Drugging the Undruggable Using Advanced Fragment-Based Drug Discovery

Fragment screening is an excellent method to predict protein druggability. This presentation looks at advanced technologies available for the target-to-hit developmental stage of the drug discovery process. Successful solutions integrate multiple aspects, including target acquisition, hit identification, and comprehensive characterization of hit series, including a dissection of mechanism of action (MoA) by using state-of-the art structural biology approaches. With an ever-increasing number of challenging and often "first-in-the class" targets, we examine the value of unique workflows ranging from protein engineering to screenings (fragment and DNA encoded library screenings) and beyond to accelerate the drug discovery process.

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A Conversation with Richard Lerner: DELopen Promotes Worldwide Academic Research Using DNA-Encoded Libraries, Far More Than Just a Numbers Game

Richard Lerner is a visionary. He and Sydney Brenner, both of the Scripps Research Institute (Scripps) first published on DNA-encoded libraries (DELs) in 1992 in the Proceedings of the National Academy of Sciences. Yet it was only within the last few years has interest in DELs, a potentially disruptive technology, become “viral” in the life science industry. Twenty-six years later, in December 2018 DELopen was announced as an open-access platform supported by WuXi AppTec to better enable academics and non-profit organizations to utilize DEL technology in drug discovery.

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Infographic: Drugging the Undruggable: Leveraging the Right Screening Methods for Challenging Targets

Challenging targets, such as membrane proteins or protein-protein interactions were considered undruggable in the past. However, today a variety of screening methods can be used to help develop drugs against these formerly undruggable targets. Together with WuXi AppTec, we have created an infographic showing you exactly how it can be done.

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Unlocking the potential of DEL | Inspire Hit Discovery

March 4, 2020 - By going commercial, DNA Encoded Library (DEL) technology facilitates rapid discovery and provides access to more chemical entities at lower cost.

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