Selectivity and Cooperativity of PROTAC®s using HT-SPR

Introduction

The unique heterobifunctional nature of PROTACs necessitates expanding the toolbox of characterization techniques to enable efficient drug discovery. Multiple warhead and linker combinations must be tested against the target protein(s) and ligases. Highlighted here is a strategy to characterize both binary and ternary kinetics for PROTACs against a panel of targets in parallel. Utilizing HT-SPR, a comprehensive assessment of both detailed binding selectivity and cooperativity can be obtained quickly using very small quantities of reagents.

Posted by Rebecca L. Rich, PhD

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