The invention provides lipid A mimics in which one or both of the sugar residues of a natural lipid A disaccharide backbone has been replaced with an aromatic group. These lipid A mimics may further differ from a natural lipid A molecule with respect to other structural characteristics, such as, a different number of phosphate groups present, changes in the number, structure and location of lipid chains and/or changes in the spacing and linkage of the sugar residues (or their aromatic replacements). The lipid A mimics may be lipid A agonists and as such may be useful as immunostimulatory agents in inducing or patenting an antibody and/or cell-mediated immune response, or may be lipid A antagonists and as such may be useful in treating or preventing a lipopolysaccharide (LPS)/lipid A-mediated disease or disorder. Also provided are methods for preparing the lipid A mimics.
本发明提供了脂
多糖A(lipid A)类似物,其中天然脂
多糖A二糖骨架的一个或两个糖残基已被芳香族基团取代。这些脂
多糖A类似物可能还与天然脂
多糖A分子在其他结构特征方面有所不同,例如,存在不同数量的
磷酸基团,脂肪链的数量、结构和位置发生变化和/或糖残基(或其芳香族替代物)的间距和连接发生变化。这些脂
多糖A类似物可以是脂
多糖A激动剂,因此可用作免疫刺激剂,诱导或产生
抗体和/或细胞介导的免疫反应,或者可以是脂
多糖A拮抗剂,因此可用于治疗或预防脂
多糖体(LPS)/脂
多糖A介导的疾病或障碍。还提供了制备这些脂
多糖A类似物的方法。