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

Diana Castagna, Emma L. Duffy, Dima Semaan, Louise C. Young, John M. Pritchard, Simon J. F. Macdonald, David C. Budd, Craig Jamieson, Allan J. B. Watson

Research output: Contribution to journalArticle

6 Citations (Scopus)
64 Downloads (Pure)

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.
Original languageEnglish
Pages (from-to)1149-1155
Number of pages6
JournalMedChemComm
Volume2015
Issue number6
Early online date8 May 2015
DOIs
Publication statusPublished - 1 Jun 2015

Keywords

  • autotaxin
  • drug discovery
  • lysophosphatidic acid
  • lead compound
  • inhibitor

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    Castagna, D., Duffy, E. L., Semaan, D., Young, L. C., Pritchard, J. M., Macdonald, S. J. F., ... Watson, A. J. B. (2015). Identification of a novel class of autotaxin inhibitors through cross-screening. MedChemComm, 2015(6), 1149-1155. https://doi.org/10.1039/C5MD00081E