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Pyrokinin/PBAN antagonists: Potent research tools and a basis for the design of a novel group of insect control agents [abstract]
Year:
2001
Authors :
Altstein, Miriam
;
.
Ben-Aziz, Orna
;
.
Schaeffler, Irit
;
.
Volume :
Co-Authors:

C. Gilon

Facilitators :
From page:
0
To page:
0
(
Total pages:
1
)
Abstract:

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.
 

Note:
Related Files :
Antagonists
Heliothis peltigera
Insect control
insects
Lepidoptera
Neuropeptides
PBAN
plant protection
pyrokinin
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DOI :
Article number:
0
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Publication Type:
Abstract
;
.
Conference paper
;
.
Language:
English
Editors' remarks:
ID:
52306
Last updated date:
02/03/2022 17:27
Creation date:
14/12/2020 09:15
Scientific Publication
Pyrokinin/PBAN antagonists: Potent research tools and a basis for the design of a novel group of insect control agents [abstract]

C. Gilon

Pyrokinin/PBAN antagonists: Potent research tools and a basis for the design of a novel group of insect control agents

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.
 

Scientific Publication
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