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Iodination of CART(61‐102) peptide: Preserved binding and anorexigenic activity in mice
Author(s) -
Pražienková Veronika,
Marek Aleš,
Maletínská Lenka
Publication year - 2021
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3871
Subject(s) - cart , chemistry , peptide , cocaine and amphetamine regulated transcript , receptor , medicine , endocrinology , biochemistry , neuropeptide , biology , mechanical engineering , engineering
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 Met 67 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 Met 67 . All analogs revealed a high affinity to binding sites at PC12 cells and preserved biological activity.