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PROTACs and Molecular Glues: High-Throughput Quantitative Assays for Rationale Design

PROTACs and Molecular Glues: High-Throughput Quantitative Assays for Rationale Design

Authors: Janelle Pedroza1, Kenneth Wallace1, Derrick Padykula, Alexandra Russell1, and Karteek Kadimisetty*1

Introduction

PROTACs have emerged as new class of drugs that can target the “undruggable” proteome by hijacking the ubiquitin proteasome system. Traditional methods like western blotting and reporter gene assays are prone to artifacts. New methods that can monitor PROTAC function on endogenous targets at physiological expression levels are essential to accelerate the PROTAC discovery process. Current study highlights use of TUBE technology to rationally design molecular glue and PROTAC mediated ubiquitination and degradation of targets.

*Corresponding Author – Kadimisetty@Lifesensors.com

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