Development of Cell-Active N6-Methyladenosine RNA Demethylase FTO Inhibitor
B Chen, F Ye, L Yu, G Jia, X Huang… - Journal of the …, 2012 - ACS Publications
The direct nucleic acid repair dioxygenase FTO is an enzyme that demethylates N 6-
methyladenosine (m6A) residues in mRNA in vitro and inside cells. FTO is the first RNA …
methyladenosine (m6A) residues in mRNA in vitro and inside cells. FTO is the first RNA …
Structural insights into FTO's catalytic mechanism for the demethylation of multiple RNA substrates
FTO demethylates internal N 6-methyladenosine (m6A) and N 6, 2′-O-dimethyladenosine
(m6Am; at the cap+ 1 position) in mRNA, m6A and m6Am in snRNA, and N 1 …
(m6Am; at the cap+ 1 position) in mRNA, m6A and m6Am in snRNA, and N 1 …
A strategy based on nucleotide specificity leads to a subfamily-selective and cell-active inhibitor of N 6-methyladenosine demethylase FTO
The AlkB family of nucleic acid demethylases are of intense biological and medical interest
because of their roles in nucleic acid repair and epigenetic modification. However their …
because of their roles in nucleic acid repair and epigenetic modification. However their …
Targeting the RNA demethylase FTO for cancer therapy
LL Zhou, H Xu, Y Huang, CG Yang - RSC chemical biology, 2021 - pubs.rsc.org
N 6-Methyladenosine (m6A) is the most prevalent internal modification on mRNA and
represents a new layer of gene expression in eukaryotes. The field of m6A-encoded …
represents a new layer of gene expression in eukaryotes. The field of m6A-encoded …
Identification of Flavin Mononucleotide as a Cell‐Active Artificial N6‐Methyladenosine RNA Demethylase
LJ Xie, XT Yang, RL Wang, HP Cheng… - Angewandte …, 2019 - Wiley Online Library
Abstract N6‐Methyladenosine (m6A) represents a common and highly dynamic modification
in eukaryotic RNA that affects various cellular pathways. Natural dioxygenases such as FTO …
in eukaryotic RNA that affects various cellular pathways. Natural dioxygenases such as FTO …
Rational design of RNA demethylase FTO inhibitors with enhanced antileukemia drug-like properties
P Xiao, Z Duan, Z Liu, L Chen, D Zhang… - Journal of Medicinal …, 2023 - ACS Publications
The fat mass and obesity-associated protein (FTO) is an RNA N 6-methyladenosine (m6A)
demethylase highly expressed in diverse cancers including acute myeloid leukemia (AML) …
demethylase highly expressed in diverse cancers including acute myeloid leukemia (AML) …
Small-molecule targeting of oncogenic FTO demethylase in acute myeloid leukemia
FTO, an mRNA N 6-methyladenosine (m 6 A) demethylase, was reported to promote
leukemogenesis. Using structure-based rational design, we have developed two promising …
leukemogenesis. Using structure-based rational design, we have developed two promising …
Differential m6A, m6Am, and m1A demethylation mediated by FTO in the cell nucleus and cytoplasm
FTO, the first RNA demethylase discovered, mediates the demethylation of internal N 6-
methyladenosine (m 6 A) and N 6, 2-O-dimethyladenosine (m 6 A m) at the+ 1 position from …
methyladenosine (m 6 A) and N 6, 2-O-dimethyladenosine (m 6 A m) at the+ 1 position from …
Meclofenamic acid selectively inhibits FTO demethylation of m6A over ALKBH5
Y Huang, J Yan, Q Li, J Li, S Gong, H Zhou… - Nucleic acids …, 2015 - academic.oup.com
Two human demethylases, the fat mass and obesity-associated (FTO) enzyme and ALKBH5,
oxidatively demethylate abundant N 6-methyladenosine (m6A) residues in mRNA …
oxidatively demethylate abundant N 6-methyladenosine (m6A) residues in mRNA …
N6-Methyladenosine in nuclear RNA is a major substrate of the obesity-associated FTO
We report here that fat mass and obesity-associated protein (FTO) has efficient oxidative
demethylation activity targeting the abundant N 6-methyladenosine (m6A) residues in RNA …
demethylation activity targeting the abundant N 6-methyladenosine (m6A) residues in RNA …