[HTML][HTML] BET inhibitors: a novel epigenetic approach
DB Doroshow, JP Eder, PM LoRusso - Annals of Oncology, 2017 - Elsevier
Epigenetics has been defined as 'the structural adaptation of chromosomal regions so as to
register, signal or perpetuate altered activity states.'Currently, several classes of anticancer …
register, signal or perpetuate altered activity states.'Currently, several classes of anticancer …
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 …
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 …
The bromodomain and extra-terminal domain (BET) family: functional anatomy of BET paralogous proteins
Y Taniguchi - International journal of molecular sciences, 2016 - mdpi.com
The Bromodomain and Extra-Terminal Domain (BET) family of proteins is characterized by
the presence of two tandem bromodomains and an extra-terminal domain. The mammalian …
the presence of two tandem bromodomains and an extra-terminal domain. The mammalian …
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 …
The expanding world of N-MYC–driven tumors
DS Rickman, JH Schulte, M Eilers - Cancer discovery, 2018 - AACR
Enhanced and deregulated expression of N-MYC, a member of the MYC family of
transcription factors, drives the development of multiple tumors, including tumors of the …
transcription factors, drives the development of multiple tumors, including tumors of the …
Regulation of prostate cancer progression by the tumor microenvironment
SL Shiao, GCY Chu, LWK Chung - Cancer letters, 2016 - Elsevier
Prostate cancer remains the most frequently diagnosed cancer in men in North America, and
despite recent advances in treatment patients with metastatic disease continue to have poor …
despite recent advances in treatment patients with metastatic disease continue to have poor …
[HTML][HTML] Inhibition of BET bromodomains as a therapeutic strategy for cancer drug discovery
As a conserved protein interaction module that recognizes and binds to acetylated lysine,
bromodomain (BRD) contains a deep, largely hydrophobic acetyl lysine binding site …
bromodomain (BRD) contains a deep, largely hydrophobic acetyl lysine binding site …
The oncogenic BRD4-NUT chromatin regulator drives aberrant transcription within large topological domains
AA Alekseyenko, EM Walsh, X Wang… - Genes & …, 2015 - genesdev.cshlp.org
NUT midline carcinoma (NMC), a subtype of squamous cell cancer, is one of the most
aggressive human solid malignancies known. NMC is driven by the creation of a …
aggressive human solid malignancies known. NMC is driven by the creation of a …
The bromodomain: from epigenome reader to druggable target
R Sanchez, J Meslamani, MM Zhou - Biochimica et Biophysica Acta (BBA) …, 2014 - Elsevier
Lysine acetylation is a fundamental post-translational modification that plays an important
role in the control of gene transcription in chromatin in an ordered fashion. The …
role in the control of gene transcription in chromatin in an ordered fashion. The …