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Vaccine Detail
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3′-fluoro-6TF–MUC1–BSA conjugate vaccine |
| Vaccine Information |
- Vaccine Name: 3′-fluoro-6TF–MUC1–BSA conjugate vaccine
- Target Pathogen: Cancer
- Target Disease: Cancer
- Type: Conjugate vaccine
- Status: Research
- Host Species for Licensed Use: Mouse
- Antigen: MUC1 VNTR (20-mer, PAHGVTSAPDTRPAPGSTAP), 3′-F-TF at T6 (Hoffmann-Röder and Johannes, 2011)
- Immunization Route: subcutaneous injection
- Description: A synthetic MUC1-glycopeptide–BSA conjugate vaccine bearing the 3′-deoxy-3′-fluoro-Thomsen–Friedenreich (TF) antigen at Thr6 of the 20-amino acid MUC1 tandem-repeat-derived sequence (PAHGVTSAPDTRPAPGSTAP). The glycopeptide was assembled by automated Fmoc solid-phase peptide synthesis (SPPS) on trityl-TentaGel resin preloaded with Fmoc-Pro-OH and conjugated to BSA via diethyl squarate chemistry, with an average loading of five glycopeptide molecules per BSA molecule as determined by MALDI-TOF mass spectrometry. A triethylene glycol spacer was attached at the N-terminus prior to conjugation. Fluorination was incorporated as it might enhance both the immunogenicity and the bioavailability of the tumor-associated antigen, exploiting the absence of fluorine in most biological systems and the high C–F bond strength. Preliminary immunological experiments using neutralization ELISA demonstrated that mouse anti-MUC1 serum antibodies raised against the structurally related ⁶TF–MUC1–TTox and 6′,6-difluoro-⁶TF–MUC1–TTox vaccines were considerably neutralized by the 3′-fluorinated glycopeptide antigen 10, supporting the notion that the fluorinated glycoconjugate 11 is a promising cancer vaccine candidate, with further immunization studies ongoing (Hoffmann-Röder and Johannes, 2011).
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| Host Response |
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| References |
Hoffmann-Röder and Johannes, 2011: Hoffmann-Röder A, Johannes M. Synthesis of a MUC1-glycopeptide-BSA conjugate vaccine bearing the 3'-deoxy-3'-fluoro-Thomsen-Friedenreich antigen. Chemical communications (Cambridge, England). 2011; 47(35); 9903-9905. [PubMed: 21818465].
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