G-protein-coupled receptors (GPCRs) are crucial in biology and medicine, but only a fraction of them have drugs to target them. One of the hardest barriers to GPCR research has been the lack of satisfactory assays.
To overcome this challenge and promote drug development, scientists at Tanso Biosciences have innovated a versatile and sensitive assay method. Based on this platform, we engage in drug discovery for orphan GPCRs and provide contract assay services.
Comprehensive Orphan GPCR Drug Discovery Project
Research on GPCRs, especially orphan GPCRs, has been hindered by a lack of adequate assays. To overcome the barriers of GPCR drug discovery, we have innovated a high-performance functional assay. It works excellently for all receptors coupled with any of the major Gα proteins including Gq, Gs, Gi/o, and G12/13.
We have taken advantage of our proprietary assay and embarked on orphan GPCR drug discovery, broadly targeting ~100 of them. As a first step, compound library screening is ongoing for their agonists, with a priority on disease-associated receptors.
We have identified agonists for six orphan GPCRs, namely, GPR39, GPR55, GPR65, GPR68, GPR132, and P2RY10, and characterized their concentration-dependent potency.
Agonists identified in the previous step will be further characterized. They will also play crucial roles in screening for orphan GPCR antagonists.
Tanso Biosciences provides super-sensitive and reliable functional assays for more than 300 human G-protein-coupled receptors (GPCRs) to expand frontiers, accelerate drug discovery, and reduce R&D risks.
Besides assays illustrated here, we can arrange various tests, such as allosteric modulation and GPCR homologs in other species than human.
Large-Scale Comprehensive Panels
Our large-scale panel assays allow comprehensive screening for up to 200 non-orphan GPCRs and 94 orphan GPCRs. Panel Assay
FlexPanel48 is reasonable small-scale panels with 48 receptors and consists of custom panels and therapeutic area panels. Panel Assay
One can choose any 48 receptors from 200 non-orphan GPCRs and 94 orphan GPCRs.
Therapeutic Area Panels
Panels of 48 GPCRs associated with one of 13 therapeutic areas.
TAK-875, a Phase 3 antidiabetic, was screened in the agonist mode in the FlexPanel48 Endocrinology/Metabolism Panel. The agent selectively activated free fatty acid receptor 1 (FFAR1).
We analyze concentration dependence n various assay modes (agonist, inverse agonist, antagonist, PAM, NAM) and are flexible in study design, such as the numbers of replicates and concentrations.
TAK-875, a Phase 3 antidiabetic, was shown to activate FFAR1 in a concentration-dependent manner.
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Service Flow Chart
Request for Quotation
Tell us about the types of tests you need, the number of compounds, the receptors of interest, and other preferences. A non-disclosure agreement is optional.
A non-disclosure agreement is optional.
The client ships test compounds to our laboratory. We usually perform assays and write a report in three weeks from the receipt of the compounds.
Receipt of the Report
We provide the report and raw data for the client via email or a cloud service.