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Polyvalent transition-state analogues of sialyl substrates strongly inhibit bacterial sialidases.
preprintrevised on 20.10.2020, 07:28 and posted on 20.10.2020, 07:37 by coralie assailly, clarisse bridot, amélie saumonneau, paul lottin, Benoit Roubinet, Eva-Maria Krammer, francesca François, frederica vena, ludovic landemarre, Dimitri Alvarez-Dorta, david deniaud, cyrille grandjean, charles tellier, Sagrario Pascual, Véronique montembault, Laurent Fontaine, Franck Daligault, Julie Bouckaert, sebastien gouin
Conjugation of the transitionstate-cation analogue DANA to polymeric scaffolds led to highly potent inhibitors of bacterial sialidases. Each clustered DANA on the polymers saw its inhibitory potency for S. pneumoniae or B. thetaiotaomicron sialidases improved by more than four orders of magnitude. This extends the multivalent concept to this important class of enzymes.
Read the published paper
in Chemistry – A European Journal