Fundación Instituto de Inmunología de Colombia (FIDIC), Universidad del Rosario and Universidad Nacional de Colombia, Bogotá DC, Colombia.
Molecules. 2010 Dec 6;15(12):8856-89. doi: 10.3390/molecules15128856.
Synthetic vaccines constitute the most promising tools for controlling and preventing infectious diseases. When synthetic immunogens are designed from the pathogen native sequences, these are normally poorly immunogenic and do not induce protection, as demonstrated in our research. After attempting many synthetic strategies for improving the immunogenicity properties of these sequences, the approach consisting of identifying high binding motifs present in those, and then performing specific changes on amino-acids belonging to such motifs, has proven to be a workable strategy. In addition, other strategies consisting of chemically introducing non-natural constraints to the backbone topology of the molecule and modifying the α-carbon asymmetry are becoming valuable tools to be considered in this pursuit. Non-natural structural constraints to the peptide backbone can be achieved by introducing peptide bond isosters such as reduced amides, partially retro or retro-inverso modifications or even including urea motifs. The second can be obtained by strategically replacing L-amino-acids with their enantiomeric forms for obtaining both structurally site-directed designed immunogens as potential vaccine candidates and their Ig structural molecular images, both having immuno-therapeutic effects for preventing and controlling malaria.
合成疫苗是控制和预防传染病最有前途的工具。当从病原体天然序列设计合成免疫原时,这些免疫原通常免疫原性差,不能诱导保护,正如我们的研究所示。在尝试了许多提高这些序列免疫原性特性的合成策略之后,确定存在于这些序列中的高结合基序并对属于这些基序的氨基酸进行特异性改变的方法已被证明是一种可行的策略。此外,通过在分子骨架拓扑结构上化学引入非天然约束并修饰α-碳原子不对称性的其他策略也成为在这方面考虑的有价值的工具。可以通过引入肽键类似物(如还原酰胺、部分反式或反式-反式修饰或甚至包含脲基模体)来实现肽骨架的非天然结构约束。可以通过战略性地用其对映体替代 L-氨基酸来获得第二种方法,以获得结构上定向设计的免疫原,作为潜在的疫苗候选物及其 Ig 结构分子图像,两者都具有免疫治疗效果,可预防和控制疟疾。