Achieving clinical success with BET inhibitors as anti-cancer agents

T Shorstova, WD Foulkes, M Witcher - British journal of cancer, 2021 - nature.com
The transcriptional upregulation of oncogenes is a driving force behind the progression of
many tumours. However, until a decade ago, the concept of 'switching off'these oncogenic …

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 …

Histone modifications and cancer

JE Audia, RM Campbell - Cold Spring Harbor …, 2016 - cshperspectives.cshlp.org
Histone posttranslational modifications represent a versatile set of epigenetic marks
involved not only in dynamic cellular processes, such as transcription and DNA repair, but …

Epigenetics in cancer stem cells

TB Toh, JJ Lim, EKH Chow - Molecular cancer, 2017 - Springer
Compelling evidence have demonstrated that bulk tumors can arise from a unique subset of
cells commonly termed “cancer stem cells” that has been proposed to be a strong driving …

Targeting bromodomains: epigenetic readers of lysine acetylation

P Filippakopoulos, S Knapp - Nature reviews Drug discovery, 2014 - nature.com
Lysine acetylation is a key mechanism that regulates chromatin structure; aberrant
acetylation levels have been linked to the development of several diseases. Acetyl-lysine …

Molecular targeting therapies for neuroblastoma: Progress and challenges

A Zafar, W Wang, G Liu, X Wang, W Xian… - Medicinal research …, 2021 - Wiley Online Library
There is an urgent need to identify novel therapies for childhood cancers. Neuroblastoma is
the most common pediatric solid tumor, and accounts for~ 15% of childhood cancer‐related …

CDK7 inhibition suppresses super-enhancer-linked oncogenic transcription in MYCN-driven cancer

E Chipumuro, E Marco, CL Christensen, N Kwiatkowski… - Cell, 2014 - cell.com
The MYC oncoproteins are thought to stimulate tumor cell growth and proliferation through
amplification of gene transcription, a mechanism that has thwarted most efforts to inhibit …

CDK7-dependent transcriptional addiction in triple-negative breast cancer

Y Wang, T Zhang, N Kwiatkowski, BJ Abraham, TI Lee… - Cell, 2015 - cell.com
Triple-negative breast cancer (TNBC) is a highly aggressive form of breast cancer that
exhibits extremely high levels of genetic complexity and yet a relatively uniform …

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 …

Drug discovery targeting bromodomain-containing protein 4

Z Liu, P Wang, H Chen, EA Wold, B Tian… - Journal of medicinal …, 2017 - ACS Publications
BRD4, the most extensively studied member of the BET family, is an epigenetic regulator
that localizes to DNA via binding to acetylated histones and controls the expression of …