Vaccines are one of the greatest achievements of modern medicine. Due to their safer profile, the latest investigations usually focus on subunit vaccines. However, the active component often needs to be coupled with an adjuvant to be effective and properly trigger an immune response. We are developing a new synthetic monosaccharide-based TLR4 agonist, such as glucosamine-derived compounds FP18 and FP20, as a potential vaccine adjuvant. In this study, we present a new FP20 derivative, FP20Hmp, with a hydroxylated ester linked to the glucosamine core. We show that the modification introduced improves the activity of the adjuvant and its solubility. This study presents the synthesis of FP20Hmp, its in vitro characterization, and in vivo activity while coupled with the ovalbumin antigen or in formulation with an enterococcal antigen. We show that FP20Hmp enables increased production of antigen-specific antibodies that bind to the whole bacterium.

Franco, A., Sadones, O., Romerio, A., Artusa, V., Shaik, M., Pasco, S., et al. (2024). Novel TLR4-Activating Vaccine Adjuvant Enhances the Production of Enterococcus faecium-binding Antibodies. JOURNAL OF MEDICINAL CHEMISTRY, 67(7), 5603-5616 [10.1021/acs.jmedchem.3c02215].

Novel TLR4-Activating Vaccine Adjuvant Enhances the Production of Enterococcus faecium-binding Antibodies

Franco, AR;Romerio, A;Artusa, V;Shaik, MM;Italia, A;Peri, F
2024

Abstract

Vaccines are one of the greatest achievements of modern medicine. Due to their safer profile, the latest investigations usually focus on subunit vaccines. However, the active component often needs to be coupled with an adjuvant to be effective and properly trigger an immune response. We are developing a new synthetic monosaccharide-based TLR4 agonist, such as glucosamine-derived compounds FP18 and FP20, as a potential vaccine adjuvant. In this study, we present a new FP20 derivative, FP20Hmp, with a hydroxylated ester linked to the glucosamine core. We show that the modification introduced improves the activity of the adjuvant and its solubility. This study presents the synthesis of FP20Hmp, its in vitro characterization, and in vivo activity while coupled with the ovalbumin antigen or in formulation with an enterococcal antigen. We show that FP20Hmp enables increased production of antigen-specific antibodies that bind to the whole bacterium.
Articolo in rivista - Articolo scientifico
Immunology; vaccines; resistant bacteria; TLR4; medicinal chemistry
English
21-mar-2024
2024
67
7
5603
5616
reserved
Franco, A., Sadones, O., Romerio, A., Artusa, V., Shaik, M., Pasco, S., et al. (2024). Novel TLR4-Activating Vaccine Adjuvant Enhances the Production of Enterococcus faecium-binding Antibodies. JOURNAL OF MEDICINAL CHEMISTRY, 67(7), 5603-5616 [10.1021/acs.jmedchem.3c02215].
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10281/474259
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