Cheng Fang

TL;DR: It is shown that the targeted inhibitor AG-221 suppresses the mutant IDH2 enzyme in multiple preclinical models and induces differentiation of malignant blasts, supporting its clinical development.

TL;DR: AG-120 (ivosidenib), an inhibitor of the IDH1 mutant enzyme that exhibits profound 2-HG lowering in tumor models and the ability to effect differentiation of primary patient AML samples ex vivo is reported.

TL;DR: Induction of serine auxotrophy by PKM2 activation was accompanied by reduced carbon flow into the serine biosynthetic pathway and increased expression of high affinity serine transporters, supporting the hypothesis that PKM1 expression confers metabolic flexibility to cancer cells that allows adaptation to nutrient stress.

TL;DR: The first full-length crystal structure of GAC in the presence and absence of BPTES molecules is reported, which appears to lock the GAC tetramer into a nonproductive conformation.

TL;DR: In this article, the authors reported the discovery of PKM2 activators with a unique allosteric binding mode, which resulted in a metabolic rewiring of cancer cells manifested by a profound dependency on the amino acid serine for continued cell proliferation.