Leptin-activity blockers: Development and potential use in experimental biology and medicine1

Arieh Gertler*, Gili Solomon

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

22 Scopus citations

Abstract

The first adipokine, leptin, discovered almost 20 years ago, is secreted into circulation mainly from adipose tissue and acts both centrally and peripherally. Leptin regulates energy metabolism, reproductive function, bone metabolism, and immune response. However in some physiological or pathological situations such as enhancement of undesired immune responses in autoimmune diseases, tumorigenesis, elevated blood pressure, and certain cardiovascular pathologies, leptin activity may be harmful. In this review we screen different approaches to blocking leptin action, in vitro and in vivo. The recent development of superactive leptin muteins exhibiting antagonistic properties, and other leptin-action-blocking peptides, proteins, monoclonal antibodies, and nanobodies, opens new perspectives for their use in research, and eventually, therapy for cachexia, autoimmune disease, cancer, and other pathologies.

Original languageEnglish
Pages (from-to)873-882
Number of pages10
JournalCanadian Journal of Physiology and Pharmacology
Volume91
Issue number11
DOIs
StatePublished - Jun 2013

Keywords

  • Antagonist
  • Anti-autoimmune diseases
  • Blood pressure
  • Cancer
  • Inflammatory disease
  • Leptin
  • Metabolic syndrome
  • T2DM model
  • Uremic cachexia

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