| Title: | Discovery of a linear lead antagonist to the insect pheromone biosynthesis activating neuropeptide (PBAN) |
| Author(s): | Zeltser I; Gilon C; Ben-Aziz O; Schefler I; Altstein M; |
| Address: | "Dept. of Organic Chemistry, The Hebrew Univ. of Jerusalem, 91904, Jerusalem, Israel" |
| DOI: | 10.1016/s0196-9781(00)00298-9 |
| ISSN/ISBN: | 0196-9781 (Print) 0196-9781 (Linking) |
| Abstract: | We report the discovery of a linear lead antagonist for the insect pheromone biosynthesis activating neuropeptide (PBAN) which inhibits sex pheromone biosynthesis in the female moth Heliothis peltigera. Two approaches have been used in attempting to convert PBAN agonists into antagonists. The first involved omission of the C-terminal amide and reduction of the sequence from the N-terminus in a linear library based on PBAN 1-33NH(2.) The second involved replacement of L amino-acids by the D hydrophobic amino acid D-Phe in a linear library based on PBAN28-33NH(2.) Screening of the two libraries for pheromonotropic antagonists resulted in the disclosure of one compound out of the D-Phe library (Arg-Tyr-Phe-D-Phe-Pro-Arg-Leu-NH(2)) which inhibited sex pheromone production by 79 and 64% at 100 pmol in two moth colonies and exhibited low agonistic activity. Omission of the C-terminal amide in PBAN 1-33NH(2) and its shorter analogs did not lead to the discovery of an antagonistic compound |
| Keywords: | Amino Acid Sequence Animals Female Moths/*drug effects/metabolism Neuropeptides/agonists/*antagonists & inhibitors/chemistry/metabolism Oligopeptides/chemical synthesis/chemistry/pharmacology Peptide Fragments/chemical synthesis/chemistry/*pharmacology Pe; |
| Notes: | "MedlineZeltser, I Gilon, C Ben-Aziz, O Schefler, I Altstein, M eng Research Support, Non-U.S. Gov't 2000/11/09 Peptides. 2000 Oct; 21(10):1457-65. doi: 10.1016/s0196-9781(00)00298-9" |
