Benjamin Schwartz

TL;DR: The data indicate that adaptation to anchorage independence requires a fundamental change in citrate metabolism, initiated by IDH1-dependent reductive carboxylation and culminating in suppression of mitochondrial ROS.

TL;DR: The discovery of inhibitors that fill this void with an unprecedented metal-binding group, trifluoromethyloxadiazole (TFMO), which circumvents the selectivity and pharmacologic liabilities of hydroxamates is reported.

TL;DR: GSK2830371 is the first orally active, allosteric inhibitor of Wip1 phosphatase, an oncogenic phosphat enzyme common to multiple cancers and results in expected pharmacodynamic effects and causes inhibition of lymphoma xenograft growth.

TL;DR: Crystallographic and biochemical results demonstrated that compounds of this chemical series bind to an allosteric site and lock the enzyme in a catalytically inactive conformation, thereby enabling inhibition of different clinically relevant IDH1 mutants.

TL;DR: The design and characterization of an engineered human SIRT1 construct containing the minimal structural elements required for lysine deacetylation and catalytic activation by small molecule sirtuin-activating compounds (STACs) are reported and the STAC-binding site within the N-terminal domain of hSIRT1 is revealed.