The Classified Progression in Binding Modes of Autotaxin (ATX) Inhibitors

Hongrui Lei¹, Fang Jia¹, Ming Guo¹, Dajun Zhang²* and Xin Zhai¹*²

Received: July 25, 2018;   Published: July 30, 2018

DOI: 10.26717/BJSTR.2018.07.001496

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Abstract

Autotaxin (ATX) is a secreted enzyme which hydrolyzes lysophosphatidylcholine (LPC) to lysophosphatidic acid (LPA) and choline. The ATX-LPA axis has attracted increasing interest recently for both ATX and LPA are involved in various pathological conditions such as tumor progression and metastasis, fibrotic diseases, arthritis, autoimmune diseases and obesity. Thus, great efforts have been devoted in identifying synthetic ATX inhibitors as new agents for treating various diseases including cancer and fibrotic diseases. Herein, this mini review mainly focused on the binding modes of the reported ATX inhibitors and their indications correspondingly.

Keywords: ATX; ATX-LPA Axis; ATX Inhibitors; Binding Mode; Indications

Keywords: ENPPs: Ectonucleotide Pyrophosphatases/Phosphodiesterases; lysoPLD: Lysophospholipase D; SMB: Somatomedin B; PDE: Phosphodiesterase; NUC: Nuclease; Thr210: Threonine Residue; IPF: Idiopathic Pulmonary Fibrosis

Abstract | Introduction | Binding Modes of Reported ATX Inhibitors | The Main Indications of ATX Inhibitors | Perspective | Acknowledgments | References |