Article
Hits of a high-throughput screen identify the hydrophobic pocket of autotaxin/lysophospholipase D as an inhibitory surface.
Molecular pharmacology - 1 Sept 2013
Fells James I, Lee Sue Chin, Fujiwara Yuko, Norman Derek D, Lim Keng Gat, Tsukahara Ryoko, Liu Jianxiong, Patil Renukadevi, Miller Duane D, Kirby R Jason, Nelson Sandra, Seibel William, Papoian Ruben, Parrill Abby L, Baker Daniel L, Bittman Robert, Tigyi Gabor
Abstract excerpt
Autotaxin (ATX), a lysophospholipase D, plays an important role in cancer invasion, metastasis, tumor progression, tumorigenesis, neuropathic pain, fibrotic diseases, cholestatic pruritus, lymphocyte homing, and thrombotic diseases by producing the lipid mediator lysophosphatidic acid (LPA). A high-throughput screen of ATX inhibition using the lysophosphatidylcholine-like substrate fluorogenic substrate 3 (FS-3)...
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