Fleur M. Ferguson

TL;DR: An overview of the novel targets, biological processes and disease areas that kinase-targeting small molecules are being developed against, highlight the associated challenges and assess the strategies and technologies that are enabling efficient generation of highly optimized kinase inhibitors are provided.

TL;DR: Chemo-proteomics is used to annotate the degradable kinome and develop multitargeted degraders to answer fundamental questions about the ubiquitin proteasome system, uncovering that kinase degradation is p97 dependent.

TL;DR: QC-01–175 effected clearance of tau in frontotemporal dementia (FTD) patient-derived neuronal cell models, with minimal effect on tau from neurons of healthy controls, indicating specificity for disease-relevant forms.

TL;DR: An ethyl derivative of an existing small-molecule inhibitor, I-BET/JQ1, is developed and it is shown that it binds leucine/alanine mutant bromodomains with nanomolar affinity and achieves up to 540-fold selectivity relative to wild-type bromidomains.

TL;DR: In this paper, an exclusively selective VHL-recruiting degradation tag (dTAG) molecule was proposed to degrade FKBP12F36V-tagged proteins, which overcomes a limitation of previously reported CRBN-recruitting dTAG molecules to degrade recalcitrant oncogenes, supports combination degrader studies and facilitates investigations of protein function in cells and mice.