Table 3.
Inhibition and relative potencies of galectin-3 binding to ASF by soluble tetrasaccharides and neo-glycoproteins. Relative potencies are related to the corresponding tetrasaccharide and additionally to one binding site. Neo-glycoproteins show up to 15 times enhanced potencies per glycan compared to soluble tetrasaccharides.
| Compound | IC50 [µM] | Relative potency | Relative potency per glycan |
|---|---|---|---|
| 4 | 13.04 ± 3.43 | 1.0 ± 0.26 | 1.0 ± 0.26 |
| 11j | 0.85 ± 0.21 | 15.3 ± 3.14 | 2.0 ± 0.42 |
| 11k | 0.09 ± 0.02 | 145.2 ± 2.45 | 8.2 ± 0.14 |
| 11g | 0.04 ± 0.01 | 367.8 ± 5.12 | 15.2 ± 0.21 |
| 5 | 7.23 ± 0.87 | 1.0 ± 0.12 | 1.0 ± 0.12 |
| 12j | 1.10 ± 0.22 | 6.6 ± 1.42 | 0.9 ± 0.19 |
| 12k | 0.06 ± 0.02 | 127.1 ± 2.56 | 7.1 ± 0.15 |
| 12g | 0.04 ± 0.02 | 182.0 ± 4.06 | 7.5 ± 0.17 |