Galapagos Genomics and fellow Belgian company Euroscreen have enteredinto a collaboration to identify activators of G-protein coupled receptors for which no ligands are known. The alliance, for which no financial details have been disclosed, will combine the former's PhenoSelect expression platform with Euroscreen's AequoScreen cell-based assay technology.
Under the terms of the agreement, Galapagos will supply Euroscreen with an arrayed collection of secreted proteins and peptides from human cells infected with its PhenoSelect library, that includes tens of thousands of human genes, which will be screened for ligands that activate orphan GPCRs. The companies said that this approach is unique in that the ligands identified in the screen can be immediately traced back to the corresponding gene in the PhenoSelect library, "significantly facilitating the further characterization of the ligand." The firms then plan to out-license the validated ligands to pharmaceutical and biotechnology companies for drug discovery programs.
Euroscreen's vice president of R&D, Richard White, said that GPCRs mediate about 90% of the signal transduction through the cell membrane "and are therefore very attractive drug targets for the pharmaceutical industry." He claimed that GPCRs are the target for about one-third of the leading 100 pharmaceutical products, naming such drugs as Schering-Plough's Claritin (loratadine), Merck & Co's Cozaar (losartan), Eli Lilly's Prozac (fluoxetine) and GlaxoSmithKline's Zantac (ranitidine) and Imitrex (sumatriptan).
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