2013
DOI: 10.1021/bc400242y
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First Self-Adjuvant Multicomponent Potential Vaccine Candidates by Tethering of Four or Eight MUC1 Antigenic Immunodominant PDTRP Units on a Calixarene Platform: Synthesis and Biological Evaluation

Abstract: MUC1 protein overexpressed in human epithelial carcinoma is a target in development of novel anticancer vaccines. Multiple units of immunodominant B-cell epitope PDTRP MUC1 core sequence were conjugated to calix[4,8]arene platforms containing TLR2 ligand, to produce two novel anticancer self-adjuvant vaccine candidates. The immunogenicity of the synthetic constructs was investigated by immunization of mice in vivo. ELISA assay evidenced that the vaccine candidates stimulate anti MUC1 IgG antibody production (m… Show more

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Cited by 47 publications
(40 citation statements)
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“…Geraci et al 30 also explored the immunotherapeutic anticancer activity of calixarene. They focused on MUC-1 protein, overexpression of which is associated with human epithelial carcinomas.…”
Section: Mechanisms Of Action Of Calixarene-based Anticancer Agentsmentioning
confidence: 99%
“…Geraci et al 30 also explored the immunotherapeutic anticancer activity of calixarene. They focused on MUC-1 protein, overexpression of which is associated with human epithelial carcinomas.…”
Section: Mechanisms Of Action Of Calixarene-based Anticancer Agentsmentioning
confidence: 99%
“…Spadoro and co-workers designed four-valent and eight-valent vaccines using calixarene to present the PDTRP motif from MUC1. The TLR2 agonist was introduced to the template by the ether group, and the vaccine produced antibodies against the PDTRP motif ( Figure 8 ) [ 59 ].…”
Section: Multivalency In Vaccine Designmentioning
confidence: 99%
“…Similarly, Geraci et al [90] synthesized the first examples of self-adjuvant vaccine candidates/immunotherapeutic anticancer agents of type 29 based on a calix [4] arene (Scheme 14). The main focus of this study was on MUC-1 protein, overexpression of which is connected with human epithelial carcinomas.…”
Section: Lower-and Upper-rim-functionalized Calix[4]arenesmentioning
confidence: 99%