| Title: | "A novel dihydroimidazoline, trans-Pro mimetic analog is a selective PK/PBAN agonist" |
| Author(s): | Nachman RJ; Ben Aziz O; Davidovitch M; Kaczmarek K; Zabrocki J; Williams H; Strey A; Altstein M; |
| Address: | "US Department of Agriculture, Areawide Pest Management Research, Southern Plains Agricultural Research Center, College Station, TX 77845, USA. nachman@tamu.edu" |
| ISSN/ISBN: | 1945-0508 (Electronic) 1945-0494 (Linking) |
| Abstract: | "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" |
| Keywords: | "Analysis of Variance Animals Dose-Response Relationship, Drug Imidazolines/*chemistry Insect Proteins/genetics/*metabolism/pharmacology Insecta/*metabolism Larva/drug effects/metabolism *Models, Molecular Molecular Mimicry Muscle Contraction/drug effects;" |
| Notes: | "MedlineNachman, Ronald J Ben Aziz, Orna Davidovitch, Michael Kaczmarek, Krzysztof Zabrocki, Janusz Williams, Howard Strey, Allison Altstein, Miriam eng Research Support, Non-U.S. Gov't Singapore 2009/12/29 Front Biosci (Elite Ed). 2010 Jan 1; 2(1):195-203. doi: 10.2741/e82" |
