On September 1, 2011 CRT reported small molecule inhibitors of Autotaxin (ATX) have been discovered using an HTS approach and are currently undergoing lead optimisation (Press release, Cancer Research Technology, DEC 15, 2011, View Source [SID1234523522]). ATX cleaves choline from lysophosphatidylcholine (LPC) forming lysophosphatidic acid (LPA), a potent mitogen that has been implicated in the pathophysiology of cancer. ATX has been demonstrated to increase cell motility, neovascularization, proliferation and aggressiveness of tumours. It is upregulated in numerous tumour lineages (breast, glioblastoma, ovarian and prostate cancer).
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