EphB4 Tyrosine Kinase Cancer

The protein kinase EphB4 (erythropoietin producing human hepatocellular carcinoma receptor tyrosine kinase B4) is a highly attractive angiogenic target involved in many types of cancer [109]. It seems to be rather recalcitrant to inhibition because, despite its potential therapeutic importance, very few inhibitors have been reported in the literature up to date. 

We have developed and applied the ALTA (anchor-based library tailoring) approach to identify ATP-competitive inhibitors of EphB4 [99] (Eigure 17.5). ALTA is an automatic fragment-based procedure for focusing libraries of compounds. First, molecular fragments are docked and prioritized (i.e., anchors are selected based on a 

The surface of WNV NS2B-NS3 pro is colored by electrostatic potential with red and blue for negative and positive potentials, respectively. The figure was prepared using PyMOL (Delano Scientific, San Carlos, CA) and the APBS program [107] was used for calculation of the electrostatic surface. 

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