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.
Diana Castagna  1 ,  David C Budd  2 ,  Simon J F Macdonald  2 ,  Craig Jamieson  1 ,  Allan J B Watson  1
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.