Structure鈥揂ctivity Relationship of a Broad-Spectrum Insect Odorant Receptor Agonist
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- 作者：Robert W. Taylor ; Ian M. Romaine ; Chao Liu ; Poornima Murthi ; Patrick L. Jones ; Alex G. Waterson ; Gary A. Sulikowski ; Laurence J. Zwiebel
- 刊名：ACS Chemical Biology
- 出版年：2012
- 出版时间：October 19, 2012
- 年：2012
- 卷：7
- 期：10
- 页码：1647-1652
- 全文大小：447K
- 年卷期：v.7,no.10(October 19, 2012)
- ISSN：1554-8937
文摘
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.