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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
Using adaptive K-nearest neighbor algorithm and cellular automata images to predicting G-Protein-Coupled Receptor
1Computer Department, Jing-De-Zhen Ceramic Institute, Jingdezhen, China. xiaoxuan0326@yahoo.com.cn
Interdisciplinary Sciences, Computational Life Sciences
|July 20, 2010
Summary
This study introduces a computational method using adaptive K-nearest neighbor and protein CAI to classify G-Protein-Coupled Receptors (GPCRs) by their primary sequence, aiding drug discovery.
Area of Science:
- Biochemistry
- Computational Biology
- Pharmacology
Background:
- G-Protein-Coupled Receptors (GPCRs) are crucial cell surface receptors involved in numerous physiological processes.
- Many GPCR functions remain unknown due to challenges in crystallization and solubility, hindering drug development.
Purpose of the Study:
- To develop a computational method for classifying GPCR families and subfamilies based on primary sequence.
- To aid in the classification of drugs targeting GPCRs and facilitate the design of new medications.
Main Methods:
- Utilized the adaptive K-nearest neighbor algorithm.
- Employed protein Cellular Automata Image (CAI) and derived complexity measure factors for Pseudo amino acid composition.
- Categorized GPCRs into nine distinct subtypes.
Main Results:
- Achieved an overall success rate of approximately 83.5% in identifying GPCRs within their nine family classes.
- Demonstrated the effectiveness of the combined computational approach for GPCR classification.
Conclusions:
- The adaptive K-nearest neighbor algorithm and protein CAI show significant potential as tools for GPCR research.
- This method can advance the understanding of drug actions on GPCRs and support the design of more effective and safer medications.
Related Concept Videos
01:15G Protein-coupled Receptors
G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
01:15G Protein-coupled Receptors
G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
01:30Transducer Mechanism: G Protein–Coupled Receptors
G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
GPCRs are also called heptahelical, 7TM, or...
GPCRs are also called heptahelical, 7TM, or...
01:21G-protein Coupled Receptors
G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
01:21G-protein Coupled Receptors
G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
01:27Adrenergic Receptors (Adrenoceptors): Classification
Adrenergic receptors, or adrenoceptors, respond to the autonomic neurotransmitter noradrenaline and other endogenous catecholamine agonists. They are classified into two main families, α and β, based on their pharmacological response and are further subdivided depending on their location, elicited response, and affinity to specific agonists or antagonists.
α-Adrenoceptors
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α-Adrenoceptors
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