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Design, Synthesis, and Preliminary Immunological Studies of MUC1-Based Antitumor Vaccines Adjuvanted with R- and S‑FSL‑1
journal contribution
posted on 2020-06-24, 18:43 authored by Yonghui Liu, Bocheng Yan, Zhaoyu Wang, Haomiao Zhu, Xiaona Yin, Kun Wang, Menglei Wang, Wei ZhaoFibroblast 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.
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TLR 6TLR 2adjuvant effectFSLstereoisomeric building blocks Rstereoisomeric mixtureMUC 1-Based Antitumor Vaccines AdjuvantedFmoc-Pam 2 Cys-OHMUC 1-based antitumor vaccines adjuvantedantitumor vaccinesvaccine adjuvantR stereoisomerstereoisomers RMUC 1-based antitumor vaccinesPreliminary Immunological StudiesImmunological evaluationadjuvant activitieslipopeptide 1S stereoisomer
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