Identification of 8-Hydroxyquinoline Derivatives That Decrease Cystathionine Beta Synthase (CBS) Activity was written by Conan, Pierre;Leon, Alice;Gourdel, Mathilde;Rollet, Claire;Chair, Loubna;Caroff, Noeline;Le Goux, Nelig;Le Jossic-Corcos, Catherine;Sinane, Maha;Gentile, Lucile;Maillebouis, Louise;Loaec, Nadege;Martin, Jennifer;Vilaire, Marie;Corcos, Laurent;Mignen, Olivier;Croyal, Mikael;Voisset, Cecile;Bihel, Frederic;Friocourt, Gaelle. And the article was included in International Journal of Molecular Sciences in 2022.Electric Literature of C8H10NO6P The following contents are mentioned in the article:
CBS encodes a pyridoxal 5-phosphate-dependent enzyme that catalyzes the condensation of homocysteine and serine to form cystathionine. Due to its implication in some cancers and in the cognitive pathophysiol. of Down syndrome, the identification of pharmacol. inhibitors of this enzyme is urgently required. However, thus far, attempts to identify such mols. have only led to the identification of compounds with low potency and limited selectivity. We consequently developed an original, yeast-based screening method that identified three FDA-approved drugs of the 8-hydroxyquinoline family: clioquinol, chloroxine and nitroxoline. These mols. reduce CBS enzymic activity in different cellular models, proving that the mol. mechanisms involved in yeast phenotypic rescue are conserved in mammalian cells. A combination of genetic and chem. biol. approaches also revealed the importance of copper and zinc intracellular levels in the regulation of CBS enzymic activity-copper promoting CBS activity and zinc inhibiting its activity. Taken together, these results indicate that our effective screening approach identified three new potent CBS inhibitors and provides new findings for the regulation of CBS activity, which is crucial to develop new therapies for CBS-related human disorders. This study involved multiple reactions and reactants, such as (4-Formyl-5-hydroxy-6-methylpyridin-3-yl)methyl dihydrogen phosphate (cas: 54-47-7Electric Literature of C8H10NO6P).
(4-Formyl-5-hydroxy-6-methylpyridin-3-yl)methyl dihydrogen phosphate (cas: 54-47-7) belongs to pyridine derivatives. Pyridines are an important class of heterocycles and occur in polysubstituted forms in many naturally occurring biologically active compounds, drug molecules and chiral ligands. Pyridine, its benzo and pyridine-based compounds play diverse roles in organic chemistry. Pyridine-based materials are valued for their optical and physical properties as well as their medical potential. Electric Literature of C8H10NO6P