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Autotaxin inhibitors: a perspective on initial medicinal chemistry efforts

Abby L Parrill1, Daniel L Baker

  • 1The University of Memphis, Department of Chemistry, Memphis, TN 38152, USA. aparrill@memphis.edu

Expert Opinion on Therapeutic Patents
|November 5, 2010
PubMed

Insights

Autotaxin (ATX) inhibitors show promise for treating diseases like cancer and Alzheimer's. Further in vivo studies are crucial for translating these ATX inhibitors into clinical applications.

Area of Science:

  • Biochemistry
  • Enzymology
  • Drug Discovery

Background:

  • Autotaxin (ATX) is a lysophospholipase D enzyme implicated in various human diseases, including cancer, neuropathic pain, obesity, and Alzheimer's disease.
  • While ATX was identified in 1992, its role in bioactive lipid metabolism was established in 2002.
  • Significant progress has been made in identifying ATX inhibitors, including metal chelators, product analogs, and small non-lipid molecules.

Purpose of the Study:

  • To review the development and characterization of autotaxin (ATX) inhibitors.
  • To highlight the need for expanded in vivo characterization of ATX inhibitors to facilitate clinical translation.

Main Methods:

  • Review of existing literature on autotaxin (ATX) enzyme and its inhibitors.
  • Analysis of characterization methods for ATX inhibitors, focusing on in vitro versus in vivo studies.

Main Results:

  • Numerous ATX inhibitors have been identified using various chemical approaches.
  • The majority of characterized ATX inhibitors have been studied using recombinant purified enzyme in vitro.
  • There is a limited number of studies investigating ATX inhibitors in more complex biological systems or in vivo.

Conclusions:

  • The development of effective ATX inhibitors has advanced significantly.
  • Translating ATX inhibitors into clinical use necessitates comprehensive in vivo characterization beyond current in vitro assessments.
  • Further research focusing on in vivo efficacy and safety is essential for the clinical application of ATX inhibitors.

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