Autotaxin (ATX) Substrate FS-3
- The fluorogenic Autotaxin (ATX) substrate FS-3 is a doubly labeled analog of LPC wherein the fluorophore is quenched through intramolecular energy transfer.
Hydrolysis of the substrate produces an increase in fluorescence.
- Autotaxin, which has lysophospholipase D (lysoPLD) activity, cleaves choline from lysophosphatidylcholine forming lysophosphatidic acid (LPA), a potent mitogen that has been implicated in the
pathophysiology of ovarian cancer. LysoPLD/ATX has been demonstrated to increase cell motility, neovascularization, proliferation, and aggressiveness of tumors and is upregulated in
numerous cancer lineages (non-small cell lung, glioma, mammary carcinoma, renal cell carcinoma, hepatocellular carcinoma).
In addition, dysregulation of the ATX/LPA pathway is central to the pathophysiology of idiopathic pulmonary fibrosis, rheumatoid arthritis, and other inflammatory diseases.
Modulation of ATX activity through small molecules is a currently underexplored target, but one with high potential for novel cancer and anti-inflammatory therapeutics.
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