Pieters Roland J
Department of Medicinal Chemistry and Chemical Biology, Utrecht Institute for Pharmaceutical Sciences, Utrecht University, NL-3508 TB Utrecht, The Netherlands.
Med Res Rev. 2007 Nov;27(6):796-816. doi: 10.1002/med.20089.
Bacterial adhesion is often a prelude to infection. In many cases, this process is governed by protein-carbohydrate interactions. Intervention at this early stage of infection is a conceptually highly attractive alternative to conventional antibiotics that are increasingly prone to resistance. The lack of high-affinity inhibitors of adhesion has proven to be a hurdle for further exploitation of this concept; however, new developments indicate a positive change. Structure-based design at the monovalent level and also evaluation of glycodendrimers and glycopolymers have yielded structures of high affinity. In addition to the development of inhibitors, topics of this review include available structural information of adhesion proteins, carbohydrate specificities of the various pathogens and their adhesion proteins. Other new developments aimed at affecting bacterial adhesion and the use of the adhesins for bacterial detection are also discussed.
细菌黏附通常是感染的前奏。在许多情况下，这一过程由蛋白质 - 碳水化合物相互作用所调控。在感染的这个早期阶段进行干预，相对于越来越容易产生耐药性的传统抗生素而言，在概念上是极具吸引力的替代方案。事实证明，缺乏高亲和力的黏附抑制剂是进一步利用这一概念的障碍；然而，新的进展表明情况正在积极变化。基于结构的单价水平设计以及对糖树枝状大分子和糖聚合物的评估已产生了高亲和力的结构。除了抑制剂的开发，本综述的主题还包括黏附蛋白的现有结构信息、各种病原体及其黏附蛋白的碳水化合物特异性。还讨论了旨在影响细菌黏附的其他新进展以及利用黏附素来进行细菌检测的情况。
