Full synthesis and bioactivity evaluation of Tn-RC-529 derivative conjugates as self-adjuvanting cancer vaccines
Full synthesis and bioactivity evaluation of Tn-RC-529 derivative conjugates as self-adjuvanting cancer vaccines
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DOI：
10.1016/j.cclet.2021.03.046
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发表时间：
2021-11-17
影响因子：
9.1
通讯作者：
Liao, Guochao
中科院分区：
文献类型：
--
作者：
Gao, Lingqiang;Lian, Qinghai;Liao, Guochao
为RC-529及其衍生物的构建建立了一种简便有效的策略。合成了RC-529衍生物与Tn抗原的四种缀合物，并且全部在小鼠中引发强烈的和T细胞依赖性免疫应答，而不需要外部佐剂。此外，由这些缀合物诱导的所有抗血清都可以特异性地识别、结合并杀死过度表达Tn的癌细胞。因此，RC-529显示出作为用于开发用于治疗癌症的具有自佐剂性质的新疫苗载体的有用平台的前景。此外，初步的构效关系分析为RC-529的进一步优化和进一步研究提供了令人信服的支持。(c)2021中国化学会、中国医学科学院药物研究所。Elsevier B. V.出版，保留所有权利。
A facile and efficient strategy was established for the construction of RC-529 and its derivatives. Four conjugates of RC-529 derivatives with Tn antigen were synthesized and all elicited strong and T cell dependent immune responses in mice without requiring external adjuvants. In addition, all antisera induced by these conjugates could specifically recognize, bind to and kill Tn-overexpressing cancer cells. Thus, RC-529 shows promise as a useful platform for the development of new vaccine carriers with self-adjuvanting properties for the treatment of cancer. Moreover, preliminary structure-activity relationship analysis provides convincing support for further optimization of, and additional investigation into RC-529. (c) 2021 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. Published by Elsevier B.V. All rights reserved.