[HTML][HTML] MYC as a target for cancer treatment

MJ Duffy, S O'Grady, M Tang, J Crown - Cancer treatment reviews, 2021 - Elsevier
The MYC gene which consists of 3 paralogs, C-MYC, N-MYC and L-MYC, is one of the most
frequently deregulated driver genes in human cancer. Because of its high prevalence of …

[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 …

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 …

[HTML][HTML] NRAS mutant melanoma: Towards better therapies

T Randic, I Kozar, C Margue, J Utikal, S Kreis - Cancer treatment reviews, 2021 - Elsevier
Genetic alterations affecting RAS proteins are commonly found in human cancers. Roughly
a fourth of melanoma patients carry activating NRAS mutations, rendering this malignancy …

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 …

First-in-human study of mivebresib (ABBV-075), an oral pan-inhibitor of bromodomain and extra terminal proteins, in patients with relapsed/refractory solid tumors

SA Piha-Paul, JC Sachdev, M Barve, P LoRusso… - Clinical Cancer …, 2019 - AACR
Purpose: Bromodomain and extraterminal (BET) proteins play important roles in
transcriptional regulation relevant to cancer pathogenesis, and therapeutic …

Kinase and BET inhibitors together clamp inhibition of PI3K signaling and overcome resistance to therapy

EE Stratikopoulos, M Dendy, M Szabolcs, AJ Khaykin… - Cancer cell, 2015 - cell.com
Unsustained enzyme inhibition is a barrier to targeted therapy for cancer. Here, resistance to
a class I PI3K inhibitor in a model of metastatic breast cancer driven by PI3K and MYC was …

Resistance to BET bromodomain inhibitors is mediated by kinome reprogramming in ovarian cancer

AM Kurimchak, C Shelton, KE Duncan, KJ Johnson… - Cell reports, 2016 - cell.com
Small-molecule BET bromodomain inhibitors (BETis) are actively being pursued in clinical
trials for the treatment of a variety of cancers, but the mechanisms of resistance to BETis …

Targeting post-translational histone modifying enzymes in glioblastoma

E Kunadis, E Lakiotaki, P Korkolopoulou… - Pharmacology & …, 2021 - Elsevier
Glioblastoma (GBM) is the most common primary brain tumor in adults, and the most lethal
form of glioma, characterized by variable histopathology, aggressiveness and poor clinical …

[HTML][HTML] Control of embryonic stem cell identity by BRD4-dependent transcriptional elongation of super-enhancer-associated pluripotency genes

R Di Micco, B Fontanals-Cirera, V Low, P Ntziachristos… - Cell reports, 2014 - cell.com
Transcription factors and chromatin-remodeling complexes are key determinants of
embryonic stem cell (ESC) identity. Here, we demonstrate that BRD4, a member of the …