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Metabolism of 2022 FDA approved small molecule drugs PART 2

Metabolite Tales Blog

Metabolism of 2022 FDA approved small molecule drugs part 2 Mixing it Up By Julia Shanu-Wilson In Part 1 of this topic we looked at metabolism of the small molecule drugs approved by the FDA in 2022 that were mediated by CYP3A4. Oxidation of adagrasib occurs on the methylpyrrolidine group 4.

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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.

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AI in Drug Discovery 2023 - A Highly Opinionated Literature Review (Part I)

Practical Cheminformatics

In a brief section entitled “Predicting Protein-Small Molecule Complexes”, the authors mention their efforts to generate structures of bound non-covalent and covalent small molecule ligands. My only complaint about this paper is that there may have been too much information presented. from the deposited model.

Drugs 142
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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?