Iodination of CART(61-102) peptide: Preserved binding and anorexigenic activity in mice
Language English Country England, Great Britain Media print-electronic
Document type Journal Article, Review
PubMed
32678955
DOI
10.1002/jlcr.3871
Knihovny.cz E-resources
- Keywords
- CART peptide, PC12 cells, competitive binding experiments, food intake,
- MeSH
- Appetite Depressants chemistry pharmacokinetics therapeutic use MeSH
- PC12 Cells MeSH
- Cocaine- and Amphetamine-Regulated Transcript Protein MeSH
- Rats MeSH
- Mice MeSH
- Nerve Tissue Proteins chemistry pharmacokinetics therapeutic use MeSH
- Radiopharmaceuticals chemistry pharmacokinetics therapeutic use MeSH
- Iodine Radioisotopes chemistry MeSH
- Protein Binding MeSH
- Animals MeSH
- Check Tag
- Rats MeSH
- Mice MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Review MeSH
- Names of Substances
- Appetite Depressants MeSH
- Cocaine- and Amphetamine-Regulated Transcript Protein MeSH
- Nerve Tissue Proteins MeSH
- Radiopharmaceuticals MeSH
- Iodine Radioisotopes MeSH
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.
See more in PubMed
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