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Small-Molecule Targeting of Oncogenic FTO Demethylase in Acute Myeloid Leukemia
FTO, an mRNA N6-methyladenosine (m6A) demethylase, was reported to promote leukemogenesis. Using structure-based rational design, we have developed two promising FTO inhibitors, namely FB23 and FB23-2, which directly bind to FTO and selectively inhibit ...
Yue Huang, Rui Su, Lei Dong
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Here we show that FTO as an N6-methyladenosine (m6A) RNA demethylase is degraded by selective autophagy, which is impaired by low-level arsenic exposure to promote tumorigenesis. We found that in arsenic-associated human skin lesions, FTO is upregulated,
Yan-Hong Cui, Seungwon Yang, Jiangbo Wei
exaly +2 more sources
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Orthogonal Demethylase-Activated Deoxyribozyme for Intracellular Imaging and Gene Regulation
Journal of the American Chemical Society, 2021The epigenetic modification of nucleic acids represents a versatile approach for achieving high-efficient control over gene expression and transcription and could dramatically expand their biosensing and therapeutic applications.
Qing Wang, Xiaoqing Liu, Xiaocheng Weng
exaly +2 more sources
Autophagy is essential for cellular survival and energy homeostasis under nutrient deprivation. Despite the emerging importance of nuclear events in autophagy regulation, epigenetic control of autophagy gene transcription remains unclear. Here, we report
Young-Chae Kim, Yang Zhang, Peter M Yau
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RNA N6-methyladenosine demethylase FTO promotes breast tumor progression through inhibiting BNIP3
N6-methyladenosine (m6A) modification is the most pervasive modification in mRNA, and has been considered as a new layer of epigenetic regulation on mRNA processing, stability and translation.
Honglei Chen, Yuan Wang, Bo Wei
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Global warming has profound effects on plant growth and fitness. Plants have evolved sophisticated epigenetic machinery to respond quickly to heat, and exhibit transgenerational memory of the heat-induced release of post-transcriptional gene silencing ...
Qun Li, Muyang Wang, Yiwen Deng
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N6-methyladenosine (m6A) is the most abundant base modification found in messenger RNAs (mRNAs). The discovery of FTO as the first m6A mRNA demethylase established the concept of reversible RNA modification. Here, we present a comprehensive transcriptome-
Marek Bartosovic +2 more
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When Is a Demethylase Not a Demethylase?
Science, 2011The histone lysine demethylase JARID1a has demethylase-independent function in the circadian clock.
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Inhibitors of histone demethylases
Bioorganic & Medicinal Chemistry, 2011Methylated lysines are important epigenetic marks. The enzymes involved in demethylation have recently been discovered and found to be involved in cancer development and progression. Despite the relative recent discovery of these enzymes a number of inhibitors have already appeared.
Lohse, Brian +6 more
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