[HTML][HTML] A biocatalytic approach to a key intermediate for the synthesis of the COVID-19 experimental drug Molnupiravir
A Burke, W Birmingham, Y Zhuo, C BZd, R Crawshaw… - 2021 - europepmc.org
Herein we report the conversion of cytidine 2 to N-hydroxy-cytidine 7 catalysed by cytidine
deaminase (CD). The wild-type enzyme operates efficiently at high sustrate loadings and
hydroxylamine concentrations to favor N-hydroxy-cytidine formation over uridine. Although
the wild-type enzyme demonstrated good activity, we were able to further enhance the ratio
of N-hydroxy-cytidine to uridine produced through directed evolution of CD. In particular, a
T123G mutation close to the active site dramatically reduces cytidine hydrolysis activity …
deaminase (CD). The wild-type enzyme operates efficiently at high sustrate loadings and
hydroxylamine concentrations to favor N-hydroxy-cytidine formation over uridine. Although
the wild-type enzyme demonstrated good activity, we were able to further enhance the ratio
of N-hydroxy-cytidine to uridine produced through directed evolution of CD. In particular, a
T123G mutation close to the active site dramatically reduces cytidine hydrolysis activity …
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