Small Molecule Antagonists for Arthropod Kinin Receptor Control
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Solution Overview
Problem
Current methods for controlling arthropod pests, such as ticks and mosquitoes, face challenges due to the high cost and instability of peptide-based solutions, as well as increasing resistance to acaricides, necessitating the development of novel, cheaper, and more stable compounds that can effectively target arthropod kinin receptors.
Innovation Solution
The development of small molecule antagonists and agonists for arthropod kinin receptors, which can be formulated into antiparasitic compositions for topical application or used in sugar baits, to control parasitic infestations and prevent disease spread, while also being suitable for in silico screening and validation.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If peptide-based solutions are used to control arthropod pests, then they can effectively target kinin receptors, but they are expensive and unstable
Solution Approach 1:
The patent creates small molecule copies that mimic the biological activity of peptide ligands. These small molecules replicate the kinin receptor binding capability of peptides but with improved stability and lower cost, effectively copying the desirable functional properties while eliminating the drawbacks of the original peptides
Solution Approach 2:
The patent changes the chemical parameters from peptide-based structures to small molecule structures. This parameter change transforms the compounds from expensive and unstable peptides to cost-effective and stable small molecules while maintaining the ability to bind to and modulate kinin receptors
2Reliability
If peptide-based solutions are used to control arthropod pests, then they can effectively target kinin receptors, but they are expensive to mass-produce
Solution Approach 1:
The patent creates small molecule copies that mimic the biological activity of peptide ligands. These small molecules replicate the kinin receptor binding capability of peptides but with improved stability and lower cost, effectively copying the desirable functional properties while eliminating the drawbacks of the original peptides
Solution Approach 2:
The patent replaces expensive peptide compounds with inexpensive small molecule alternatives. These small molecules can be mass-produced at lower cost while maintaining the necessary biological activity for pest control applications
3Productivity
If human neurokinin receptor antagonists are screened for tick kinin receptor activity, then high-throughput screening can be performed, but the activity is low due to evolutionary differences
Solution Approach 1:
The patent uses recombinant tick kinin receptors expressed in heterologous cells as an intermediary system. This allows high-throughput screening to be performed while maintaining relevance to the target arthropod receptor, bridging the gap between convenient screening methods and species-specific biological activity
Solution Approach 2:
The patent creates a universal screening platform using recombinant receptor expression that can evaluate compounds against arthropod-specific kinin receptors. This universal system allows human-derived compound libraries to be screened for activity against insect and tick receptors despite evolutionary divergence
4Reliability
If conventional acaricides are used for tick control, then they can effectively kill ticks, but resistance is increasing worldwide
Solution Approach 1:
The patent inverts the conventional approach by targeting a neuropeptide receptor (kinin receptor) rather than traditional insecticide targets. This novel mechanism of action, opposite to conventional acaricides, provides effectiveness against ticks while avoiding the resistance issues that have developed against traditional chemicals
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
These small molecules demonstrate significant activity against arthropod kinin receptors, offering a cost-effective and stable solution for pest control, with potential for broad-spectrum action and resistance management, as evidenced by their ability to prolong feeding time on sugar baits and inhibit tick kinin receptor activity.
Implementation Method 1
The tick kinin receptor couples to Gαq/11 protein. Upon binding of an agonist, GPCRs coupled with different Gα proteins trigger different downstream cellular signaling pathways
Implementation Method 2
Upon binding of an agonist, GPCRs coupled with different Gα proteins trigger different downstream cellular signaling pathways and result in changes in concentration of second messengers, such as calcium ions (Ca2+) or cyclic adenosine monophosphate (cAMP)
Data Source
AI summary
Applicants have developed novel methods and compositions for controlling, treating, preventing, or ameliorating arthropod infection and identifying kinin receptor agonists and antagonists. Novel compositions include one or more active agents of small molecules antagonists or agonists of arthropod kinin receptor. Methods of preventing disease development and infestation by arthropods are disclosed as well as methods of making, using, and producing such compositions.