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Structure-Activity Relationship of a Broad-Spectrum Insect Odorant Receptor Agonist

  作者 TAYLOR ROBERT W; ROMAINE IAN M; LIU CHAO; MURTHI POORNIMA; JONES PATRICK L; WATERSON ALEX G; SULIKOWSKI GARY A; ZWIEBEL LAURENCE J  
  选自 期刊  ACS CHEMICAL BIOLOGY;  卷期  2012年7-10;  页码  1647-1652  
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[摘要]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.

 
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