Jeremy Murray

TL;DR: In vivo evaluation of compound 1h showed significant antitumor activity in RT112 bladder cancer xenografts models overexpressing wild-type FGFR3 and support the potential therapeutic use of 1h as a new anticancer agent.

TL;DR: Engineering compounds that inhibit USP7 activity by attenuating ubiquitin binding suggests opportunities for developing other deubiquitinase inhibitors and may be a strategy more broadly applicable to inhibiting proteins that require ubiquit in binding for full functional activity.

TL;DR: Chemical optimization of arylomycins results in an inhibitor of bacterial type I signal peptidase that shows activity both against multidrug-resistant clinical isolates of Gram-negative bacteria in vitro and in several in vivo infection models.

TL;DR: The discovery of 2 (GDC-0980), a class I PI3K and mTOR kinase inhibitor for oncology indications, has demonstrated significant efficacy in mouse xenografts when dosed as low as 1 mg/kg orally and is currently in phase I clinical trials for cancer.

TL;DR: It is shown that human TEADs are palmitoylated at a universally conserved cysteine, and it is demonstrated that this modification is required for proper TEAD folding and stability, indicating a potential new avenue for pharmacologically regulating the Hippo pathway through the modulation of TEADPalmitoylation.