Development of Autotaxin Inhibitors: An Overview of the Patent and Primary Literature

Diana Castagna; David C Budd; Simon J F Macdonald; Craig Jamieson; Allan J B Watson

doi:10.1021/acs.jmedchem.5b01599

Development of Autotaxin Inhibitors: An Overview of the Patent and Primary Literature

J Med Chem. 2016 Jun 23;59(12):5604-21. doi: 10.1021/acs.jmedchem.5b01599. Epub 2016 Jan 28.

Authors

Diana Castagna¹, David C Budd², Simon J F Macdonald², Craig Jamieson¹, Allan J B Watson¹

Affiliations

¹ WestCHEM, Department of Pure and Applied Chemistry, University of Strathclyde , Glasgow, G1 1XL, U.K.
² Medicines Research Centre, GlaxoSmithKline , Gunnel Wood Road, Stevenage, Hertfordshire, SG1 2NY, U.K.

PMID: 26745766
DOI: 10.1021/acs.jmedchem.5b01599

Abstract

The autotaxin-lysophophatidic acid (ATX-LPA) signaling pathway is implicated in a variety of human disease states including angiogenesis, autoimmune diseases, cancer, fibrotic diseases, inflammation, neurodegeneration, and neuropathic pain, among others. As a result, ATX-LPA has become of significant interest within both the industrial and the academic communities. This review aims to provide a concise overview of the development of novel ATX inhibitors, including the disclosure of the first ATX clinical trial data.

Publication types

Review
Research Support, Non-U.S. Gov't

MeSH terms

Benzoxazoles / chemistry
Benzoxazoles / pharmacology*
Boronic Acids / chemistry
Boronic Acids / pharmacology*
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology*
Humans
Models, Molecular
Molecular Structure
Phosphoric Diester Hydrolases / metabolism*
Structure-Activity Relationship

Substances

Benzoxazoles
Boronic Acids
Enzyme Inhibitors
benzoxazolone
Phosphoric Diester Hydrolases
alkylglycerophosphoethanolamine phosphodiesterase