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)

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.
LanguageEnglish
Pages1149-1155
Number of pages6
JournalMedChemComm
Volume2015
Issue number6
Early online date8 May 2015
DOIs
Publication statusPublished - 1 Jun 2015

Fingerprint

Lysophosphatidic Acid Receptors
Lead compounds
Screening
Blood
Solubility
Enzyme Inhibitors
Enzymes
lysophosphatidic acid

Keywords

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

Cite this

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
Castagna, Diana ; Duffy, Emma L. ; Semaan, Dima ; Young, Louise C. ; Pritchard, John M. ; Macdonald, Simon J. F. ; Budd, David C. ; Jamieson, Craig ; Watson, Allan J. B. / Identification of a novel class of autotaxin inhibitors through cross-screening. In: MedChemComm. 2015 ; Vol. 2015, No. 6. pp. 1149-1155.
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Castagna, D, Duffy, EL, Semaan, D, Young, LC, Pritchard, JM, Macdonald, SJF, Budd, DC, Jamieson, C & Watson, AJB 2015, 'Identification of a novel class of autotaxin inhibitors through cross-screening' MedChemComm, vol. 2015, no. 6, pp. 1149-1155. https://doi.org/10.1039/C5MD00081E

Identification of a novel class of autotaxin inhibitors through cross-screening. / Castagna, Diana; Duffy, Emma L.; Semaan, Dima ; Young, Louise C.; Pritchard, John M.; Macdonald, Simon J. F.; Budd, David C.; Jamieson, Craig; Watson, Allan J. B.

In: MedChemComm, Vol. 2015, No. 6, 01.06.2015, p. 1149-1155.

Research output: Contribution to journalArticle

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AU - Macdonald, Simon J. F.

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KW - drug discovery

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Castagna D, Duffy EL, Semaan D, Young LC, Pritchard JM, Macdonald SJF et al. Identification of a novel class of autotaxin inhibitors through cross-screening. MedChemComm. 2015 Jun 1;2015(6):1149-1155. https://doi.org/10.1039/C5MD00081E