Fatty acid-binding proteins: role in metabolic diseases and potential as drug targets

Nat Rev Drug Discov. 2008 Jun;7(6):489-503. doi: 10.1038/nrd2589.


Lipids are vital components of many biological processes and crucial in the pathogenesis of numerous common diseases, but the specific mechanisms coupling intracellular lipids to biological targets and signalling pathways are not well understood. This is particularly the case for cells burdened with high lipid storage, trafficking and signalling capacity such as adipocytes and macrophages. Here, we discuss the central role of lipid chaperones--the fatty acid-binding proteins (FABPs)--in lipid-mediated biological processes and systemic metabolic homeostasis through the regulation of diverse lipid signals, and highlight their therapeutic significance. Pharmacological agents that modify FABP function may provide tissue-specific or cell-type-specific control of lipid signalling pathways, inflammatory responses and metabolic regulation, potentially providing a new class of drugs for diseases such as obesity, diabetes and atherosclerosis.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Binding Sites
  • Fatty Acid-Binding Proteins / antagonists & inhibitors*
  • Fatty Acid-Binding Proteins / chemistry
  • Fatty Acid-Binding Proteins / genetics
  • Fatty Acid-Binding Proteins / physiology
  • Humans
  • Ligands
  • Lipid Metabolism / drug effects
  • Metabolic Diseases / drug therapy*
  • Metabolic Diseases / metabolism
  • Models, Molecular
  • Organ Specificity


  • Fatty Acid-Binding Proteins
  • Ligands