Iodination of CART(61-102) peptide: Preserved binding and anorexigenic activity in mice

J Labelled Comp Radiopharm. 2021 Feb;64(2):61-64. doi: 10.1002/jlcr.3871. Epub 2020 Aug 10.

Abstract

CART (cocaine- and amphetamine-regulated transcript) peptides are involved in food intake regulation, stress, and other physiological functions. Although CART peptides have been known for over 25 years, their receptor(s) have not yet been characterized. In this short review, we will summarize our previous studies, where we reported specific binding of 125 I-CART(61-102) to PC12 rat pheochromocytoma cells. Competitive binding experiments performed with mono- and di-iodinated peptides and their isoforms with oxidized Met67 resulted in nanomolar binding affinity. Moreover, in our previous study, CART(61-102), as well as di-iodinated CART(61-102), have shown a strong anorexigenic effect in fasted lean mice after intracerebroventricular administration. In conclusion, from our previous studies, iodination of CART(61-102) resulted in mono- and di-iodinated analogs with or without oxidized Met67 . All analogs revealed a high affinity to binding sites at PC12 cells and preserved biological activity.

Keywords: CART peptide; PC12 cells; competitive binding experiments; food intake.

Publication types

  • Review

MeSH terms

  • Animals
  • Appetite Depressants / chemistry
  • Appetite Depressants / pharmacokinetics*
  • Appetite Depressants / therapeutic use
  • Iodine Radioisotopes / chemistry
  • Mice
  • Nerve Tissue Proteins / chemistry
  • Nerve Tissue Proteins / pharmacokinetics*
  • Nerve Tissue Proteins / therapeutic use
  • PC12 Cells
  • Protein Binding
  • Radiopharmaceuticals / chemistry
  • Radiopharmaceuticals / pharmacokinetics*
  • Radiopharmaceuticals / therapeutic use
  • Rats

Substances

  • Appetite Depressants
  • Iodine Radioisotopes
  • Nerve Tissue Proteins
  • Radiopharmaceuticals
  • cocaine- and amphetamine-regulated transcript protein