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 WebMay 26, 2024 · Fig. 1: METTL3 inhibition is a promising therapy against AML. a, The position of small molecules or ligands within the SAM-binding pocket of human METTL3. Surface …
Small-molecule inhibition of METTL3 as a strategy against ... - Nature
Web1 Small molecule inhibition of METTL3 as a strategy against myeloid 2 . leukaemia. 3 . 4 Eliza Yankova. 1,2,3 *, Wesley Blackaby. 3, Mark Albertella. 3, Justyna Rak. 2,4 ... 60 anti-leukaemic strategy, we developed the small molecule STM2457. A high throughput screen 61 (HTS) of 250,000diverse drug like compounds was carried out. STM1760 ... 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 … dropsa 1655308
RCSB PDB - 6TTP: Crystal structure of the human METTL3 …
WebSep 23, 2024 · Remarkably, a small-molecule inhibitor of ALKBH5 enhanced the efficacy of cancer immunotherapy (Li et al, 2024). The complex and varied roles of m 6 A in tumors suggest that much needs to be done to further understand the importance and dynamic of this modification in cancer biology and its clinical application. Besides, apart from total ... WebFeb 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 ... WebOct 22, 2024 · STORM has used state-of-the-art drug discovery capabilities, combined with unique analytical technologies specifically developed to target RNA epigenetics, to generate highly potent selective and orally bioavailable, small molecule inhibitors of METTL3 and other RNA modifying enzymes. dropropizina xarope preço