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Game-changing pan-TEAD inhibitor for solid tumours

Drug Target Review

The current version of Chemistry42 uses over 40 generative models, including generative autoencoders and generative adversarial networks as well as both structure-based and ligand-based drug design to generate and optimise de novo small molecules. The novel molecules were further ranked based on their ADME and selectivity profiles.

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N-glucuronidation: the human element

Metabolite Tales Blog

N -glucuronidation: the human element By Julia Shanu-Wilson In our last blog of the year, we look at why N -glucuronidation of drugs is important in human drug metabolism. Glucuronidation is the most common phase II reaction observed in the metabolism of drugs in humans. Xenobiotica, 41:8, 652-669; [link]. [3] Tukey, Ryoichi Fujiwara.

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Obstacles and innovations of macrocyclic drug development

Drug Target Review

Traditionally, drug discovery has focused on small-molecule therapeutics, typically with a molecular weight of less than 500 Daltons. 2 Typically, small-molecule drugs target active sites buried inside proteins. What are macrocycles and why are they interesting for drug discovery?