In Silico Identification of Novel Orthosteric Inhibitors of Sphingosine Kinase 1 (SK1)

Background: Sphingosine kinase 1 (SK1) overexpression and elevated sphingosine-1-phosphate (S1P) levels have been correlated with many disease states from cancer to inflammatory diseases to diabetes. Even though SK1 inhibitors are of consideberable interest as effective chemotherapeutic agents, poor potency, lack of selectivity and poor pharmacokinetic properties have been major problems in the first generation SK1 inhibitors.