Fueling Target Protein Degradation Drug Discovery: In Vitro Evaluation and Synthesis Strategies

Target protein degradation (TPD) has emerged as an innovative “event-driven” therapeutic approach, overcoming the limitations of traditional small-molecule drugs by enabling the targeting of “undruggable” proteins with high potency and selectivity.

It offers a significant advantage by targeting these proteins at low doses, thus bringing new hope for clinical treatment. Molecular glues and proteolysis-targeting chimeras (PROTACs) have emerged as rapidly evolving molecules in the TPD field; however, their complex mechanisms introduce significant hurdles in preclinical drug discovery.

The synthesis of TPD molecules, particularly PROTACs, is highly complex due to their large molecular weight and intricate structures. This demands advanced synthetic strategies and the availability of a comprehensive E3 ligand library to achieve precise molecular assembly. Moreover, the in vitro evaluation of degraders relies on robust high-throughput screening methods and the capability to comprehensively profile compounds to ensure accurate assessment of their pharmacological effects. A novel approach leverages these capabilities to drive TPD drug discovery.

Register for this webinar today to explore insights into TPD drug discovery and solutions for these challenges.

Speakers

Yanchun Guo, PhD, Associate Director of Discovery, BioDuro

Dr. Yanchun Guo received her PhD from Ulm University in Germany and completed her postdoctoral training at the City of Hope National Medical Center in the US. With extensive experience in gene editing and cancer biology, Dr. Yanchun Guo joined BioDuro in 2019 and established an in vitro evaluation platform for PROTAC drug discovery from scratch. The TPD platform, led by Dr. Guo, has received high recognition from many clients, including Pfizer.

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Xingao Peng, PhD, Senior Director of Medicinal Chemistry, BioDuro

Dr. Xingao Peng received his PhD from the Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences in 2008, and then completed postdoctoral training at Colorado State University in the US and Nanyang Technological University in Singapore. With extensive experience in synthetic chemistry, Dr. Peng joined BioDuro in 2015, where he focused on medicinal chemistry, particularly with a strong emphasis on the chemistry synthesis of PROTACs for drug discovery.

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