1-(sulfonyl)-5-(arylsulfonyl) indoline as activators of the tumor cell specific M2 isoform of pyruvate kinase

…, E Ben-Zeev, N Schutz, O Bohana-Kashtan…

Index: Yacovan, Avihai; Ozeri, Rachel; Kehat, Tzofit; Mirilashvili, Sima; Sherman, Daniel; Aizikovich, Alex; Shitrit, Alina; Ben-Zeev, Efrat; Schutz, Nili; Bohana-Kashtan, Osnat; Konson, Alexander; Behar, Vered; Becker, Oren M. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 20 p. 6460 - 6468

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Citation Number: 15

Abstract

Cancer cells preferentially use glycolysis rather than oxidative phosphorylation for their rapid growth. They consume large amount of glucose to produce lactate even when oxygen is abundant, a phenomenon known as the Warburg effect. This metabolic change originates from a shift in the expression of alternative spliced isoforms of the glycolytic enzyme pyruvate kinase (PK), from PKM1 to PKM2. While PKM1 is constitutively active, PKM2 is ...