Inhibitors of protein methyltransferases and demethylases
Post-translational modifications of histones by protein methyltransferases (PMTs) and
histone demethylases (KDMs) play an important role in the regulation of gene expression …
histone demethylases (KDMs) play an important role in the regulation of gene expression …
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 …
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 …
Nucleosome turnover regulates histone methylation patterns over the genome
Recent studies have indicated that nucleosome turnover is rapid, occurring several times
per cell cycle. To access the effect of nucleosome turnover on the epigenetic landscape, we …
per cell cycle. To access the effect of nucleosome turnover on the epigenetic landscape, we …
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 …
[HTML][HTML] The histone methyltransferase DOT1L: regulatory functions and a cancer therapy target
M Wong, P Polly, T Liu - American journal of cancer research, 2015 - ncbi.nlm.nih.gov
DOT1L is a unique histone methyltransferase that targets the histone H3 lysine 79 (H3K79)
residue for mono-, di-and tri-methylation. Histone H3K79 mono-and di-methylation results in …
residue for mono-, di-and tri-methylation. Histone H3K79 mono-and di-methylation results in …
Mixed-lineage leukemia fusions and chromatin in leukemia
AV Krivtsov, T Hoshii… - Cold Spring …, 2017 - perspectivesinmedicine.cshlp.org
Recent studies have shown the importance of chromatin-modifying complexes in the
maintenance of developmental gene expression and human disease. The mixed lineage …
maintenance of developmental gene expression and human disease. The mixed lineage …
Systematic Design of Adenosine Analogs as Inhibitors of a Clostridioides difficile-Specific DNA Adenine Methyltransferase Required for Normal Sporulation and …
Antivirulence agents targeting endospore-transmitted Clostridioides difficile infections are
urgently needed. C. difficile-specific DNA adenine methyltransferase (CamA) is required for …
urgently needed. C. difficile-specific DNA adenine methyltransferase (CamA) is required for …
Inhibitors of emerging epigenetic targets for cancer therapy: a patent review (2010–2014)
M Tanaka, JM Roberts, J Qi… - Pharmaceutical patent …, 2015 - Taylor & Francis
Gene regulatory pathways comprise an emerging and active area of chemical probe
discovery and investigational drug development. Emerging insights from cancer genome …
discovery and investigational drug development. Emerging insights from cancer genome …
New small molecule inhibitors of histone methyl transferase DOT1L with a nitrile as a non-traditional replacement for heavy halogen atoms
A number of new nucleoside derivatives are disclosed as inhibitors of DOT1L activity. SARs
established that DOT1L inhibition could be achieved through incorporation of polar groups …
established that DOT1L inhibition could be achieved through incorporation of polar groups …