GPR72 Ligand Identification via Labeled PUFAs
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Solution Overview
Problem
Current methods lack effective identification and modulation of agents binding to the orphan G protein coupled receptor GPR72, which is crucial for understanding its role in various physiological and pathological processes, particularly in neurological disorders.
Innovation Solution
Polyunsaturated free fatty acids (PUFAs) and their derivatives, such as arachidonic acid and N-arachidonoyl-glycine, are identified as natural ligands for GPR72, enabling methods for screening agents that bind or modulate its activity, including the use of detectably labeled PUFAs and specific antibodies.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If traditional screening methods are used to identify GPR72 ligands, then the screening process can be performed with existing methodologies, but the ability to effectively identify and modulate agents binding to GPR72 is insufficient
Solution Approach 1:
The patent uses detectably labeled PUFAs as intermediaries to facilitate the identification of GPR72 binding agents. The labeled PUFAs serve as mediators between the GPR72 receptor and detection systems, enabling effective identification through their binding interactions while allowing for sensitive detection of agonists, antagonists, and inverse agonists
Solution Approach 2:
The patent employs parameter changes by utilizing detectable labels on PUFAs that allow measurement of binding events. By changing the detection parameters through labeled ligands, the screening method achieves both reliability in identification and productivity in screening capacity
2Loss of information
If no specific ligands are identified for GPR72, then the receptor remains uncharacterized, but understanding its role in physiological and pathological processes cannot be achieved
Solution Approach 1:
The patent performs preliminary action by identifying PUFAs as ligands for GPR72 before fully characterizing the receptor's physiological role. This preliminary identification of binding agents enables subsequent studies to understand the receptor's function in neurological and other physiological processes, preventing loss of critical information
3Loss of information
If GPR72 signaling pathways are not understood, then therapeutic applications cannot be developed, but insights into neurological disorders cannot be obtained
Solution Approach 1:
The patent employs feedback mechanisms by using detected binding events of labeled PUFAs to GPR72 to inform further characterization of signaling pathways. The detection results provide feedback that guides subsequent experiments to understand therapeutic potentials for neurological disorders, gradually building pathway knowledge
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
This approach allows for the identification of agonists, antagonists, and inverse agonists of GPR72, providing insights into its signaling pathways and potential therapeutic applications for neurological disorders.
Implementation Method 1
Upon binding of a ligand to an extra-cellular portion or fragment of a GPCR, a signal is transduced within the cell
Implementation Method 2
The detection or measuring of a signalling activity or measuring the binding of said GPR72 polypeptide comprises measurement of guanine nucleotide binding or exchange
Data Source
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AI summary
The present invention relates to methods, reagents and kits for detecting of GPR72 polypeptide activity in a sample and identifying agents which modulate polypeptide activity. It further relates to antibodies raised against GPR72. It further relates to substances for preventing, treating and/or alleviating diseases or disorders characterized by dysregulation of GPR72 polypeptide signalling.