Calix[4]arene decorated with four tn antigen glycomimetic units and P3CS immunoadjuvant:: Synthesis, characterization, and anticancer immunological evaluation
Calix[4]arene decorated with four tn antigen glycomimetic units and P3CS immunoadjuvant:: Synthesis, characterization, and anticancer immunological evaluation
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DOI：
10.1021/bc700411w
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发表时间：
2008-03-01
影响因子：
4.7
通讯作者：
Spadaro, Angelo
中科院分区：
文献类型：
--
作者：
Geraci, Corrada;Consoli, Grazia M. L.;Spadaro, Angelo
已经合成了一种基于非肽支架的新型抗癌候选疫苗。四种S-Tn肿瘤相关的糖模拟抗原已经聚集到带有免疫佐剂部分（P3 CS）的杯[4]芳烃支架上。通过小鼠体内免疫研究了合成构建体的免疫原性。ELISA测定证明，与类似的单价化合物相比，四价构建体刺激更高的抗Tn抗原IgG抗体的产生。这一结果归因于抗原簇效应，并使得所报道的疫苗候选物成为粘蛋白表面上存在的天然基序的良好模拟物。
A novel anticancer vaccine candidate built on a nonpeptidic scaffold has been synthesized. Four S-Tn tumor-associated glycomimetic antigens have been clustered onto a calix[4]arene scaffold bearing an immunoadjuvant moiety (P3CS). The immunogenicity of the synthetic construct has been investigated by immunization of mice in vivo. ELISA assay has evidenced that the tetravalent construct stimulates a higher production of anti-Tn antigen IgG antibodies when compared to an analogous monovalent compound. This result is ascribable to an antigen cluster effect and makes the reported vaccine candidate a good mimic of the natural motifs present on the mucine surface.