Small molecule inhibition of mettl3
WebMay 14, 2024 · Working with STORM therapeutics, researchers developed and characterised a drug (STM2457) that inhibits part of the METTL3 protein, stopping it from carrying out its function in AML cells, which will now enter the clinic for trials in 2024. This research provides proof that METTL3 inhibitors show promise in treating AML. 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
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WebOct 10, 2024 · m6A RNA methyltransferases METTL3/14 regulate immune responses to anti‐PD‐1 therapy - PMC Back to Top Skip to main content An official website of the United States government Here's how you know The .gov means it’s official. Federal government websites often end in .gov or .mil. WebPublications Caflisch Group since 2010 . since 2010 - 2004-2009 - 1992-2003. 2024
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. 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
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. WebApr 4, 2024 · Abstract. METTL3 is the RNA methyltransferase predominantly responsible for the addition of N-6-methyladenosine (m6A), the most abundant modification to mRNA. The prevalence of m6A and the activity and expression of METTL3 have been linked to the appearance and progression of acute myeloid leukemia (AML)1. EPICS has discovered …
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 ...
http://www.bioc.uzh.ch/en/research/research-groups/caflisch/publications.html can of can\\u0027tWebNotably, our latest study of the first-in-class METTL3 inhibitor (Yankova et al, Nature, 2024) provides strong proof-of-concept that RNA-modifying enzymes represent a new avenue for anti-cancer therapeutics. flaghouse speakersWebOct 20, 2024 · Yankova E, Blackaby W, Albertella M, Rak J, De Braekeleer E, Tsagkogeorga G, et al. Small-molecule inhibition of METTL3 as a strategy against myeloid leukaemia. Nature. 2024;593:597–601. can of can\u0027tWeb1 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 … can of campbell\\u0027s tomato soupWebMar 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 … flag house spring city paWebDec 1, 2024 · Small molecule inhibitors from 2 distinct chemical series were identified and optimised using a structure-guided medicinal chemistry platform. Compounds 1 and 2 are … flag house sportsWebMar 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 … can of caramel tesco