Open Access
A novel dihydroimidazoline, trans-Pro mimetic analog is a selective PK/PBAN agonist
Ronald J Nachman1,Orna Ben Aziz1,Michael Davidovitch1,Krzysztof Kaczmarek1,Janusz Zabrocki1,Howard Williams1,Allison Strey1,Miriam Altstein1
US Department of Agriculture, Areawide Pest Management Research, Southern Plains Agricultural Research Center, College Station, TX 77845, USA.
DOI: 10.2741/E82 Volume 2 Issue 1, pp.195-203
Published: 01 January 2010
(This article belongs to the Special Issue Developmental and neuronal plasticity)

The pyrokinin/pheromone biosynthesis activating neuropeptide (PK/PBAN) family plays a significant role in the regulation of reproductive and developmental processes in a variety of insects. A transPro, type I beta-turn has been previously identified as important for the activity of PK/PBAN peptides. A PK/PBAN analog (PPK-Jo) incorporating a novel dihydroimidazole transPro mimetic motif was evaluated in four PK/PBAN bioassays (pheromonotropic, melanotropic, pupariation and hindgut myotropic). PPK-Jo proved to be a pure, selective melanotropic agonist in S. littoralis. The melanotropic receptor in S. littoralis demonstrates more tolerance to deviations from the ideal transPro structure than those of other PK/PBAN assays. The selective PK/PBAN agonist represents a new tool to better understand the endogenous mechanisms of these peptides and serves as a probe of the plasticity of PK/PBAN regulated systems and receptors. The dihydroimidazoline moiety is shown to function as a surrogate for a transPro in certain circumstances, and provides a novel scaffold with which to construct mimetic PK/PBAN analogs with enhanced selectivity and the potential to disrupt critical physiological processes in insect pests.

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Ronald J Nachman, Orna Ben Aziz, Michael Davidovitch, Krzysztof Kaczmarek, Janusz Zabrocki, Howard Williams, Allison Strey, Miriam Altstein. A novel dihydroimidazoline, trans-Pro mimetic analog is a selective PK/PBAN agonist. Frontiers in Bioscience-Elite. 2010. 2(1); 195-203.