תפריט נגישות
ניגודיות עדינהניגודיות גבוהה
מונוכרום
הדגשת קישורים
חסימת אנימציה
פונט קריא
סגור
איפוס הגדרות נגישות
להורדת מודול נגישות חינם תפריט נגישותניגודיות עדינהניגודיות גבוההמונוכרוםהדגשת קישוריםחסימת אנימציהפונט קריאסגוראיפוס הגדרות נגישותלהורדת מודול נגישות חינםC. Gilon
Insect neuropeptides are a prime target in the development of novel insect-control agents due to their major importance in regulating the physiology of insects. Antagonists, which are selective inhibitors of the neuropeptide receptors, may disrupt and interfere with the normal growth, development, homeostasis and behavior of the insect by blocking the receptor of the neuropeptide; therefore, they can form receptor-selective, insect-specific insecticides. Recently, we have developed a novel approach, termed the backbone cyclic neuropeptide-based antagonist (BBC-NBA) for the discovery of neuropeptide antagonists. This approach has been applied to the insect pyrokinin/pheromone biosynthesis activating neuropeptide (PBAN) family and resulted in the discovery of highly potent, stable and selective antagonists. The steps that comprise the BBC-NBA approach (e.g., development of simple and quantitative in vitro and in vivo bioassays for monitoring bioactivity of compounds of interest, elucidation of the shortest sequence of PBAN that constitutes the active site, determination of the structure activity relationship of peptides originating from linear peptide libraries and backbone cyclic conformational libraries) will be presented, and the application of the antagonists for the study of the functional diversity and characterization of the receptor(s) of the pyrokinin/PBAN family as well as their possible application as insect control agents will be discussed.
C. Gilon
Insect neuropeptides are a prime target in the development of novel insect-control agents due to their major importance in regulating the physiology of insects. Antagonists, which are selective inhibitors of the neuropeptide receptors, may disrupt and interfere with the normal growth, development, homeostasis and behavior of the insect by blocking the receptor of the neuropeptide; therefore, they can form receptor-selective, insect-specific insecticides. Recently, we have developed a novel approach, termed the backbone cyclic neuropeptide-based antagonist (BBC-NBA) for the discovery of neuropeptide antagonists. This approach has been applied to the insect pyrokinin/pheromone biosynthesis activating neuropeptide (PBAN) family and resulted in the discovery of highly potent, stable and selective antagonists. The steps that comprise the BBC-NBA approach (e.g., development of simple and quantitative in vitro and in vivo bioassays for monitoring bioactivity of compounds of interest, elucidation of the shortest sequence of PBAN that constitutes the active site, determination of the structure activity relationship of peptides originating from linear peptide libraries and backbone cyclic conformational libraries) will be presented, and the application of the antagonists for the study of the functional diversity and characterization of the receptor(s) of the pyrokinin/PBAN family as well as their possible application as insect control agents will be discussed.
