DKK1 and osteosarcoma: Again, researchers at Wyeth looking for Wnt agonists, useda HTS and ligand-based optimization approach to discover WAY-262611(23), a small molecule inhibitor of DKK1 as measuredby a TCF-luciferase reporter assay in an osteosarcoma cell line treatedwith Wnt3a and DKK1 conditioned media (EC50 0.63 μM).WAY-262611 was optimized to be highly selective over GSK-3β,have favorable pharmacokinetic (PK) properties, and display efficacyin an in vivo rat model of bone formation when dosedorally.85