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Fibroblast growth factor receptor (FGFR)

Two separate studies identified an allosteric inhibitor of FGFR that could help treat cancer. In the first study, NMR, molecular dynamics and X-ray crystallography analysis found that the small molecule SSR128129E (SSR) bound the extracellular D3 domain at a site distinct from FGFR ligand binding and acted as an allosteric inhibitor by altering FGF binding site conformation. In the second study, oral dosing of SSR decreased tumor size, tumor invasiveness and metastasis in mouse models for cancer compared with oral dosing of vehicle. In mouse models for pancreatic and colorectal cancers, SSR plus a VEGF receptor 2 (KDR/Flk-1; VEGFR-2) inhibitor decreased tumor growth better than either treatment alone.
Next steps include clinical testing of SSR analogs.
At least six selective FGFR inhibitors are in Phase II testing or earlier to treat various cancers (see FGFR allosteric inhibition, page 4).

SciBX 6(17); doi:10.1038/scibx.2013.411
Published online May 2, 2013

SSR and related compounds from both studies patented by Sanofi; Sanofi and the Flanders Institute for Biotechnology (VIB) have a joint patent covering methods used; unavailable for licensing

Herbert, C. et al. Cancer Cell;
published online April 15, 2013;
Contact: Françoise Bono, Sanofi Research and Development, Toulouse, France
Contact: Harald Schwalbe, Goethe University Frankfurt, Frankfurt, Germany
Contact: Francesco Luigi Gervasio, Spanish National Cancer Research Centre (CNIO), Madrid, Spain

Bono, F. et al. Cancer Cell;
published online April 15, 2013;
Contact: Peter Carmeliet, Catholic University Leuven, Leuven, Belgium