Fluorogenic phospholipid substrate to detect lysophospholipase D/autotaxin activity.
[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.
Ferguson
Colin G
CG
Echelon Biosciences Inc., Salt Lake City, Utah 84108, USA. cferguson@echelon-inc.com
Bigman
Cleve S
CS
Richardson
Robyn D
RD
van Meeteren
Laurens A
LA
Moolenaar
Wouter H
WH
Prestwich
Glenn D
GD