Paper Picks
Take a look at our favourite publications around biotransformation and metabolism of drugs in Hypha’s “Paper Picks”.
Hypha's Paper Picks
MetID guided target design is the topic of our paper pick for February 2023, published by Li and colleagues at Merck.
Major O-demethylated human metabolites of ivermectin that reduce Anopheles survival were made by Hypha’s microbial biotransformation system, and are the focus feature of our Q3 2023 newsletter.
Metabolites of the FDA approved anti-fungal drug rezafungin were made by Hypha’s microbial biotransformation system.
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.