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Fluorogenic phospholipid substrate to detect lysophospholipase D/autotaxin activity.


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.

SUBMITTER: Ferguson CG 

PROVIDER: S-EPMC2528860 | biostudies-literature | 2006 May

REPOSITORIES: biostudies-literature

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Fluorogenic phospholipid substrate to detect lysophospholipase D/autotaxin activity.

Ferguson Colin G CG   Bigman Cleve S CS   Richardson Robyn D RD   van Meeteren Laurens A LA   Moolenaar Wouter H WH   Prestwich Glenn D GD  

Organic letters 20060501 10


[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. ...[more]

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