Synthesis of chitooligomer-based glycoconjugates and their binding to the rat natural killer cell activation receptor NKR-P1.

摘要: NKR-P1 protein is an important activating receptor at the surface of rat natural killer cells. GlcNAc and chitooligomers were identified as strong activation ligands in vitro vivo. Their clustering brings about increase their affinity to by 3–6 orders. Here we describe novel methodology for preparation neoglycoproteins based on BSA carying (n = 2–5). Further developed coupling glycosylamines via aromatic-SCN activated linker both or synthetic cores. Inhibition studies chitooligomer glycoconjugates with show that our are very high binding (−log IC50 13–15). In analogy previous observations clustered PAMAM backbones clusters should provide considerably better vivo antitumor treatment.