Fluorogenic phospholipid substrate to detect lysophospholipase D/autotaxin activity

CG Ferguson, CS Bigman, RD Richardson… - Organic …, 2006 - ACS Publications
CG Ferguson, CS Bigman, RD Richardson, LA van Meeteren, WH Moolenaar, GD Prestwich
Organic letters, 2006ACS Publications
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.
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.
ACS Publications