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Sulikowski Lab

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

AUTHORS

Taylor RWRobert W , Romaine IM Ian M , Liu C Chao , Murthi P Poornima , Jones PL Patrick L , Waterson AG Alex G , Sulikowski GA Gary A , Zwiebel LJ Laurence J . ACS chemical biology. 2012 10 19; 7(10). 1647-52

ABSTRACT

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.

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.