| DOI | Resolve DOI: https://doi.org/10.1039/c3ob40515j |
|---|
| Author | Search for: Garcia-Hartjes, J.; Search for: Bernardi, S.; Search for: Weijers, C.A.G.M.; Search for: Wennekes, T.; Search for: Gilbert, M.1; Search for: Sansone, F.; Search for: Casnati, A.; Search for: Zuilhof, H. |
|---|
| Affiliation | - National Research Council of Canada. NRC Institute for Biological Sciences
|
|---|
| Format | Text, Article |
|---|
| Subject | Binding domain; Calix[5]arene; Causative agents; Cholera toxin; Epithelial cells; Inhibition assays; Multivalency effects; Valencies; Positive ions; Chemistry |
|---|
| Abstract | Cholera toxin (CT), the causative agent of cholera, displays a pentavalent binding domain that targets the oligosaccharide of ganglioside GM1 (GM1os) on the periphery of human abdominal epithelial cells. Here, we report the first GM1os-based CT inhibitor that matches the valency of the CT binding domain (CTB). This pentavalent inhibitor contains five GM1os moieties linked to a calix[5]arene scaffold. When evaluated by an inhibition assay, it achieved a picomolar inhibition potency (IC50 = 450 pM) for CTB. This represents a significant multivalency effect, with a relative inhibitory potency of 100000 compared to a monovalent GM1os derivative, making GM1os-calix[5]arene one of the most potent known CTB inhibitors. This journal is © The Royal Society of Chemistry 2013. |
|---|
| Publication date | 2013 |
|---|
| In | |
|---|
| Language | English |
|---|
| Peer reviewed | Yes |
|---|
| NPARC number | 21269768 |
|---|
| Export citation | Export as RIS |
|---|
| Report a correction | Report a correction (opens in a new tab) |
|---|
| Record identifier | e27d4c2a-b951-4934-9b06-cd5bc8b51466 |
|---|
| Record created | 2013-12-13 |
|---|
| Record modified | 2020-04-22 |
|---|
