Design, Synthesis, and Preliminary Immunological Studies of MUC1-Based Antitumor Vaccines Adjuvanted with R- and S-FSL-1
| Autor: | Haomiao Zhu, Bocheng Yan, Yonghui Liu, Zhaoyu Wang, Xiaona Yin, Kun Wang, Menglei Wang, Wei Zhao |
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| Rok vydání: | 2020 |
| Předmět: |
Fibroblast-stimulating lipopeptide-1
010405 organic chemistry Chemistry medicine.medical_treatment Organic Chemistry Pharmacology Ligand (biochemistry) 01 natural sciences Biochemistry 0104 chemical sciences 010404 medicinal & biomolecular chemistry Vaccine adjuvant Design synthesis Drug Discovery medicine Adjuvant MUC1 |
| Zdroj: | ACS Med Chem Lett |
| ISSN: | 1948-5875 |
| DOI: | 10.1021/acsmedchemlett.9b00579 |
| Popis: | [Image: see text] 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-Pam(2)Cys-OH and S-Fmoc-Pam(2)Cys-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. |
| Databáze: | OpenAIRE |
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