METTL3 from target validation to the first small-molecule inhibitors: a medicinal chemistry journey

F Fiorentino, M Menna, D Rotili… - Journal of Medicinal …, 2023 - ACS Publications
RNA methylation is a critical mechanism for regulating the transcription and translation of
specific sequences or for eliminating unnecessary sequences during RNA maturation …

Mining for METTL3 inhibitors to suppress cancer

J Li, RI Gregory - Nature structural & molecular biology, 2021 - nature.com
The RNA methyltransferase METTL3 catalyzes N 6-methyladenosine (m6A) modification of
messenger RNAs (mRNAs). It is overexpressed in many types of cancer, including acute …

Discovery of METTL3 small molecule inhibitors by virtual screening of natural products

Y Du, Y Yuan, L Xu, F Zhao, W Wang, Y Xu… - Frontiers in …, 2022 - frontiersin.org
N6-Methyladenosine (m6A) is the most prevalent mRNA modification in mammalian cells
that is mainly catalyzed by the methyltransferase complex of methyltransferase-like 3 and …

METTL3 inhibitors for epitranscriptomic modulation of cellular processes

EV Moroz‐Omori, D Huang, R Kumar Bedi… - …, 2021 - Wiley Online Library
The methylase METTL3 is the writer enzyme of the N6‐methyladenosine (m6A) modification
of RNA. Using a structure‐based drug discovery approach, we identified a METTL3 inhibitor …

Small‐molecule inhibitors of METTL3, the major human epitranscriptomic writer

RK Bedi, D Huang, SA Eberle, L Wiedmer… - …, 2020 - Wiley Online Library
The RNA methylase METTL3 catalyzes the transfer of a methyl group from the cofactor S‐
adenosyl‐L‐methionine (SAM) to the N6 atom of adenine. We have screened a library of …

[HTML][HTML] METTL3 plays multiple functions in biological processes

S Liu, L Zhuo, J Wang, Q Zhang, Q Li, G Li… - American journal of …, 2020 - ncbi.nlm.nih.gov
Abstract N 6-methyladenosine (m 6 A) is the most common internal modification of mRNAs
in higher eukaryotic. This process is performed by methyltransferase. Methyltransferase-like …

A mass spectrometric assay of METTL3/METTL14 methyltransferase activity

SM Buker, ZA Gurard-Levin… - … the Science of Drug …, 2020 - journals.sagepub.com
A variety of covalent modifications of RNA have been identified and demonstrated to affect
RNA processing, stability, and translation. Methylation of adenosine at the N6 position (m6A) …

Roles of METTL3 in cancer: mechanisms and therapeutic targeting

C Zeng, W Huang, Y Li, H Weng - Journal of hematology & oncology, 2020 - Springer
Abstract N 6-methyladenosine (m 6 A) is the most abundant mRNA modification and is
catalyzed by the methyltransferase complex, in which methyltransferase-like 3 (METTL3) is …

METTL6 is a tRNA m3C methyltransferase that regulates pluripotency and tumor cell growth

VV Ignatova, S Kaiser, JSY Ho, X Bing, P Stolz… - Science …, 2020 - science.org
Recently, covalent modifications of RNA, such as methylation, have emerged as key
regulators of all aspects of RNA biology and have been implicated in numerous diseases …

Roles and drug development of METTL3 (methyltransferase-like 3) in anti-tumor therapy

P Xu, R Ge - European journal of medicinal chemistry, 2022 - Elsevier
Methyltransferase complex, such as METTL3/METTL14/WTP, catalyze N 6-methyladenosine
(m 6 A), which is the most abundant mRNA modification in mammals. Besides acting as am …