Fluorogenic Phospholipid Substrate to Detect Lysophospholipase D/Autotaxin Activity

Colin G. Ferguson(University of Utah), Cleve S. Bigman(Echelon Biosciences), Robyn D. Richardson(University of Utah), Laurens A. van Meeteren(Echelon Biosciences), Wouter H. Moolenaar(University of Utah), Glenn D. Prestwich(Echelon Biosciences)
Organic Letters
April 13, 2006
Cited by 109Open Access
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Abstract

[reaction: see text] Lysophospholipase D (lysoPLD), also known as autotaxin (ATX), is an important source of the potent mitogen lysophosphatidic acid (LPA). Two fluorogenic substrate analogues for lysoPLD were synthesized in nine steps from (S)-PMB-glycerol. The substrates (FS-2 and FS-3) show significant increases in fluorescence when treated with recombinant ATX and have potential applications in screening for this emerging drug target.


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