Natalie Page

TL;DR: The identification, optimization and detailed characterization of highly potent, selective USP7 inhibitors together with their less active, enantiomeric counterparts are described and co-crystal structures of a human DUB enzyme complexed with small-molecule inhibitors are disclosed, revealing a previously undisclosed allosteric binding site.

TL;DR: Potent, novel, and selective inhibitors of USP7 have been developed using both rational and structure-guided design enabled by high-resolution cocrystallography, and initial efforts aimed at developing compounds suitable for in vivo experiments are described.

TL;DR: A comparative study of the tissue specific promoter prostate specific membrane antigen (PSMA), and the tumour‐type specific hOC promoter driving the inducible nitric oxide synthase (iNOS) transgene using both in vitro and in vivo models is presented.

TL;DR: ALM-201 is a novel, targeted microtubule binding agent which exhibits potent anti-angiogenic activity in vitro and in vivo and is well tolerated with no signs of toxicity observed in mouse xenograft models up to 80 days of dosing.

TL;DR: Alm301 as discussed by the authors is a novel, allosteric, sub-type selective inhibitor of AKT1/2, which was shown to be highly selective against a panel of over 450 kinases and potently inhibited cellular proliferation.