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Issue 6, 2015
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Identification of a novel class of autotaxin inhibitors through cross-screening

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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 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

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Submitted
23 Feb 2015
Accepted
07 May 2015
First published
08 May 2015

Med. Chem. Commun., 2015,6, 1149-1155
Article type
Concise Article
Author version available

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

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