Histone deacetylases and their inhibitors in cancer, neurological diseases and immune disorders
KJ Falkenberg, RW Johnstone - Nature reviews Drug discovery, 2014 - nature.com
Epigenetic aberrations, which are recognized as key drivers of several human diseases, are
often caused by genetic defects that result in functional deregulation of epigenetic proteins …
often caused by genetic defects that result in functional deregulation of epigenetic proteins …
Metabolic reprogramming and epigenetic modifications on the path to cancer
L Sun, H Zhang, P Gao - Protein & cell, 2022 - academic.oup.com
Metabolic rewiring and epigenetic remodeling, which are closely linked and reciprocally
regulate each other, are among the well-known cancer hallmarks. Recent evidence …
regulate each other, are among the well-known cancer hallmarks. Recent evidence …
Targeting transcription factors for cancer treatment
M Lambert, S Jambon, S Depauw… - Molecules, 2018 - mdpi.com
Transcription factors are involved in a large number of human diseases such as cancers for
which they account for about 20% of all oncogenes identified so far. For long time, with the …
which they account for about 20% of all oncogenes identified so far. For long time, with the …
Potent inhibition of DOT1L as treatment of MLL-fusion leukemia
SR Daigle, EJ Olhava, CA Therkelsen… - Blood, The Journal …, 2013 - ashpublications.org
Rearrangements of the MLL gene define a genetically distinct subset of acute leukemias
with poor prognosis. Current treatment options are of limited effectiveness; thus, there is a …
with poor prognosis. Current treatment options are of limited effectiveness; thus, there is a …
The PRMT5 arginine methyltransferase: many roles in development, cancer and beyond
N Stopa, JE Krebs, D Shechter - Cellular and molecular life sciences, 2015 - Springer
Post-translational arginine methylation is responsible for regulation of many biological
processes. The protein arginine methyltransferase 5 (PRMT5, also known as Hsl7, Jbp1 …
processes. The protein arginine methyltransferase 5 (PRMT5, also known as Hsl7, Jbp1 …
Targeting histone methyltransferases and demethylases in clinical trials for cancer therapy
L Morera, M Lübbert, M Jung - Clinical epigenetics, 2016 - Springer
The term epigenetics is defined as heritable changes in gene expression that are not due to
alterations of the DNA sequence. In the last years, it has become more and more evident …
alterations of the DNA sequence. In the last years, it has become more and more evident …
Metabolism, biochemical actions, and chemical synthesis of anticancer nucleosides, nucleotides, and base analogs
Nucleoside, nucleotide, and base analogs have been in the clinic for decades to treat both
viral pathogens and neoplasms. More than 20% of patients on anticancer chemotherapy …
viral pathogens and neoplasms. More than 20% of patients on anticancer chemotherapy …
Chromatin proteins and modifications as drug targets
K Helin, D Dhanak - Nature, 2013 - nature.com
A plethora of groundbreaking studies have demonstrated the importance of chromatin-
associated proteins and post-translational modifications of histones, proteins and DNA (so …
associated proteins and post-translational modifications of histones, proteins and DNA (so …
An orally bioavailable chemical probe of the lysine methyltransferases EZH2 and EZH1
EZH2 or EZH1 is the catalytic subunit of the polycomb repressive complex 2 that catalyzes
methylation of histone H3 lysine 27 (H3K27). The trimethylation of H3K27 (H3K27me3) is a …
methylation of histone H3 lysine 27 (H3K27). The trimethylation of H3K27 (H3K27me3) is a …
Mechanism of cross-talk between H2B ubiquitination and H3 methylation by Dot1L
Methylation of histone H3 K79 by Dot1L is a hallmark of actively transcribed genes that
depends on monoubiquitination of H2B K120 (H2B-Ub) and is an example of histone …
depends on monoubiquitination of H2B K120 (H2B-Ub) and is an example of histone …