Cytosine-based tet enzyme inhibitors
WebSep 5, 2024 · Ten-eleven translocation protein 1 (TET1) is one member of TET proteins family which plays a key role in dynamic DNA methylation-demethylation process. … WebBobcat339 is a novel cytosine-based TET enzyme inhibitor with IC50 of 33 uM (TET1) and 73 uM (TET2). Bobcat339 has mid-μM inhibitor activity against TET1 and TET2, but does not inhibit the DNA methyltransferase, DNMT3a. These new molecular tools will be useful to the field of epigenetics and serve as a starting point for new therapeutics that …
Cytosine-based tet enzyme inhibitors
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WebJan 31, 2024 · Cytosine-Based TET Enzyme Inhibitors. Gabriella N L Chua Department of Chemistry and Biochemistry, Bates College, 2 Andrews Road, Lewiston, Maine 04240, … WebThese probes are based on the broad-spectrum cysteine protease inhibitor E-64 and bind covalently to the active sites of the enzymes. Therefore, with these probes, one can …
WebFeb 21, 2024 · Additionally, the virtual ligand screening of natural products further identified compound 35 (termed C35), a catechol-containing small molecule, as a novel TET … WebMost known inhibitors of TET are α-ketoglutarate mimics that may interfere with other α-ketoglutarate dependent enzymes. Recently, a novel cytosine-based inhibitor of TET, Bobcat339, was reported to have mid-μM inhibitory activity against TET1 and TET2. The molecule is now sold as a TET inhibitor by several vendors.
WebMechanism-based inhibition of C5-cytosine DNA methyltransferases by 2-H pyrimidinone WebAbout. I am a biochemist/molecular biologist with 13 years of experience specializing in the activity, inhibition, and detection of the APOBEC3 …
WebJan 8, 2024 · Little is known about TET protein function due to a lack of pharmacological tools to manipulate DNA hydroxymethylation levels. In this study, we examined the role …
WebBobcat339 is a novel cytosine-based TET enzyme inhibitor (IC50s: 33/73 uM for TET1/2), but not DNMT3a, does not inhibit the DNA methyltransferase DNMT3a. All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use. Bobcat339, CAS 2280037-51-4 grace church yonkersWebNational Center for Biotechnology Information grace church yateWebNotably, we found that Bobcat339, belonging to a new class of cytosine-based TET enzyme inhibitor, was able to inhibit reversibly the hydroxylation activity of these enzymes . This inhibition has permitted as evidence the role of de-methylation of genomic DNA in IL-1β-induced tumor progression and bone metastasis in MCF-7 non-metastatic breast ... gracechu wisliveWebJan 31, 2024 · We identify a promising cytosine-based lead compound, Bobcat339, that has mid-μM inhibitor activity against TET1 and TET2, but does not inhibit the DNA … grace church youtubeWebOct 4, 2024 · All told, seven Bates students broadly contributed to research leading to the creation of Bobcat339; for their contributions, the seven … chill camping wagonWebJan 8, 2024 · The ten-eleven translocation (TET) enzyme family catalyzes the hydroxymethylation and subsequent demethylation of DNA by oxidizing 5-methylcytosine (5mC) to 5-hydroxymethylcytosine (5hmC). Little is known about TET protein function due to a lack of pharmacological tools to manipulate DNA hydroxymethylation levels. chill calloutsWebAug 1, 2024 · Cytosine-based TET enzyme inhibitors. ACS Med. Chem. Lett. (2024) View more references. Cited by (22) Genetics of osteoarthritis. 2024, Osteoarthritis and Cartilage. Show abstract. Osteoarthritis genetics has been transformed in the past decade through the application of large-scale genome-wide association scans. So far, over 100 … gracechu wislive-th