Lin, Hong published the artcileDiscovery of Potent and Selective Covalent Protein Arginine Methyltransferase 5 (PRMT5) Inhibitors, Quality Control of 22483-09-6, the main research area is covalent inhibitor PRMT5 hemiaminals cocrystal structure.
Protein arginine methyltransferase 5 (PRMT5) is known to sym. dimethylate numerous cytosolic and nuclear proteins that are involved in a variety of cellular processes. Recent findings have revealed its potential as a cancer therapeutic target. PRMT5 possesses a cysteine (C449) in the active site, unique to PRMT5. Therefore, covalent PRMT5 inhibition is an attractive chem. approach. Herein, we report an exciting discovery of a series of novel hemiaminals that under physiol. conditions can be converted to aldehydes and react with C449 to form covalent adducts, which presumably undergo an unprecedented elimination to form the thiol-vinyl ethers, as indicated by electron d. in the co-crystal structure of the PRMT5/MEP50 complex.
ACS Medicinal Chemistry Letters published new progress about Antitumor agents. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Quality Control of 22483-09-6.
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