PARIS ¿ The Belgian functional genomics company Galapagos Genomics NV entered a collaboration with another Belgian biotechnology company, Euroscreen SA, to identify activators (or ligands) of G protein-coupled receptors for which no ligands are currently known.

Euroscreen is a specialist in research on GPCRs, which are known to be potential therapeutic targets in many disease areas, as its vice president, research and development, Richard White, explained: ¿GPCRs mediate about 90 percent of the signal transduction through the cell membrane and are therefore very attractive drug targets for the pharmaceutical industry. GPCRs are the target for about one-third of the 100 leading pharmaceutical products.¿

Galapagos, of Mechelen, will use its PhenoSelect gene expression platform in conjunction with Brussels-based Euroscreen¿s AequoScreen cell-based assay technology to identify and characterize the natural ligands for a number of orphan GPCRs. Specifically, Galapagos will supply Euroscreen with an arrayed collection of secreted proteins and peptides from human cells transduced with genes from its PhenoSelect library, which comprises tens of thousands of human genes. Euroscreen will then screen that peptide library for ligands that activate orphan GPCRs using its cellular assays.

The companies said their approach is unique insofar as any ligands identified in the screening process can be immediately traced back to the corresponding gene in the PhenoSelect library, greatly facilitating the further characterization of the ligand. Galapagos CEO Onno van de Stolpe said its PhenoSelect library is ¿well suited to produce large numbers of secreted proteins and peptides that are potential ligands of orphan GPCRs.¿

Galapagos¿ vice president, business development, Dirk Pollet, said the ¿combination of Galapagos¿ peptide library and Euroscreen¿s assay technology will make it easy to identify and characterize ligands of orphan receptors discovered in the screening process.¿ He added that the results of their research would be shared equally between the two companies, but he was unable to give any indication of the kind of pathology for which drug targets might be identified, since it is orphan GPCRs that are being targeted and GPCRs are involved in many different disease processes.

Pollet said the two companies planned to license out the intellectual property generated by the research, but that it was not possible at this stage to say how far they would go in validating and optimizing therapeutic targets before licensing them out. The agreement is for an initial term of one and a half years, he said, adding that it could be extended beyond that if the results warrant it. But Pollet refused to discuss the financial arrangements of the collaboration.

Galapagos is due to close a private funding round before the end of this year in which it expects to raise EUR20 million (US$18 million) from a number of venture capital funds, giving it a greater degree of autonomy. At present, it is a joint subsidiary of the Dutch company Crucell NV, of Leiden, and the Belgian firm Tibotec-Virco NV, of Mechelen, and its technology is based on Crucell¿s PER.C6 human cell line expression platform, for which it has an exclusive license in functional genomics applications.

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