Leptin-based therapeutics

Abstract

Leptin, a pluripotent adipokine, has been discovered as a hormone controlling energy balance in hypothalamic neuroendocrine centers. In addition, recent studies provided ample evidence that leptin can be produced by cells other than adipocytes, and that the hormone can regulate many physiological processes other than energy balance and appetite. In this context, it is not surprising that both leptin excess as well as leptin insufficiency have been implicated in various pathologies. Consequently, despite initially disappointing results with recombinant leptin as the drug for obesity management, new leptin receptor modifiers have been developed and emerged as potential treatment modalities for numerous metabolic, immunological and neoplastic diseases. The major focus of this paper is a systematic review of current experimental leptin-based therapies, including pharmacological advantages and limitations of each prodrug category.

Keywords::

• leptin
• leptin mutants
• peptide drugs
• preclinical drug development

Financial & competing interests disclosure

This work was supported by funds from the Sbarro Health Research Organization and the Pennsylvania Department of Health. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

No writing assistance was utilized in the production of this manuscript.