Targeting Chemerin Receptor CMKLR1 in Multiple Sclerosis

Abstract

Therapies that target leukocyte trafficking pathways can reduce disease activity and improve clinical outcomes in multiple sclerosis (MS). Experimental autoimmune encephalomyelitis (EAE) is a widely studied animal model that shares many clinical and histological features with human MS. Chemokine-like receptor-1 (CMKLR1) is a chemoattractant receptor that is expressed by key effector cells in EAE and MS, including macrophages, subsets of dendritic cells, natural killer cells and microglia. CMKLR1-deficient mice develop less severe clinical and histological EAE than wild-type mice. In this study, we identified alphanaphthoyl ethyltrimethylammonium iodide (alpha-NETA) as a selective CMKLR1 small molecule antagonist that inhibits chemerin-triggered CMKLR1+ cell migration. Prophylactic dosing with alpha-NETA significantly delayed the onset of EAE induced in C57BL/6 mice. In addition, alpha-NETA treatment significantly inhibited accumulation of inflammatory leukocytes within the CNS. This study provides additional proof-of-concept data that targeting CMKLR1:chemerin interactions may be beneficial in preventing or treating MS.

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Document Details

Document Type
Technical Report
Publication Date
Sep 01, 2012
Accession Number
ADA575594

Entities

People

  • Brian Zabel

Organizations

  • Palo Alto Veterans Institute for Research

Tags

DTIC Thesaurus Topics

  • Biomedical And Dental Materials
  • Blood
  • Blood Proteins
  • Cell Physiological Processes
  • Cells
  • Cellular Structures
  • Chemical Synthesis
  • Chemistry
  • Demyelinating Diseases
  • Diseases And Disorders
  • Dosage Forms
  • Liquid Chromatography
  • Lymphocytes
  • Organic Chemistry
  • Polymer Chemistry
  • Polymeric Films
  • Small Molecules

Fields of Study

  • Biology
  • Medicine

Readers

  • Immunology and Pathology
  • Oncology (Cancer Research).