In this webinar, Dr Fleur Ferguson discussed the large-scale chemical exploration of key variables for targeted protein degradation across the kinome that helped develop a global map of kinase degradability. This expansive dataset provided chemical leads for some 200 kinases and has led to insights into the relative degradability of the kinome, with the data made publicly available as an open-access chemical proteomics resource.

Targeted protein degradation (TPD) is an innovative chemical approach, whereby small molecules are used to induce ubiquitin-dependent degradation of proteins, and proteins are selectively targeted for degradation by the proteasome. TPD is of interest in drug development as it can address previously inaccessible targets, yet relatively little is understood about the factors governing a target’s propensity for ubiquitination and degradation. Dr Ferguson’s lab are working to tackle fundamental challenges in degrader design and discovery, using chemoproteomic approaches to annotate the degradable kinome.

Invited speaker:

• Dr Fleur Ferguson, William A. Lee Assistant Professor, University of California San Diego, USA

This session was chaired by Dr Elton Zeqiraj, Sir Henry Dale Fellow and University Academic Fellow, University of Leeds, UK.