Journal
PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY
Volume 120, Issue -, Pages 82-90Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.pestbp.2014.10.017
Keywords
Glutamate-gated chloride channel; Ivermectin; Haemonchus contortus; Bombyx mori; Photoreactive probe; Photoaffinity labeling
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Funding
- JSPS KAKENHI [21310147, 26292031]
- Grants-in-Aid for Scientific Research [21310147, 26292031] Funding Source: KAKEN
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Glutamate-gated chloride channels (GluCls) are inhibitory neurotransmitter receptors that are present only in invertebrates such as nematodes and insects. These channels are important targets of insecticidal, acaricidal, and anthelmintic macrolides such as avermectins, ivermectin (IVM), and milbemycins. To identify the amino acid residues that interact with IVM in GluCls, three IVM B-1a derivatives with different photoreactive substitutions at C-13 were synthesized in the present study. These derivatives displayed low- or subnanomolar affinity for parasitic nematode (Haemonchus contortus) and silkworm (Bombyx mori) GluCls expressed in COS-1 cells. The derivatives also activated homomeric H. contortus GluCls expressed in Xenopus oocytes. The results indicate that synthesized photoreactive IVM B-1a derivatives have superior affinity and functionality for chemically labeling the macrolide-binding site in GluCls. (C) 2014 Elsevier Inc. All rights reserved.
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