Skip to main content

Table 2 Competitive inhibition of Gal-3 binding to ASF by glycopolymers 2439 determined by ELISA

From: Biocompatible glyconanomaterials based on HPMA-copolymer for specific targeting of galectin-3

Compound Mn (g/mol)a Ð a Sugar motif n b IC50/glycan (μM) IC50 (μM) r cp rp/nd
Lactose 342.3 n.a. Galβ1, 4Glc 1 n.a. 137 ± 26 1 1
LacNAc 383.4 n.a. Galβ1, 4GlcNAc 1 n.a. 53 ± 16 1 1
LacdiNAc e 424.4 n.a. GalNAcβ1, 4GlcNAc 1 n.a. 64 ± 20 1 1
24 25,200 1.08 LacdiNAc-OEt-triazole 6.6 (4.4%) 62.9 ± 9.6 9.5 ± 1.5 7 1.0
25 27,300 1.10 LacdiNAc-OEt-triazole 11.9 (8.2%) 66.5 ± 14.9 5.6 ± 1.2 11 1.0
26 34,270 1.18 LacdiNAc-OEt-triazole 20.3 (12.5%) 66 ± 17 3.25 ± 0.85 20 1.0
27 34,000 1.20 LacdiNAc-OEt-triazole 23.9 (16.3%) 94 ± 19 3.92 ± 0.81 16 0.7
28 38,600 1.15 LacdiNAc-OEt-triazole 37.2 (29.0%) 126 ± 22 3.39 ± 0.60 19 0.5
29 21,700 1.10 LacdiNAc-N-triazole 3.7 (2.7%) 32.7 ± 7.9 8.6 ± 2.1 8 2.0
30 24,100 1.10 LacdiNAc-N-triazole 10.6 (8.1%) 27.5 ± 4.6 2.59 ± 0.44 25 2.3
31 30,800 1.12 LacdiNAc-N-triazole 18.2 (12.0%) 62 ± 20 3.4 ± 1.1 19 1.0
32 38,900 1.39 LacdiNAc-N-triazole 36.1 (24.8%) 128 ± 17 3.53 ± 0.46 18 0.5
33 31,500 1.07 LacdiNAc-OEt-DBCO 9.6 (5.7%) 54.2 ± 5.9 5.65 ± 0.69 11 1.2
34 28,600 1.06 LacdiNAc-N-DBCO 5.2 (3.0%) 84 ± 19 16.2 ± 3.7 4 0.8
35 28,300 1.18 LacdiNAc-N-triazole-Ph 5.6 (3.2%) 31.5 ± 0.85 5.62 ± 0.15 11 2.0
36 51,700 1.18 LacdiNAc-N-triazole-Ph 34.7 (15.7%) 139 ± 54 4.0 ± 1.5 16 0.5
37 43,400 1.24 LacdiNAc-OEt-triazole-Ph 29.9 (17.2%) 101 ± 20 3.37 ± 0.66 19 0.6
38 48,600 1.30 (LacdiNAc-OEt-triazole)2Ph 28.0 (12.3%) 98 ± 20 3.5 ± 0.72 18 0.6
39 46,100 1.10 (LacdiNAc-N-triazole)2Ph 29.8 (14.0%) 76.8 ± 16.9 2.58 ± 0.57 25 0.8
  1. n.a. not applicable, Et, ethyl; Ph, phenyl
  2. aMolecular weight (Mn) and dispersity (Ð) of polymers were determined using GPC with MALS and RI detection. Glycopolymers 28 and 32 were analyzed using Superose 12 column and 0.3 M sodium acetate buffer, pH 6.5 as the mobile phase; otherwise TSKgel Super SW3000 column and methanol/0.3 M sodium acetate buffer, pH 6.5 (4/1, v/v) as the mobile phase was employed. For monovalent standards, we give Mw (g/mol)
  3. bAverage number of glycans per polymer chain (glycan content, mol. %); n = 1, monovalent standard
  4. cRelative potency, i.e. IC50 (monovalent standard)/IC50 (multivalent glycopolymer)
  5. dRelative potency per one glycan
  6. eSynthesis of LacdiNAc standard (Scheme 1) is described in the Experimental section