Gpcr serves

comments (0) November 17th, 2019     

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Anserj339 Anserj339, member
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Gpcr serves protein-coupled receptors (GPCRs) are a large protein family of 7-transmembrane domain receptors. They can detect extracellular molecules, activate cellular signaling pathways and eventually elicit cellular responses. Based on their structural and functional characteristics, GPCRs are widely used as potential drug targets; they have become the targets for nearly 40% of all modern drugs.


GPCRs are found only in eukaryotes. Their ligands can be varied from light-sensitive compounds, odors, hormones, pheromones to neurotransmitters; the biological natures of which ranging from small molecules to peptides to large proteins. The binding of GPCR with its ligand will then initiate downstream signal transduction pathway. Studies have shown that GPCRs are extensively involved in a wide range of physiological processes, which can cause various diseases.


The conformational change of GPCRs upon ligand binding is vital for performing its function of signaling transduction. The downstream events following GPCR activation include GPCR dissociation into α- and β/γ- subunits and signaling cascade triggered by second messengers (cAMP, IP3, Ca2+, etc.).


GPCR superfamily can be grouped into 6 classes based on 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 significant roles in the regulation of cell proliferation, cell division and cell migration, etc. The structure-function relationship of a GPCR makes it a perfect drug target. These days, GPCR screening and profiling technology is widely used in novel drug screening for infectious diseases, cardiovascular diseases, mental diseases, Acquired Immune Deficiency Syndrome (AIDS), diabetes, and cancer, etc.


Illustration for the cellular signalling of GPCRs

Illustration for the cellular signalling of GPCRs


Profacgen provides a comprehensive package of services to facilitate your preclinical drug screening study concerning GPCR, from cell membrane preparation, signal detection to high-throughput screening.


Our signal detection assays include:


  Cell-based functional assay: second messengers and reporter genes.

  Ligand-receptor binding assay (radio-labeled isotope ligand): arrestin recruitment, receptor internalization.

  Cell-based high content screening.

Profacgen has developed a large collection of screening panels covering all kinds of GPCRs. We can do rapid profiling of your compounds against a panel of GPCRs, or perform in-depth EC50/IC50 determinations. We can also provide custom GPCR screening assay based on your preliminary data, i.e., GPCR agonist screening, GPCR antagonist screening, GPCR allosteric modulator screening, GPCR inverse agonist screening, etc. We will make our greatest efforts to accelerate your GPCR research, including hit identification, selectivity profiling or structure-activity relationship (SAR) optimization, etc. We will include necessary controls in each assay and provide a comprehensive report upon project completion. We can also adjust our screening platform flexibly based on your requirements.


Our package GPCR screening service includes:


  Scalable imaging, detection instruments and liquid handling systems for radiometric, fluorescence and luminescence detection.

  Optimized cell-based assay platforms.

  Developed GPCR cell lines.



  Professional and high-quality service.

  Thoroughly validated high-throughput drug screening model

  Short turn-around time

  Best price in the market

Our available GPCR targets and the functional/binding assays we have developed so far are listed in the attached instruction manual.


Please contact us for more details of our preclinical GPCR screening service. Our experts will provide you an optimal solution for your GPCR screening project and trouble-shooting for you throughout the whole process.

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