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.Product Details of 54-47-7 The following contents are mentioned in the article:
CBS encodes a pyridoxal 5鈥?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: 54-47-7Product Details of 54-47-7).
(4-Formyl-5-hydroxy-6-methylpyridin-3-yl)methyl dihydrogen phosphate (cas: 54-47-7) belongs to pyridine derivatives. Pyridine has a conjugated system of six 蟺 electrons that are delocalized over the ring. The molecule is planar and, thus, follows the H眉ckel criteria for aromatic systems. One of the examples of pyridines is the well-known alkaloid lithoprimidine, which is an A3 adenosine receptor antagonist and N,N-dimethylaminopyridine (DMAP) analog, commonly used in organic synthesis.Product Details of 54-47-7