Design, Synthesis, and Preliminary Immunological Studies of MUC1-Based Antitumor Vaccines Adjuvanted with R- and S-FSL-1.,ACS Medicinal Chemistry Letters

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Design, Synthesis, and Preliminary Immunological Studies of MUC1-Based Antitumor Vaccines Adjuvanted with R- and S-FSL-1.
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2020-06-22 , DOI: 10.1021/acsmedchemlett.9b00579
Yonghui Liu ₁ , Bocheng Yan ₁ , Zhaoyu Wang ₁ , Haomiao Zhu ₁ , Xiaona Yin ₁ , Kun Wang ₁ , Menglei Wang ₁ , Wei Zhao ₁

Affiliation

Fibroblast stimulating lipopeptide 1 (FSL-1) is the ligand of TLR2 and TLR6 and can be used as the vaccine adjuvant to prepare antitumor vaccines. However, FSL-1 is a stereoisomeric mixture that contains the R stereoisomer and S stereoisomer, and it is still unclear which stereoisomer has better adjuvant activities. In this work, we designed and synthesized MUC1-based antitumor vaccines adjuvanted with the stereoisomers R-FSL-1 and S-FSL-1, which were synthesized from the stereoisomeric building blocks R-Fmoc-Pam₂Cys-OH and S-Fmoc-Pam₂Cys-OH, respectively. Immunological evaluation indicated that both R-FSL-1 and S-FSL-1 can be used as adjuvants for the construction of MUC1-based antitumor vaccines, with R-FSL-1 showing a better adjuvant effect than S-FSL-1.

中文翻译：

基于MUC1的抗肿瘤疫苗与R-和S-FSL-1结合的设计，合成和初步免疫学研究。

成纤维细胞刺激脂肽1（FSL-1）是TLR2和TLR6的配体，可以用作制备抗肿瘤疫苗的疫苗佐剂。然而，FSL-1是包含R立体异构体和S立体异构体的立体异构混合物，并且仍不清楚哪种立体异构体具有更好的佐剂活性。在这项工作中，我们设计和合成了基于MUC1的抗肿瘤疫苗，这些疫苗佐以立体异构体R -FSL-1和S -FSL-1，它们是由立体异构体R -Fmoc-Pam ₂ Cys-OH和S -Fmoc合成的-Pam ₂ Cys-OH。免疫学评估表明，R-FSL-1和S -FSL-1可用作构建基于MUC1的抗肿瘤疫苗的佐剂，R -FSL-1显示出比S -FSL-1更好的佐剂效果。

更新日期：2020-07-09

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