Jump to main content
Jump to site search

Issue 6, 2015
Previous Article Next Article

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

Author affiliations

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 LPA1antagonists led us to the discovery of three novel series of inhibitors of the ectoenzyme autotaxin (ATX), responsible for LPA production in blood, with potencies in the range of 1–4 μM together with good (>100 μg mL−1) solubility.

Graphical abstract: Identification of a novel class of autotaxin inhibitors through cross-screening

Back to tab navigation

Supplementary files

Publication details

The article was received on 23 Feb 2015, accepted on 07 May 2015 and first published on 08 May 2015


Article type: Concise Article
DOI: 10.1039/C5MD00081E
Author version available: Download Author version (PDF)
Citation: Med. Chem. Commun., 2015,6, 1149-1155
  •   Request permissions

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

    D. Castagna, E. L. Duffy, D. Semaan, L. C. Young, J. M. Pritchard, S. J. F. Macdonald, D. C. Budd, C. Jamieson and A. J. B. Watson, Med. Chem. Commun., 2015, 6, 1149
    DOI: 10.1039/C5MD00081E

Search articles by author

Spotlight

Advertisements