Structure-activity relationship of a broad-spectrum insect odorant receptor agonist.

Taylor RW, Romaine IM, Liu C, Murthi P, Jones PL, Waterson AG, Sulikowski GA, Zwiebel LJ
ACS Chem Biol. 2012 7 (10): 1647-52

PMID: 22924767 · DOI:10.1021/cb300331z

Agonism of insect odorant receptor (OR) cation channels may represent a new strategy for the manipulation of destructive insect olfactory-driven behaviors. We have explored the chemical space around VUAA1, the first in class agonist of the obligate OR co-receptor ion channel (Orco), and describe novel compound analogues with increased potency across insect taxa. Functional analyses reveal several of these VUAA1 structural analogues display significantly greater potency as compared to the activity of the previously described active compounds in mobility-based behavioral assays on mosquito larvae.

MeSH Terms (13)

Animals Anopheles Behavior, Animal HEK293 Cells Humans Ion Channels Larva Motor Activity Receptors, Odorant RNA, Small Interfering Structure-Activity Relationship Thioglycolates Triazoles

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