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Updated: May 12, 2026
06:01
Extracellular Protein Microarray Technology for High Throughput Detection of Low Affinity Receptor-Ligand Interactions
Published on: January 7, 2019
G protein-coupled receptor microarrays for drug discovery
Ye Fang1, Joydeep Lahiri, Laurent Picard
1Biochemical Sciences Science and Technology, Division Corning Incorporated, Sullivan Park, Corning, NY 14831, USA. fangy2@corning.com
Drug Discovery Today
|April 12, 2013
Summary
Developing GPCR microarrays enables simultaneous screening of multiple G protein-coupled receptors (GPCRs). This technology aids in evaluating drug compound properties like binding affinity and potency efficiently.
Area of Science:
- Biochemistry
- Pharmacology
- Biotechnology
Background:
- G protein-coupled receptors (GPCRs) are a major class of drug targets.
- High-throughput screening is crucial due to expanding compound libraries and target identification.
Purpose of the Study:
- To develop and discuss GPCR microarrays for simultaneous screening of multiple receptors.
- To enable efficient evaluation of pharmacological properties of drug compounds.
Main Methods:
- Fabrication of GPCR microarrays using robotic printing.
- Co-immobilization of lipid molecules and probe receptors on microarrays.
- Development of assays for screening binding affinity, relative potency, and selectivity.
Main Results:
- Successful fabrication of functional GPCR microarrays.
- Demonstration of assays for assessing compound pharmacological properties.
- Potential for high-throughput screening of GPCR-targeted drugs.
Conclusions:
- GPCR microarrays offer a powerful platform for drug discovery.
- This technology facilitates simultaneous assessment of multiple GPCRs.
- Enables efficient characterization of drug candidates' efficacy and specificity.
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...
01:21G-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.
01:30Transducer 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...
02:34DNA Microarrays
Microarrays are high-throughput and relatively inexpensive assays that can be automated to analyze large quantities of data at a time. They are used in genome-wide studies to compare gene or protein expression under two varied conditions, such as healthy and diseased states. Microarrays consist of glass or silica slides on which probe molecules are covalently attached through surface functionalization. Most commonly, the slides are prepared through the chemisorption of silanes to silica...