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首页> 外文期刊>Chemistry: A European journal >Synthesis of Branched Oxime-Linked Peptide Mimetics of the MUC1 Containing a Universal T-Helper Epitope
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Synthesis of Branched Oxime-Linked Peptide Mimetics of the MUC1 Containing a Universal T-Helper Epitope

机译：包含通用T辅助抗原决定簇的MUC1的支链肟连接肽模拟物的合成。

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Our goal was to develop mimics of MUC1,highly immunogenic to induce an efficient immune response against the tumor-associated form of MUC1,and sufficiently different from the natural antigen to bypass the tolerance barrier in humans.With the aim of obtaining a well-defined peptide construct as a means of evoking the precise immune responses required in immunotherapy,we synthesized artificial mimics of the MUC1 protein com-posed of two MUC1 repeat units of inverse orientation and a universal T-helper epitope.To synthesize these het-eromeric peptide constructs,we followed a convergent approach using chemoselective ligation based on oxime chemistry.A stem peptide was first synthesized bearing two orthogo-nally masked aldehydes.After successive deprotection,two oxime bonds can be specifically generated.The proposed strategy proved to be concise and robust,and allowed the synthesis of the tri-branched protein in a very satisfactory yield.The different constructs were tested for their ability to generate antibodies able to recognize the MUC1 protein.
机译：我们的目标是开发MUC1的模拟物，该模拟物具有高度免疫原性，可以诱导针对肿瘤相关形式的MUC1的有效免疫反应，并且与天然抗原有足够的差异以绕过人类的耐受性障碍。肽构建体作为激发免疫疗法所需的精确免疫反应的手段，我们合成了由两个反向MUC1重复单元和一个通用T辅助表位组成的MUC1蛋白的人工模拟物。 ，我们采用基于肟化学的化学选择性连接方法，采用收敛方法。首先合成了一个带有两个邻位被掩盖的醛的干肽。连续脱保护后，可以特异地生成两个肟键。并以非常令人满意的产率合成了三支蛋白质。测试了不同构建体的能力y生成能够识别MUC1蛋白的抗体。

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