Hijacking E3 Ligases to Mediate Degradation & Modulation of Undrugged Targets

As a family of over 600 known proteins, ligases pose immense potential as viable avenues for harnessing previously undrugged targets. Key challenges remain however to rapidly discover and identify novel and underexploited ubiquitin E3s. Furthermore, bottlenecks exist in the development of the established ligases; Cereblon and VHL.

It is now critical that we harness Cryo-EM, X-Ray crystallography, and other visualization tools to fully understand the structure and function of these lesser-known E3s, accelerate ligand screening with new and improved tools, leverage advances in DMPK knowledge to address concerns over toxicity in Cereblon, propel VHL from ‘academic’ to clinic, and all in, de-risk the translation of candidate ligases to the clinic.

The 3rd Ligase Targeting Drug Development Summit is returning with fresh understanding and data from the forerunners of the field and those who have recently joined the space. Together we will investigate ligase structural and functional biology, screening tools for optimal ligase, linker, and ligand identification, explore tissue specificity, uncover the key modalities where ligases can succeed, and showcase the novel assays that are maximizing validation to ensure success in the clinic.

This dedicated forum will provide an unrivaled meeting point for industry leaders all under one specialized forum to strategically accelerate and de-risk the process of identifying, validating, and therapeutically leveraging cell and tissue-specific ubiquitin E3 ligases for degradation or modulation of targets in oncology, immunology, and beyond.

To know more: https://ter.li/gapgsb