Profacgen offers professional high-throughput GPCR screening service for the identification of potential GPCR-targeting drugs. G protein-coupled receptors (GPCRs) are also known as seven-transmembrane domain receptors. They are only found in eukaryotes. Because of their extensive involvement in cell signal transduction, GPCRs have become important drug targets. Nearly 40% of modern drugs are GPCR-targeted, and 20% of top the 50 best-selling drugs are GPCR related.
GPCRs are found in yeast, choanoflagellates, and animals. Ligands that bind and activate GPCRs include light-sensitive compounds, odors, pheromones, hormones, and neurotransmitters, and range from small molecules, peptides to large proteins. The signal transduction is initiated by ligand binding to GPCR. With the change of GPCR conformation, G protein is activated and dissociates into α- and β/γ- subunits. Second messengers (cAMP, IP3, calcium, etc.) are then generated and trigger subsequent signaling cascade. The GPCR family includes about 600-1000 members, and can be grouped into 6 classes based on their sequence homology and function similarity: class A (rhodopsin-like), class B (secretin receptor family), class C (metabotropic glutamate/pheromone), class D (fungal mating pheromone receptors), class E (cyclic AMP receptors) and class F (frizzled/smoothened). GPCRs play important roles in the regulation of cell proliferation, division and migration. The structural characteristics and vital effect in signal transduction makes GPCR a perfect drug target. GPCR screening and profiling technology is now widely used in novel drug screening for infectious diseases, cardiovascular diseases, mental diseases, Acquired Immune Deficiency Syndrome (AIDS), diabetes, cancer and so on.
Schematic diagram of GPCR 
Profacgen provides a comprehensive list of services to help with your GPCR study. Our services include cell membrane preparation, signal detection and high-throughput screening.
We have developed the following signal detection assays:
We provide a large collection of screening panels covering all GPCR classes. We can do rapid profiling of your compounds against a panel of GPCRs, or perform more in-depth EC50/IC50 determinations. We can also help with design your customized GPCR analytical scheme based on your requirements and your preliminary results, such as GPCR agonist screening, GPCR antagonist screening, GPCR allosteric modulator screening, GPCR inverse agonist screening, etc. Whether you focus on hit identification, selectivity profiling or structure-activity relationship (SAR) optimization, Profacgen can help accelerate your GPCR study. We provide ultimate flexibility for the ideal screening platform to meet your requirements. All projects will include necessary controls and a comprehensive report.
Our state-of-the-art GPCR solution:
Please contact us for more details of our GPCR screening service. Our experts will provide you with optimal solution for your project in GPCR screening project.
See the instruction of GPCR screening service. Find the targets’ family list available in our GPCR service and the functional/binding assays we could provide to you.
Click here to download the Service Instruction.
 Alberts B, Johnson A, Lewis J, et al. Molecular Biology of the Cell. 5th ed. New York: Garland Science; 2008.