TY - JOUR 
A1 - Rinaldi, Francesca
AU - Fernández Lucas, Jesús
AU - Fuente, Diego de la
AU - Zheng, Changping
AU - Bavaro, Teodora
AU - Peters, Benjamin
AU - Massolini, Gabriella
AU - Annunziata, Francesca
AU - Conti, Paola
AU - Calleri, Enrica
AU - Et al.
T1 - Immobilized enzyme reactors based on nucleoside phosphorylases and 2′-deoxyribosyltransferase for the in-flow synthesis of pharmaceutically relevant nucleoside analogues
Y1 - 2020
SN - 0960-8524

UR - http://hdl.handle.net/11268/10936
AB - In this work, a mono- and a bi-enzymatic analytical immobilized enzyme reactors (IMERs) were developed as prototypes for biosynthetic purposes and their performances in the in-flow synthesis of nucleoside analogues of pharmaceutical interest were evaluated. Two biocatalytic routes based on nucleoside 2′-deoxyribosyltransferase from Lactobacillus reuteri (LrNDT) and uridine phosphorylase from Clostridium perfrigens (CpUP)/purine nucleoside phosphorylase from Aeromonas hydrophila (AhPNP) were investigated in the synthesis of 2′-deoxy, 2′,3′-dideoxy and arabinonucleoside derivatives. LrNDT-IMER catalyzed the synthesis of 5-fluoro-2′-deoxyuridine and 5-iodo-2′-deoxyuridine in 65–59% conversion yield, while CpUP/AhPNP-IMER provided the best results for the preparation of arabinosyladenine (60% conversion yield).

Both IMERs proved to be promising alternatives to chemical routes for the synthesis of nucleoside analogues. The developed in-flow system represents a powerful tool for the fast production on analytical scale of nucleosides for preliminary biological tests.
KW - Reactores biológicos
KW - Nucleósidos
KW - Biología molecular
LA - eng
ER -