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Antibiotics 2017, 6(3), 18;

Synthesis and Immunological Evaluation of Virus-Like Particle-Milbemycin A3/A4 Conjugates

Latvian Biomedical Research and Study Centre, Ratsupites 1, LV-1067 Riga, Latvia
Institute of Technology of Organic Chemistry, Riga Technical University, P. Valdena Str. 3, LV-1048 Riga, Latvia
PharmIdea Ltd., Rupnicu 4, Olaine, Riga District, LV-2114 Olaine, Latvia
Author to whom correspondence should be addressed.
Academic Editor: Christopher C. Butler
Received: 9 June 2017 / Revised: 9 August 2017 / Accepted: 7 September 2017 / Published: 11 September 2017
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Milbemycins are macrolide antibiotics with a broad spectrum of nematocidal, insecticidal, and acaricidal activity. To obtain milbemycin A3/A4 derivatives suitable for chemical conjugation to protein carriers (milbemycin haptens), succinate linker and a novel 17-atom-long linker containing a terminal carboxylic acid group were attached to the milbemycin core in a protecting group-free synthesis. The obtained milbemycin A3/A4 derivatives were coupled to Potato virus Y-like nanoparticles by the activated ester method. The reaction products were characterized and used in mice immunization experiments. It was found that the mice developed weak specific immune responses toward all tested milbemycin haptens. View Full-Text
Keywords: macrocyclic lactone; plant virus; hydrophobic hapten; ELISA macrocyclic lactone; plant virus; hydrophobic hapten; ELISA

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Zeltins, A.; Turks, M.; Skrastina, D.; Lugiņina, J.; Kalnciema, I.; Balke, I.; Bizdēna, Ē.; Skrivelis, V. Synthesis and Immunological Evaluation of Virus-Like Particle-Milbemycin A3/A4 Conjugates. Antibiotics 2017, 6, 18.

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