Bromodomains and their pharmacological inhibitors

D Gallenkamp, KA Gelato, B Haendler… - …, 2014 - Wiley Online Library
Over 60 bromodomains belonging to proteins with very different functions have been
identified in humans. Several of them interact with acetylated lysine residues, leading to the …

Small molecule bromodomain inhibitors: extending the druggable genome

CW Chung - Progress in medicinal chemistry, 2012 - Elsevier
Bromodomains are modulators of protein–protein interactions essential for epigenetic
mechanisms of transcriptional control. The recent disclosure of potent, selective, small …

Lysine acetyltransferase GCN5 potentiates the growth of non-small cell lung cancer via promotion of E2F1, cyclin D1, and cyclin E1 expression

L Chen, T Wei, X Si, Q Wang, Y Li, Y Leng… - Journal of Biological …, 2013 - ASBMB
The lysine acetyltransferases play crucial but complex roles in cancer development. GCN5
is a lysine acetyltransferase that generally regulates gene expression, but its role in cancer …

Bromodomains: a new target class for small molecule drug discovery

C Chung, DF Tough - Drug Discovery Today: Therapeutic Strategies, 2012 - Elsevier
The recent disclosure of potent, selective small molecule inhibitors (I-BET762, I-BET151 and
JQ1) of the BET family of bromodomains demonstrate that epigenetic reader proteins may …

Epigenetic drugs against cancer: an evolving landscape

A Di Costanzo, N Del Gaudio, A Migliaccio… - Archives of toxicology, 2014 - Springer
Alteration of the chromatin orchestra seems to play a critical role in cancer. In recent years,
in-depth studies of epigenetic machinery and its deregulation have led to the development …

Nonhistone targets of KAT2A and KAT2B implicated in cancer biology

E Bondy-Chorney, A Denoncourt, Y Sai… - Biochemistry and Cell …, 2019 - cdnsciencepub.com
Lysine acetylation is a critical post-translation modification that can impact a protein's
localization, stability, and function. Originally thought to only occur on histones, we now …

Differential expression of histone deacetylase and acetyltransferase genes in gastric cancer and their modulation by trichostatin A

F Wisnieski, DQ Calcagno, MF Leal, ES Chen… - Tumor Biology, 2014 - Springer
Gastric cancer is still the second leading cause of cancer-related death worldwide, even
though its incidence and mortality have declined over the recent few decades. Epigenetic …

And-1 is required for the stability of histone acetyltransferase Gcn5

Y Li, AN Jaramillo-Lambert, Y Yang, R Williams… - Oncogene, 2012 - nature.com
Histone acetyltransferases (HATs) have a central role in the modification of chromatin as
well as in the pathogenesis of a broad set of diseases including cancers. Gcn5 is the first …

Cell cycle-dependent changes in H3K56ac in human cells

S Stejskal, K Stepka, L Tesarova, K Stejskal… - Cell cycle, 2015 - Taylor & Francis
The incorporation of histone H3 with an acetylated lysine 56 (H3K56ac) into the nucleosome
is important for chromatin remodeling and serves as a marker of new nucleosomes during …

Molecular pathways: the complexity of the epigenome in cancer and recent clinical advances

M Conte, L Altucci - Clinical Cancer Research, 2012 - AACR
Human cancer is causally linked to genomic and epigenomic deregulations. Epigenetic
abnormalities occurring within signaling pathways regulating proliferation, migration, growth …