A reliable technology to develop the next generation of GPCR targeted medicines

07/09/2015 - 4 minutes

You must have heard of GPCRs, or more specifically G protein-coupled receptors. Doesn’t ring a bell? You know, it’s this large protein family of receptors that sense molecules outside the cell and trigger an inside signal. A technology called IP-One could give a large advantage to scientists working on GPCR-targeted drugs. We had the opportunity to attend a webinar dedicated to the GPCR drug discovery research in which scientists from academia and biotech companies exchanged ideas around this promising field.

As you may remember, there are several GPCR classes, coupled to different G proteins, which activation is triggered by ligand binding. In the case of Gq coupled receptors, this leads to the activation of Phospholipase C. The phospholipase cleaves PIP2 into IP3 then IP2 and finally IP1. In our case, it’s the latter that’s interesting.

IP1 pathway Gq_IP1-Gq

Based on this pathway, Cisbio Bioassays has developed IP-One, a bioassay kit that specifically measures IP1 levels in cells. By using LiCl in the process, this technology avoids the degradation of IP1,

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