Indian Institute of Science Education and Research, Dr Homi Bhabha Road, Pune-411008, India.
Chem Commun (Camb). 2021 Apr 11;57(28):3516-3519. doi: 10.1039/d1cc00964h. Epub 2021 Mar 11.
We report the discovery of a potential heparan sulfate (HS) ligand to target several growth factors using 13 unique HS tetrasaccharide ligands. By employing an HS microarray and SPR, we deciphered the crucial structure-binding relationship of these glycans with the growth factors BMP2, VEGF, HB-EGF, and FGF2. Notably, GlcNHAc(6-O-SO)-IdoA(2-O-SO) (HT-2,6S-NAc) tetrasaccharide showed strong binding with the VEGF growth factor. In vitro vascular endothelial cell proliferation, migration and angiogenesis was inhibited in the presence of VEGF and HT-2,6S-NAc or HT-6S-NAc, revealing the potential therapeutic role of these synthetic HS ligands.
我们报告了一种使用 13 种独特的 HS 四糖配体来发现针对多种生长因子的潜在肝素硫酸盐 (HS) 配体的发现。通过使用 HS 微阵列和 SPR，我们解析了这些聚糖与生长因子 BMP2、VEGF、HB-EGF 和 FGF2 的关键结构结合关系。值得注意的是，GlcNHAc(6-O-SO)-IdoA(2-O-SO) (HT-2,6S-NAc)四糖与 VEGF 生长因子具有强烈的结合能力。在存在 VEGF 和 HT-2,6S-NAc 或 HT-6S-NAc 的情况下，体外血管内皮细胞增殖、迁移和血管生成受到抑制，这揭示了这些合成 HS 配体的潜在治疗作用。
