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 …
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
Epigenetics is dynamic and heritable modifications to the genome that occur independently
of DNA sequence. It requires interactions cohesively with various enzymes and other …
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 …
involved not only in dynamic cellular processes, such as transcription and DNA repair, but …
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 …
acetylation levels have been linked to the development of several diseases. Acetyl-lysine …
Molecular targeting therapies for neuroblastoma: Progress and challenges
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 …
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 …
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 …
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 …
results in aberrant gene expression in various diseases, including cancer. The …
Drug discovery targeting bromodomain-containing protein 4
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 …
that localizes to DNA via binding to acetylated histones and controls the expression of …