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N6-methyladenosine demethylase FTO promotes M1 and M2 macrophage activation.

Cellular Signalling, 2020
Macrophage polarization is the driving force of various inflammatory diseases, especially those involved in M1/M2 imbalance. N6-methyladenosine (m6A) is the most prevalent internal mRNA modification in eukaryotes that affects multiple biological ...
Xiaofei Gu   +5 more
semanticscholar   +1 more source

Fungal Lanosterol 14α-demethylase: A target for next-generation antifungal design.

Biochimica et Biophysica Acta - Proteins and Proteomics, 2020
The cytochrome P450 enzyme lanosterol 14α-demethylase (LDM) is the target of the azole antifungals used widely in medicine and agriculture as prophylaxis or treatments of infections or diseases caused by fungal pathogens.
B. Monk   +5 more
semanticscholar   +1 more source

The m6A demethylase FTO promotes the growth of lung cancer cells by regulating the m6A level of USP7 mRNA.

Biochemical and Biophysical Research Communications - BBRC, 2019
Lung cancer is one of the leading causes of cancer-related death in developed countries. Despite decades of intensive efforts to comate this malignant disease, the prognosis of lung cancer remains unfavorable and is especially poor in advanced non-small ...
Jie Li   +7 more
semanticscholar   +1 more source

JmjC Lysine Demethylases

2015
Among the most fundamental questions in the regulation of gene expression in mammals is how epigenetic methylation patterns of histone lysine residues are established, recognized and erased. This chapter reviews recent studies on, and discusses the resulting biochemical and structural insights into, the Jumonji C (JmjC)-containing lysine demethylases ...
Xiaodong Cheng, Raymond C. Trievel
openaire   +1 more source

In Vitro Histone Demethylase Assays

2022
Dynamic histone methylation regulates gene activation and repression. It is involved in proliferation, differentiation, lineage specification, and development. Histone demethylase assays are invaluable in studying histone demethylation substrate recognition, kinetics, regulation, and inhibition by small molecules, many of which are potential ...
openaire   +2 more sources

Lysine demethylases and cancer

Pathology - Research and Practice
Epigenetic mechanisms are of pivotal importance in the normal development and maintenance of cell and tissue-specific gene expression patterns, and are fundamental to the genesis of cancer. One significant category of epigenetic modifications is histone methylation.
Tomas, Eckschlager   +2 more
openaire   +2 more sources

Opiate target site N-demethylase enzymes: Differences from the liver N-demethylase

Biochemical and Biophysical Research Communications, 1979
Abstract Mixtures of morphine-63H and morphine-N-14CH3 were incubated with rat brain subcellular fractions. Isotope ratio measurements served as the marker for identification, purification and quantitation of N-nor products which were shown to consist almost solely of N-normorphine.
E F, Hahn, B I, Norton, J, Fishman
openaire   +2 more sources

Recent Progress in Histone Demethylase Inhibitors

Journal of Medicinal Chemistry, 2016
There is increasing interest in targeting histone N-methyl-lysine demethylases (KDMs) with small molecules both for the generation of probes for target exploration and for therapeutic purposes. Here we update on previous reviews on the inhibition of the lysine-specific demethylases (LSDs or KDM1s) and JmjC families of N-methyl-lysine demethylases (JmjC
McAllister   +6 more
openaire   +2 more sources

In Vitro Histone Demethylase Assays

2009
Histone methylation plays important roles in chromatin structure, transcription, and epigenetic state of the cell. Tremendous discoveries recently demonstrated that methylation mark is not static but is dynamically regulated by both histone methyltransferases and the histone demethylases.
Kenji, Kokura, Jia, Fang
openaire   +2 more sources

Histone Demethylases

Histone methylation is a dynamic process that contributes to the control of gene expression by influencing chromatin structure. Since their initial discovery 20 years ago, histone demethylases have been shown to play a critical role in histone methylation and thus developmental, physiological, and pathological processes.
Stephen C. Kales, Anton Simeonov
openaire   +1 more source

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