Sergio Mantegani

TL;DR: The interaction between β‐catenin and Tcf family members is crucial for the Wnt signal transduction pathway, which is commonly mutated in cancer, and inhibiting such interactions using low molecular weight inhibitors is a challenge.

TL;DR: Potent and selective Aurora kinase inhibitors were identified from the combinatorial expansion of the 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole bi-cycle, a novel and versatile scaffold designed to target the ATP pocket of protein kinases.

TL;DR: In this article, the synthesis and inhibitory activity of ergolinyl-acylureas is described and some structure-activity relationship relationship considerations are also reported, and a new class of ergoline-8β-carboxamide is described.

TL;DR: The efficacy profile of NMS-E973 suggests a potential for development in different clinical settings, including tumors that have become resistant to molecular targeted agents, particularly in cases of tumors which reside beyond the BBB.

TL;DR: The identification of compound 18 (NMS-E973), which displayed significant efficacy in a human ovarian A2780 xenograft tumor model, with a mechanism of action confirmed in vivo by typical modulation of known Hsp90 client proteins, and with a favorable pharmacokinetic and safety profile.