Institute of Molecular Pharmacy, Pharmacenter, University of Basel, Klingelbergstr. 50, 4056 Basel, Switzerland.
Carbohydr Res. 2010 Jul 2;345(10):1348-59. doi: 10.1016/j.carres.2010.03.010. Epub 2010 Mar 16.
Paraplegia is caused by injuries of the central nervous system (CNS) and especially young people suffer from these severe consequences as, for example, the loss of motor functions. The lack of repair of the injured nerve strands originates from the inhibitory environment for axon regeneration in the CNS. Specific inhibitory proteins block the regrowth of nerve roots. One of these neurite outgrowth inhibitors is the myelin-associated glycoprotein (MAG), which is a member of the Siglec family (sialic acid-binding immunoglobulin-like lectin). In previous studies, we identified potent small molecule MAG antagonists. In this communication, we report new neuraminic acid derivatives modified in the 4- and 5-position, and the influence of various structural modifications on their kinetic and thermodynamic binding properties.
截瘫是由中枢神经系统 (CNS) 的损伤引起的，尤其是年轻人，他们会遭受严重的后果，例如运动功能的丧失。受损神经束无法修复的原因是中枢神经系统中轴突再生的抑制环境。特定的抑制蛋白会阻止神经根的再生。其中一种神经突生长抑制剂是髓鞘相关糖蛋白 (MAG)，它是 Siglec 家族（唾液酸结合免疫球蛋白样凝集素）的成员。在之前的研究中，我们鉴定了有效的小分子 MAG 拮抗剂。在本通讯中，我们报告了在 4 位和 5 位进行修饰的新的神经氨酸衍生物，以及各种结构修饰对其动力学和热力学结合特性的影响。
