Autotaxin in the crosshairs: taking aim at cancer and other inflammatory conditions.

摘要: Autotaxin is a secreted enzyme that produces most of the extracellular lysophosphatidate from lysophosphatidylcholine, abundant phospholipid in blood plasma. Lysophosphatidate mediates many physiological and pathological processes by signaling through at least six G-protein coupled receptors to promote cell survival, proliferation migration. The autotaxin/lysophosphatidate axis involved wound healing tissue remodeling, it drives chronic inflammatory conditions fibrosis colitis, asthma cancer. In cancer, promotes resistance chemotherapy radiotherapy, increases both angiogenesis metastasis. Research into autotaxin inhibitors accelerating, as primary adjuvant therapy. Historically, had poor bioavailability profiles thus limited efficacy vivo. This situation now changing, especially since recent crystal structure enabling rational inhibitor design. this review, we will summarize current knowledge on autotaxin-mediated disease including discuss advancements development autotaxin-targeting strategies. We also provide new insights an mediator tumor microenvironment cancer progression therapy resistance.