Table 1. Competitive Binding Assay of Lectin-Targeted Ciprofloxacin Conjugates and Control Compounds with LecA, LecBPAO1, and LecBPA14a.
LecA | |||
---|---|---|---|
compound | n | m | IC50 ± s.d. [μM] |
11 | 1 | LecA-probes | 31.7 ± 11 |
12 | 2 | 30.9 ± 8.7 | |
13 | 3 | 31.1 ± 8.3 | |
14 | 4 | 29.9 ± 9.5 | |
22 | 1 | 0 | 30.4 ± 8.0 |
23 | 1 | 1 | 21.6 ± 5.5 |
24 | 2 | 0 | 32.2 ± 3.3 |
25 | 2 | 1 | 28.0 ± 1.8 |
26 | 3 | 0 | 27.3 ± 4.0 |
27 | 3 | 1 | 29.3 ± 3.7 |
28 | 4 | 0 | 28.3 ± 8.1 |
29 | 4 | 1 | 26.2 ± 2.4 |
Me-α-d-Gal | controls | 71.7 ± 16 | |
pNP-β-d-Gal | 52.7 ± 13 |
LecBPAO1 | LecBPA14 | ||
---|---|---|---|
compound | m | IC50 ± s.d. [μM] | IC50 ± s.d. [μM] |
19 | LecB-probe | 3.91 ± 1.6 | 1.87 ± 0.21 |
30 | 0 | 2.37 ± 1.2 | 2.24 ± 0.23 |
31 | 1 | 2.53 ± 0.87 | 1.00 ± 0.06 |
Me-α-d-Man | controls | 166 ± 22 | 101 ± 10 |
l-Fuc | 2.63 ± 1.7 | 2.46 ± 0.33 | |
Me-α-l-Fuc | 0.534 ± 0.07 | 0.79 ± 0.11 |
Means and standard deviations were determined from a minimum of three independent experiments. Ki calculated from IC50 is shown in Table S1.