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

被引：47
|
作者：
Taylor, Robert W. [1 ]
Romaine, Ian M. [2 ]
Liu, Chao [1 ]
Murthi, Poornima [1 ]
Jones, Patrick L. [1 ]
Waterson, Alex G. [2 ,3 ]
Sulikowski, Gary A. [2 ]
Zwiebel, Laurence J. [1 ,3 ,4 ,5 ]
机构：
[1] Vanderbilt Univ, Dept Biol Sci, Vanderbilt Inst Chem Biol, Nashville, TN 37235 USA
[2] Vanderbilt Univ, Dept Chem, Vanderbilt Inst Chem Biol, Nashville, TN 37235 USA
[3] Vanderbilt Univ, Med Ctr, Dept Pharmacol, Nashville, TN 37235 USA
[4] Vanderbilt Univ, Med Ctr, Inst Global Hlth, Ctr Mol Neurosci, Nashville, TN 37235 USA
[5] Vanderbilt Univ, Med Ctr, Program Dev Biol, Nashville, TN 37235 USA
来源：
ACS CHEMICAL BIOLOGY | 2012年 / 7卷 / 10期
基金：
美国国家卫生研究院;
关键词：
CONSERVATION; BEHAVIOR;
D O I：
10.1021/cb300331z
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
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.
引用
收藏
页码：1647 / 1652
页数：6
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