaling

Q Wu, D Heidenreich, S Zhou, S Ackloo… - Nature …, 2019 - nature.com
Bromodomains (BRDs) are conserved protein interaction modules which recognize (read)
acetyl-lysine modifications, however their role (s) in regulating cellular states and their …

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 …

Bromodomain and extraterminal (BET) proteins: biological functions, diseases, and targeted therapy

ZQ Wang, ZC Zhang, YY Wu, YN Pi, SH Lou… - Signal transduction and …, 2023 - nature.com
BET proteins, which influence gene expression and contribute to the development of cancer,
are epigenetic interpreters. Thus, BET inhibitors represent a novel form of epigenetic …

Emerging epigenetic-modulating therapies in lymphoma

D Sermer, L Pasqualucci, HG Wendel… - Nature reviews Clinical …, 2019 - nature.com
Despite considerable advances in the treatment of lymphoma, the prognosis of patients with
relapsed and/or refractory disease continues to be poor; thus, a continued need exists for …