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 …
SAM/SAH analogs as versatile tools for SAM-dependent methyltransferases
J Zhang, YG Zheng - ACS chemical biology, 2016 - ACS Publications
S-Adenosyl-L-methionine (SAM) is a sulfonium molecule with a structural hybrid of
methionine and adenosine. As the second largest cofactor in the human body, its major …
methionine and adenosine. As the second largest cofactor in the human body, its major …
Targeting histone lysine methylation in cancer
J McGrath, P Trojer - Pharmacology & therapeutics, 2015 - Elsevier
Within the vast landscape of histone modifications lysine methylation has gained increasing
attention because of its profound regulatory potential. The methylation of lysine residues on …
attention because of its profound regulatory potential. The methylation of lysine residues on …
Targeting histone methylation for cancer therapy: enzymes, inhibitors, biological activity and perspectives
Post-translational methylation of histone lysine or arginine residues plays important roles in
gene regulation and other physiological processes. Aberrant histone methylation caused by …
gene regulation and other physiological processes. Aberrant histone methylation caused by …
Structure, function and inhibition of critical protein–protein interactions involving mixed lineage leukemia 1 and its fusion oncoproteins
Abstract Mixed lineage leukemia 1 (MLL1, also known as MLL or KMT2A) is an important
transcription factor and histone-H3 lysine-4 (H3K4) methyltransferase. It is a master …
transcription factor and histone-H3 lysine-4 (H3K4) methyltransferase. It is a master …
[HTML][HTML] Targeting DOT1L and HOX gene expression in MLL-rearranged leukemia and beyond
CW Chen, SA Armstrong - Experimental hematology, 2015 - Elsevier
Highlights•The histone methyltransferase DOT1L is required for proliferation of mixed-
lineage leukemia gene (MLL)-rearranged leukemias.•DOT1L and H3K79 methylation …
lineage leukemia gene (MLL)-rearranged leukemias.•DOT1L and H3K79 methylation …
DNA methylation targeting: the DNMT/HMT crosstalk challenge
O Castillo-Aguilera, P Depreux, L Halby, PB Arimondo… - Biomolecules, 2017 - mdpi.com
Chromatin can adopt a decondensed state linked to gene transcription (euchromatin) and a
condensed state linked to transcriptional repression (heterochromatin). These states are …
condensed state linked to transcriptional repression (heterochromatin). These states are …
Pharmacological inhibition of LSD1 for the treatment of MLL-rearranged leukemia
Background Mixed lineage leukemia (MLL) gene translocations are found in~ 75% infant
and 10% adult acute leukemia, showing a poor prognosis. Lysine-specific demethylase 1 …
and 10% adult acute leukemia, showing a poor prognosis. Lysine-specific demethylase 1 …
A chemical probe toolbox for dissecting the cancer epigenome
J Shortt, CJ Ott, RW Johnstone, JE Bradner - Nature Reviews Cancer, 2017 - nature.com
Cancer cell hallmarks are underpinned by transcriptional programmes operating in the
context of a dynamic and complicit epigenomic environment. Somatic alterations of …
context of a dynamic and complicit epigenomic environment. Somatic alterations of …
3-(Piperidin-4-ylmethoxy) pyridine containing compounds are potent inhibitors of lysine specific demethylase 1
Methylation of histone lysine residues plays important roles in gene expression regulation
as well as cancer initiation. Lysine specific demethylase 1 (LSD1) is responsible for …
as well as cancer initiation. Lysine specific demethylase 1 (LSD1) is responsible for …