Discovering Unique Ubiquitin E3 Ligase Ligands to Unlock Targeted Protein Degradation

Discovering Unique Ubiquitin E3 Ligase Ligands to Unlock Targeted Protein degradation

Gauthami Jalagadugula, Alexandra Russell¹⁺, Kenneth Wallace¹⁺, Janelle Pedroza and Abdul Haseeb^{1 *}

Introduction

PROteolytic TArgeting Chimeras (PROTACs) have emerged as new class of drugs to target “undruggable” proteome. The human genome encodes ~ 600 E3 ligases that differentially expressed across various tissues. Only a few E3 ligases have been utilized to date for PROTAC applications. We have developed technologies to expand the chemical space by identifying novel ligands for unexplored E3 ligases to design novel degraders that can be used for tissue specific therapeutics.

*Corresponding Author – Haseeb@Lifesensors.com