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.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Fluorescent Dyes / chemical synthesis*
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Fluorescent Dyes / metabolism
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Lysophospholipids
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Molecular Structure
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Multienzyme Complexes / analysis*
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Multienzyme Complexes / genetics
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Multienzyme Complexes / metabolism
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Phosphodiesterase I / analysis*
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Phosphodiesterase I / genetics
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Phosphodiesterase I / metabolism
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Phospholipids / chemistry
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Phospholipids / metabolism
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Phosphoric Diester Hydrolases / analysis*
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Phosphoric Diester Hydrolases / metabolism
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Pyrophosphatases / analysis*
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Pyrophosphatases / genetics
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Pyrophosphatases / metabolism
Substances
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Fluorescent Dyes
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Lysophospholipids
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Multienzyme Complexes
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Phospholipids
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Phosphoric Diester Hydrolases
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Phosphodiesterase I
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alkylglycerophosphoethanolamine phosphodiesterase
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Pyrophosphatases
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lysophosphatidic acid