Domain-CanadaDomain Therapeutics, a France- and Quebec-based biopharmaceutical company specialising in the research and development of new drug candidates that target G protein-coupled receptors (GPCRs), announces a collaboration agreement with Pfizer Inc. aimed at assessing the impact of mutations on different signalling pathways engaged by GPCRs.

Pfizer is interested in GPCRs with potential therapeutic relevance; Domain Therapeutics will use its proprietary bioSensAll technology to define signalling signatures for each of the wild-type and mutant receptors.

This collaboration aims to validate potential targets across a range of therapeutic indications by probing the structure-function relationships of various amino acid substitutions in each GPCR.

Pfizer will utilise the results of specific mutations on intracellular signalling to guide further investigations in disease-specific models.

“We are very pleased to have signed this collaboration with Pfizer for the profiling of mutant GPCRs using the bioSensAll platform. It is yet another example of the wide applications of the technology, from target validation through to drug discovery and development,” said Pascal Neuville, Chief Executive Officer of Domain Therapeutics.

“By building a better understanding of the signalling profile needed for efficacy, bioSensAll may reduce the attrition rate of early-stage drug development.”

Domain Therapeutics NA Inc., the Canadian affiliate of Domain Therapeutics, will use bioSensAll to characterise the basal activities and signalling profile of known ligands of wild type receptors. It will then compare these profiles with those of mutant GPCRs. These differential signalling signatures will be used to inform target validation for different therapeutic indications.

The bioSensAll technology allows for easier understanding of signalling pathways activated by each candidate molecule, thus predicting its pharmacological profile.

This approach makes it possible to choose at an early stage of drug development those molecules that have the required activity but do not present side effects or induce tolerance to treatment.

About G Protein-Coupled Receptors and Biosensor Technology 
G protein-coupled receptors (GPCRs) belong to the family of membrane receptors and constitute one of the main classes of therapeutic targets for many indications.

The binding of a hormone or a specific ligand to a receptor’s binding site activates one or several pathways for intracellular signalling.

This enables the cell to provide an adapted response to the change in its environment. The many drugs that target GPCRs represent about 40% of all treatments on the market, but only address 15% of GPCRs.

The bioSensAll platform was originally developed through a pharma and academic consortium in the Quebec region (CQDM).

A new and more powerful generation of the platform was recently developed by a team of researchers from the University of Montreal’s Institute for Research in Immunology and Cancer (IRIC), led by Prof. Michel Bouvier, and from McGill University, led by Prof. Stéphane Laporte.

Domain Therapeutics retains exclusive commercialisation of the technology.