Small molecule inhibition of mettl3
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. 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.
Small molecule inhibition of mettl3
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WebApr 26, 2024 · These data suggest that small-molecule inhibition of METTL3 is detrimental for the maintenance of AML, but has no significant or lasting impact on normal haematopoiesis. In this Article we have... WebMETTL3 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 …
WebMay 1, 2024 · Now, a selective small molecule inhibitor of METTL3 shows significant antileukemic effects in preclinical AML models, highlighting the promise of pharmacological METTL3 inhibition as a new cancer ... WebApr 13, 2024 · In CRC cells, METTL3 is an oncogene that stabilizes HK2 as well as GLUT1 expression via IGF2BP2- or IGF2BP2/3-related mechanisms and activates the subsequent aerobic glycolysis pathway to boost colorectal cancer progression [ 79 ]. Additionally, in CRC cells, KIAA1429 increases HK2 levels to boost— aerobic glycolysis rate [ 80 ].
WebMar 26, 2024 · METTL3-14-WTAP Binding Affinity and Kinetics of Small-Molecule Ligands The interaction between the small-molecule ligands and METTL3-14-WTAP complex was studied using the enzyme-catalyzed RNA methylation and the SPR using a Biacore T100 (GE Healthcare Life Sciences) instrument (cf. STAR Methods ). WebApr 13, 2024 · The first selective small-molecule inhibitors of METTT3 to be identified were adenine derivatives, which exhibited high ligand-binding efficiency, shedding light on the …
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 ...
WebThe paper entitled ‘Small molecule inhibition of METTL3 as a strategy against myeloid leukaemia’ reveals findings that further establish and validate STORM’s ground-breaking … how many banana fish volumes are thereWebMay 5, 2024 · National Center for Biotechnology Information high plains geneticsWebMar 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 how many banana trees per hectareWebMar 11, 2024 · We have screened a library of 4000 analogues and derivatives of the adenosine moiety of SAM by high-throughput docking into METTL3. Two series of adenine derivatives were identified in silico, and the binding mode of six of the predicted inhibitors was validated by protein crystallography. Two compounds, one for each series, show … high plains food kiowa coWebMar 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 … high plains genetics piedmont sd for saleWebApr 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 … high plains family medicine borger txWebApr 26, 2024 · To investigate the therapeutic potential of targeting the enzymatic activity of METTL3 as an anti-leukaemic strategy, we developed the small molecule STM2457. A … how many bananas a day should a diabetic eat