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Polymers of a Transition-State Sialyl Cation Strongly Inhibit Bacterial Sialidases.

preprint
submitted on 28.09.2020 and posted on 29.09.2020 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.

Funding

17-CE07-028-01

History

Email Address of Submitting Author

sebastien.gouin@univ-nantes.fr

Institution

Laboratory CEISAM, UMR6230

Country

France

ORCID For Submitting Author

0000-0002-0985-1165

Declaration of Conflict of Interest

NA

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