G-protein-coupled receptors (GPCRs) play a vital role in biology and medicine, but only a small number of them have drugs that target them. Tanso Biosciences has developed a versatile and sensitive assay method to overcome the challenges in GPCR research and promote drug development (Patent Publication Number WO/2020/026979). This innovative platform enables the company to engage in drug discovery for orphan GPCRs and offer 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 550 human and mouse 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 294 human GPCRs and >250 mouse GPCRs.
FlexPanel48 is reasonable small-scale panels with 48 receptors and consists of custom panels and therapeutic area panels.
One can choose any 48 receptors from >550 human/mouse 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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We hear about the study outline and propose experiments. A non-disclosure agreement is optional.
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You place an order, ship your compounds to our lab, and pay the fee via bank transfer or by credit card.
The turnaround time can be as short as two weeks, depending on the study scale and design and the backlog of orders.
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