Design, synthesis, biochemical studies, cellular characterization, and structure-based computational studies of small molecules targeting the urokinase receptor

F Wang, WE Knabe, L Li, I Jo, T Mani, H Roehm…

Index: Wang, Fang; Eric Knabe; Li, Liwei; Jo, Inha; Mani, Timmy; Roehm, Hartmut; Oh, Kyungsoo; Li, Jing; Khanna, May; Meroueh, Samy O. Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 15 p. 4760 - 4773

Full Text: HTML

Citation Number: 15

Abstract

The urokinase receptor (uPAR) serves as a docking site to the serine protease urokinase- type plasminogen activator (uPA) to promote extracellular matrix (ECM) degradation and tumor invasion and metastasis. Previously, we had reported a small molecule inhibitor of the uPAR· uPA interaction that emerged from structure-based virtual screening. Here, we measure the affinity of a large number of derivatives from commercial sources. Synthesis ...