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WuXi AppTec´s HitS/Crelux has acquired the state-of-the art device Dianthus (NanoTemper Technologies GmbH), which enables the quantification of molecular interaction by measuring Temperature Related Intensity Change (TRIC). The measurements take place free in solution and in a microplate format. Because only a very brief laser-induced temperature change is applied, we can measure 384 data points within 30 min and up to 19 000 per day. This enables us to run and analyze the carefully tendered HitS Fragment Library of 3100 fragments or your own library at an unprecedented speed. The hits can then be confirmed using various biophysical methods including X-ray crystallography. For example, a recently established crystallization system for the peptidase C30 enables either direct structural hit confirmation or an opportunity for crystallographic fragment screening. These peptidases are related to serine endopeptidases of family S1 and are involved in viral polyprotein processing during replication.
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.Read More
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.Read More
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.Read More
March 4, 2020 - By going commercial, DNA Encoded Library (DEL) technology facilitates rapid discovery and provides access to more chemical entities at lower cost.Read More