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Screening of heteroaromatic scaffolds against cystathionine beta-synthase enables identification of substituted pyrazolo[3,4-c]pyridines as potent and selective orthosteric inhibitors

Fantel, Anna-Maria ; Myrianthopoulos, Vassilios ; Georgoulis, Anastasios ; Lougiakis, Nikolaos ; Zantza, Iliana ; Lamprinidis, George ; Augsburger, Fiona ; Marakos, Panagiotis ; Vorgias, Constantinos E. ; Szabo, Csaba ; Pouli, Nicole ; Papapetropoulos, Andreas ; Mikros, Emmanuel

In: Molecules, 2020, vol. 25, no. 16, p. 3739

Cystathionine β-synthase (CBS) is a key enzyme in the production of the signaling molecule hydrogen sulfide, deregulation of which is known to contribute to a range of serious pathological states. Involvement of hydrogen sulfide in pathways of paramount importance for cellular homeostasis renders CBS a promising drug target. An in-house focused library of heteroaromatic compounds was...