Issues

Activation of the receptor tyrosine kinase Met and its ligand, hepatocyte growth factor/scatter factor, leads to dissociation of cells from the primary tumor, causing metastasis. Therefore, both proteins and their interaction are major metastasis targets. Using a fragment-based approach, small lead compounds were identified that target this protein–protein interface leading to a reduction in phosphorylation of downstream effectors such as Akt, inhibition of cell migration, and prevention of tumor formation in cell-based assays. For details, see the article by Winter and colleagues on page 3.