Hypha’s Q2 2024 Newsletter – Focus on N-glucuronidation
N-glucuronides may emerge as disproportionate metabolites due to interspecies variability and higher rates of N-glucuronidation in humans. This is particularly relevant for some aromatic N-heterocycles metabolised by UGT1A4 and UGT2B10.
In this newsletter we look at two major N-glucuronides formed by UGT1A4 that were needed for further studies. Microbial biotransformation was used to access the N-glucuronide of camonsertib, and a switch from human liver S9 to late-stage chemical synthesis enabled gram amounts of the N-glucuronide of LEO compound 1 to be made.
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