Issue 6, 2015
From the journal:

MedChemComm

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

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

* Corresponding authors

a WestCHEM, Department of Pure and Applied Chemistry, University of Strathclyde, Thomas Graham Building, 295 Cathedral Street, Glasgow, UK
E-mail: craig.jamieson@strath.ac.uk, allan.watson.100@strath.ac.uk

b Strathclyde Institute of Pharmacy and Biomolecular Science, University of Strathclyde, John Arbuthnott Building (Hamnett Wing), 161 Cathedral Street, Glasgow, UK

c Fibrosis DPU, GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, UK

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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DOI
https://doi.org/10.1039/C5MD00081E
Article type
Concise Article
Submitted
23 Feb 2015
Accepted
07 May 2015
First published
08 May 2015

Med. Chem. Commun., 2015,6, 1149-1155

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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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