Guy Vigers

TL;DR: It is demonstrated that ATP-competitive kinase inhibitors can have opposing functions as inhibitors or activators of signalling pathways, depending on the cellular context, which provides new insights into the therapeutic use of ATP- competitive RAF inhibitors.

TL;DR: Comprehensive pharmacodynamic and pharmacogenomic profiling in sensitive and partially resistant non-clinical models identified mechanisms implicated in limiting anti-tumor activity including KRAS nucleotide cycling and pathways that induce feedback reactivation and/or bypass KRAS dependence.

TL;DR: In this article, an invention related to inhibitors of p38, and methods for producing these inhibitors are described. And pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders mediated by p38 are provided.

TL;DR: The crystal structure shows that s-IL1R consists of three immunoglobulin-like domains which wrap around IL-1β in a manner distinct from the structures of previously described cytokine–receptor complexes.

TL;DR: A 2.7 Å resolution co-crystal structure of human AKT1 containing both the PH and kinase domains with a selective allosteric inhibitor bound in the interface is presented, providing a structural foundation for interpreting the effects of different classes of AKT inhibitors and designing selective ones.