Literature DB >> 16671772

Fluorogenic phospholipid substrate to detect lysophospholipase D/autotaxin activity.

Colin G Ferguson1, Cleve S Bigman, Robyn D Richardson, Laurens A van Meeteren, Wouter H Moolenaar, Glenn D Prestwich.   

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.

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Year:  2006        PMID： 16671772      PMCID： PMC2528860          DOI： 10.1021/ol060414i

Source DB:  PubMed          Journal:  Org Lett        ISSN： 1523-7052            Impact factor:   6.005


  28 in total

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7.  Fluorogenic phospholipids as head group-selective reporters of phospholipase A activity.

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Review 8.  Physiological and pathophysiological roles of lysophosphatidic acids produced by secretory lysophospholipase D in body fluids.

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Authors:  Wouter H Moolenaar
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10.  Autotaxin has lysophospholipase D activity leading to tumor cell growth and motility by lysophosphatidic acid production.

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  43 in total

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6.  Activity-Based DNA-Encoded Library Screening.

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Review 7.  Phosphatase-resistant analogues of lysophosphatidic acid: agonists promote healing, antagonists and autotaxin inhibitors treat cancer.

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8.  Identification of small-molecule inhibitors of autotaxin that inhibit melanoma cell migration and invasion.

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9.  Targeting melanoma growth and viability reveals dualistic functionality of the phosphonothionate analogue of carba cyclic phosphatidic acid.

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Review 10.  Autotaxin: structure-function and signaling.

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