Fluorogenic Phospholipid Substrate to
Detect Lysophospholipase D/Autotaxin
Activity
Colin G. Ferguson,*Cleve S. Bigman,Robyn D. Richardson,Laurens A. van Meeteren,Wouter H. Moolenaar, andGlenn D. Prestwich
Echelon Biosciences Inc., 675 Arapeen Drive 302, Salt Lake City, Utah 84108,
The Netherlands Cancer Institute, Plesmanlaan 121, 1066 CX Amsterdam,
The Netherlands, and Department of Medicinal Chemistry, University of Utah,
Salt Lake City, Utah 84108
cferguson@echelon-inc.com
Received February 16, 2006
Abstract:
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.
