A metabolically-stabilized phosphonate analog of lysophosphatidic acid attenuates collagen-induced arthritis

PLoS One. 2013 Jul 29;8(7):e70941. doi: 10.1371/journal.pone.0070941. Print 2013.

Abstract

Rheumatoid arthritis (RA) is a destructive arthropathy with systemic manifestations, characterized by chronic synovial inflammation. Under the influence of the pro-inflammatory milieu synovial fibroblasts (SFs), the main effector cells in disease pathogenesis become activated and hyperplastic while releasing a number of signals that include pro-inflammatory factors and tissue remodeling enzymes. Activated RA SFs in mouse or human arthritic joints express significant quantities of autotaxin (ATX), a lysophospholipase D responsible for the majority of lysophosphatidic acid (LPA) production in the serum and inflamed sites. Conditional genetic ablation of ATX from SFs resulted in attenuation of disease symptoms in animal models, an effect attributed to diminished LPA signaling in the synovium, shown to activate SF effector functions. Here we show that administration of 1-bromo-3(S)-hydroxy-4-(palmitoyloxy)butyl-phosphonate (BrP-LPA), a metabolically stabilized analog of LPA and a dual function inhibitor of ATX and pan-antagonist of LPA receptors, attenuates collagen induced arthritis (CIA) development, thus validating the ATX/LPA axis as a novel therapeutic target in RA.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Arthritis, Experimental / chemically induced
  • Arthritis, Experimental / drug therapy
  • Arthritis, Experimental / metabolism*
  • Arthritis, Experimental / pathology
  • Arthritis, Rheumatoid / chemically induced
  • Arthritis, Rheumatoid / drug therapy
  • Arthritis, Rheumatoid / metabolism*
  • Arthritis, Rheumatoid / pathology
  • Collagen / adverse effects
  • Enzyme Activation / drug effects
  • Female
  • Hydrolysis / drug effects
  • Lysophosphatidylcholines / metabolism
  • Lysophospholipids / metabolism*
  • Lysophospholipids / pharmacology
  • Mice
  • Phosphoric Diester Hydrolases / metabolism
  • Substrate Specificity

Substances

  • Brp-LPA
  • Lysophosphatidylcholines
  • Lysophospholipids
  • Collagen
  • Phosphoric Diester Hydrolases
  • alkylglycerophosphoethanolamine phosphodiesterase

Grants and funding

This work was supported by the European Commission LSHG-CT-2005-005203 grant to VA. The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.