Paper Picks
Take a look at our favourite publications around biotransformation and metabolism of drugs in Hypha’s “Paper Picks”.
Hypha's Paper Picks
An understanding of the metabolism of PROTACs is a growing need since their metabolism can’t be readily predicted from the individual ligands that constitute the chimera. A paper by Goracci et al. looks at the metabolic stability of a collection of PROTACs in cryopreserved human hepatocytes, and vs CYP3A4 and aldehyde oxidase. The linker appears to be the most labile moiety, with any instability localized at the attachment points. Depending on the type of linker, O- and N-dealkylations were observed.
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Hypha Discovery is a UK-based CRO supporting pharmaceutical and agrochemical companies worldwide through the production of metabolites and new derivatives of drugs and agrochemicals in discovery and development.