Identification of a novel class of autotaxin inhibitors through cross-screening

Castagna, Diana and Duffy, Emma L. and Semaan, Dima and Young, Louise C. and Pritchard, John M. and Macdonald, Simon J. F. and Budd, David C. and Jamieson, Craig and Watson, Allan J. B. (2015) Identification of a novel class of autotaxin inhibitors through cross-screening. MedChemComm, 2015 (6). pp. 1149-1155. ISSN 2040-2503

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    Abstract

    Three novel series were generated in order to mimic the pharmacophoric features displayed by lead compound AM095, a Lysophosphatidic acid (LPA1) receptor antagonist. Biological evaluation of this array of putative LPA1 antagonists led us to the discovery of three novel series of inhibitors of the ecto-enzyme Autotaxin (ATX), responsible for LPA production in blood, with potencies in the range 1 – 4 μM accompanied with good (> 100 μg/mL) solubility.

    Creators(s): Castagna, Diana ORCID logoORCID: https://orcid.org/0000-0003-2315-8073, Duffy, Emma L. ORCID logoORCID: https://orcid.org/0000-0002-0502-7216, Semaan, Dima, Young, Louise C., Pritchard, John M., Macdonald, Simon J. F., Budd, David C., Jamieson, Craig ORCID logoORCID: https://orcid.org/0000-0002-6567-8272 and Watson, Allan J. B.;
    Item type:Article
    ID code:53196
    Keywords:autotaxin, drug discovery, lysophosphatidic acid, lead compound, inhibitor, Chemistry, Pharmacy and materia medica, Chemistry(all), Biochemistry, Genetics and Molecular Biology(all)
    Subjects:Science > Chemistry
    Medicine > Pharmacy and materia medica
    Department:Faculty of Science > Pure and Applied Chemistry
    Faculty of Science > Strathclyde Institute of Pharmacy and Biomedical Sciences
    Depositing user: Pure Administrator
    Date deposited:03 Jun 2015 04:01
    Last modified:20 Jan 2021 22:09
    Related URLs:
    URI:https://strathprints.strath.ac.uk/id/eprint/53196
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