Fluorogenic Phospholipid Substrate to Detect Lysophospholipase D/Autotaxin Activity

Fluorogenic Phospholipid Substrate to Detect Lysophospholipase D/Autotaxin Activity

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 f...

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Veröffentlicht in:Organic letters 2006-05, Vol.8 (10), p.2023-2026
Hauptverfasser: Ferguson, Colin G, Bigman, Cleve S, Richardson, Robyn D, van Meeteren, Laurens A, Moolenaar, Wouter H, Prestwich, Glenn D
Format: Artikel
Sprache:eng
Schlagworte:
Fluorescent Dyes - chemical synthesis
Fluorescent Dyes - metabolism
Lysophospholipids
Molecular Structure
Multienzyme Complexes - analysis
Multienzyme Complexes - genetics
Multienzyme Complexes - metabolism
Phosphodiesterase I - analysis
Phosphodiesterase I - genetics
Phosphodiesterase I - metabolism
Phospholipids - chemistry
Phospholipids - metabolism
Phosphoric Diester Hydrolases - analysis
Phosphoric Diester Hydrolases - metabolism
Pyrophosphatases - analysis
Pyrophosphatases - genetics
Pyrophosphatases - metabolism
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Zusammenfassung: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.
ISSN:1523-7060
1523-7052
DOI:10.1021/ol060414i