Small molecule inhibition of mettl3
WebMar 30, 2024 · The m 6 A methyltransferase METTL3 has been linked to the initiation and maintenance of acute myeloid leukaemia (AML), but the potential of therapeutic applications targeting this enzyme remains unknown 5-7 ... Macromolecules Find similar proteins by: (by identity cutoff) 3D Structure Find similar proteins by: (by identity cutoff) 3D Structure http://www.bioc.uzh.ch/en/research/research-groups/caflisch/publications.html
Small molecule inhibition of mettl3
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WebHere we present pre-clinical data showing that STC-15, an orally bioavailable small molecule inhibitor of METTL3, restrains cancer growth and induces anti-cancer immunity. Materials & Methods. To characterise transcriptomic changes following METTL3 inhibition, RNA sequencing studies were performed on several cancer cell lines treated with STC-15. WebJan 24, 2024 · Overall, these studies show that METTL3 activity is required for cellular homeostasis maintenance, and while impairing its functions may be necessary in some conditions (such as certain cancer types), its inhibition may be potentially harmful to organism health. m 6 A and Viral Infections
WebApr 8, 2024 · The strategy that can be employed is to use inhibitors or activators of METTL3, METTL14, YTHDF2, ALKBH5, and FTO to control SARS-CoV-2 replication by modulating the m6A methylome. In this context, selective inhibition of METTL3 catalytic activity using STM2457 inhibits HCoV-OC43 and SARS-CoV-2 infection (Burgess et al., 2024). Since … WebNow, a selective small molecule inhibitor of METTL3 shows significant anti-leukemic effects in preclinical AML models, highlighting the promise of pharmacological METTL3 inhibition as a new cancer therapy. Publication types Research Support, N.I.H., Extramural MeSH terms Animals
WebNov 13, 2024 · Cellular target engagement was confirmed by demonstrating that compounds 1 and 2 reduced m 6 A levels and inhibited the protein expression of METTL3 … WebApr 26, 2024 · The paper demonstrates that METTL3 small molecule inhibition is effective as a new therapeutic strategy against AML, prolonging survival in a variety of AML …
WebApr 1, 2024 · The discovery of small-molecule inhibitors of METTL3 is of considerable and far-reaching importance, yet there have been relatively few small-molecule inhibitors of METTL3 detected and the small-molecule inhibitors discussed in this study have only recently been discovered. More small molecules targeting METTL3 are expected to be …
WebMar 11, 2024 · The RNA methylase METTL3 catalyzes the transfer of a methyl group from the cofactor S-adenosyl-L-methionine (SAM) to the N 6 atom of adenine. We have … paw patrol films for kidsWeb1 day ago · Silencing of METTL3-14 complexes reduced IRES activity upon inhibitor exposure and sensitized resistant GBM lines. ... Recently, we have also described the identification of a small molecule inhibitor of hnRNP A1 which blocks cyclin D1 and c-myc IRES activity and synergizes with mTOR inhibitors to achieve strong anti-GBM activities … paw patrol film stream deutschWebFeb 14, 2024 · In an effort to explore a specific inhibitor of METTL3, a virtual screening of ZINC and DrugBank 4.0 databases identified 4 compounds (18–21; Fig. 4D) with piperidine or piperazine rings, and they functioned as METTL3/14-WTAP activators to facilitate RNA methylation, which increased the mRNA m6A levels to shift the cell cycle to G 0 and G 1 ... screenshot in chromebookWebMETTL3 inhibition is a promising therapy against acute myelogenous leukemia (AML). (a)The position of small molecule or ligands within the SAM-binding pocket of human … screenshot in chrome extensionpaw patrol film streamingWebSep 25, 2024 · 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 (UZH1a) with potency in a biochemical assay of 280 nM, while its enantiomer UZH1b is 100 times less active. The crystal structure of the complex of … screenshot in chrome browserWebThe paper entitled ‘Small molecule inhibition of METTL3 as a strategy against myeloid leukaemia’ reveals findings that further establish and validate STORM’s ground-breaking … screenshot in chuwi laptop