Autotaxin (ATX, ENPP2) is a serine protease and part of the Ectonucleotide Pyrophosphatase and Phosphodiesterase family. ATX hydrolyzes lysophosphatidylcholine (LPC) to lysophosphatidic acid (LPA) in the blood. LPA then signals through lysophospholipid receptors to stimulate cell migration, proliferation and survival of a number of cells. High levels of ATX have been found in non-malignant inflamed tissues as well as in various cancers making it an enticing biological target for treating cancers, and disease pathologies that involve LPA-signaling. <br/>To rapidly identify fragments leads for developing potent ATX inhibitors we took advantage of boronic acids which are known to bind tightly to the catalytic triad of serine proteases. We screened against a boronic acid library along with our in house fragment library. We compared the hit rates of this target library to a standard fragment library and demonstrate the utility of this targeted-library methodology.<br/>

Targeted screening library for the identification of ATX fragment hits

251st National Meeting (2016)

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