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WEBINAR
This webinar was presented in June 2023. Please enjoy the recording and contact us if you have any questions.

Part 1: One-stop degrader in vitro profiling

Targeting proteins for degradation therapeutically, as an alternative to inhibiting them, holds great promise for treating diseases in which pathogenic proteins are considered "undruggable" due to a lack of active sites for conventional small molecules. To discover such compounds, there are several challenges that need to be addressed to successfully facilitate and expedite TPD drug discovery. We’ll explore these challenges in more detail, as well as take a look at TPD platforms and how they can be effective solutions for resolving key issues.

Part 2: Chemistry synthesis service for PROTACs drug discovery

PROTACs (PROteolysis TArgeting Chimeras) have emerged as a new and promising modality in medicinal discovery, and research into their potential is currently a very active area. A PROTAC is a heterobifunctional molecule that consists of a protein-of-interest (POI) ligand and an E3 ubiquitin ligase (E3) recruiting ligand, connected by a linker. Learn more about the synthesizing of PROTAC molecules, the latest tools and strategies for making this work more efficient, and how this can lead to faster drug discovery.

  

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Learn about our Speakers
Yanchun Guo, Ph.D.
Associate Director, Dept. of Discovery Biology
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-Sundia 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.
Xingao Peng, Ph.D.
Senior Director, Dept. of Medicinal Chemistry
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-Sundia in 2015, where he focused on medicinal chemistry, particularly with a strong emphasis on the chemistry synthesis of PROTACs for drug discovery.
What is PROTAC in the context of Drug Discovery?

The Nobel Prize in Chemistry 2004 was awarded jointly to three Scientists "for the discovery of ubiquitin-mediated protein degradation".

Arvinas, the pioneer company using PROTACs in drug development, advanced the first PROTACs-based drugs (ARV-110) into an initial clinical trial in 2019.

PROTACs (PROteolysis TArgeting Chimeras) have brought great hopes for making “undruggable targets” druggable in the potential new therapeutic strategy. PROTACs are referred to the synthetic heterobifunctional molecules, which contain a ligand for the target protein, a linker that recruits an E3 ubiquitin ligase for ubiquitination-mediated and proteasome-dependent protein degradation.

How does BioDuro-Sundia contribute to the field of PROTAC?

We have worked on PROTAC molecules since 2015, having collaborated extensively with MNC, Biotech/Biopharma, startups and academic institutions around the world.

We have synthesized and scaled-up (to grams quantity) 1000+ PROTAC molecules, with deep expertise in PROTAC chemistry, including linkers and E3 ligase binder design and synthesis. We have also established a comprehensive biology evaluation platform for mechanistic studies of PROTAC/TPD with more than 30 assays to investigate all cellular events associated with PROTAC/TPD. We have strong expertise in building de novo HiBiT cell lines (> 40 HiBiT and NanoLuc cell lines built internally).

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