Bioorganic & medicinal chemistry letters

Aromatic phosphonates inhibit the lysophospholipase D activity of autotaxin

G Jiang, D Madan, GD Prestwich

Index: Jiang, Guowei; Madan, Damian; Prestwich, Glenn D. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 17 p. 5098 - 5101

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Citation Number: 31

Abstract

Autotaxin (ATX) is an attractive target for the anticancer therapeutics that inhibits angiogenesis, invasion and migration. ATX is an extracellular lysophospholipase D that hydrolyzes lysophosphatidylcholine to form the bioactive lipid lysophosphatidic acid. The aromatic phosphonate S32826 was the first described nanomolar inhibitor of ATX. However, the tridecylamide substituent on aromatic ring contributed to its poor solubility and ...