Publication Type
Publication Type
Peer Reviewed Journal
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Authors
Swanson, Michael D.; Boudreaux, Daniel M.; Salmon, Loic; Chugh, Jeetender; Winter, Harry C.; Meagher, Jennifer L.; Andre, Sabine; Murphy, Paul V.; Oscarson, Stefan; Roy, Rene; et al
Year
2015
Month
October
Journal
Cell
Title
Engineering a Therapeutic Lectin by Uncoupling Mitogenicity from Antiviral Activity
Status
Published
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Engineering a Therapeutic Lectin by Uncoupling Mitogenicity from Antiviral Activity
Volume
163
Issue
3
Start Page
746
End Page
758
Abstract
A key effector route of the Sugar Code involves lectins that exert crucial regulatory controls by targeting distinct cellular glycans. We demonstrate that a single amino-acid substitution in a banana lectin, replacing histidine 84 with a threonine, significantly reduces its mitogenicity, while preserving its broad-spectrum antiviral potency. X-ray crystallog., NMR spectroscopy, and glycocluster assays reveal that loss of mitogenicity is strongly correlated with loss of pi-pi stacking between arom. amino acids H84 and Y83, which removes a wall sepg. two carbohydrate binding sites, thus diminishing multivalent interactions. On the other hand, monovalent interactions and antiviral activity are preserved by retaining other wild-type conformational features and possibly through unique contacts involving the T84 side chain. Through such fine-tuning, target selection and downstream effects of a lectin can be modulated so as to knock down one activity, while preserving another, thus providing tools for therapeutics and for understanding the Sugar Code
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http://www.sciencedirect.com/science/article/pii/S0092867415012738
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