Nachman R J, Coast G M, Holman G M, Haddon W F
U.S. Department of Agriculture, Veterinary Entomology Research Unit, College Station, TX.
Int J Pept Protein Res. 1992 Nov;40(5):423-8. doi: 10.1111/j.1399-3011.1992.tb00320.x.
The synthesis and biological activity of a bifunctional, heterodimeric insect neuropeptide analog are described. The heterodimer is composed of the C-terminal pentapeptide active core regions of the leucokinin/achetakinin and pyrokinin neuropeptide families linked via their N-terminal amino groups with a succinyl diacid moiety. Members of the leucokinin/achetakinin family can induce fluid secretion in malpighian tubules of the house cricket, Acheta domesticus, whereas the pyrokinins demonstrate activity in a cricket oviduct myotropic bioassay. No cross-activity is observed for the two neuropeptide families in these bioassays. However, the heterodimer elicits responses in both Acheta bioassays. Such a bifunctional analog may in future serve as a template for the design of stable, bifunctional pest insect control agents of greater efficiency.
描述了一种双功能异源二聚体昆虫神经肽类似物的合成及其生物活性。该异源二聚体由亮激肽/阿切激肽和焦激肽神经肽家族的C端五肽活性核心区域组成，它们通过N端氨基与琥珀酸二酸部分相连。亮激肽/阿切激肽家族的成员可诱导家蟋蟀（Acheta domesticus）马氏管中的液体分泌，而焦激肽在蟋蟀输卵管肌动生物测定中表现出活性。在这些生物测定中，未观察到这两个神经肽家族的交叉活性。然而，该异源二聚体在两种家蟋蟀生物测定中均引发反应。这种双功能类似物未来可能作为设计更高效、稳定的双功能害虫防治剂的模板。
