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Iodination of CART(61-102) peptide: Preserved binding and anorexigenic activity in mice
V. Pražienková, A. Marek, L. Maletínská
Jazyk angličtina Země Velká Británie
Typ dokumentu časopisecké články, přehledy
PubMed
32678955
DOI
10.1002/jlcr.3871
Knihovny.cz E-zdroje
- MeSH
- anorektika chemie farmakokinetika terapeutické užití MeSH
- buňky PC12 MeSH
- krysa rodu rattus MeSH
- myši MeSH
- proteiny nervové tkáně chemie farmakokinetika terapeutické užití MeSH
- radiofarmaka chemie farmakokinetika terapeutické užití MeSH
- radioizotopy jodu chemie MeSH
- vazba proteinů MeSH
- zvířata MeSH
- Check Tag
- krysa rodu rattus MeSH
- myši MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- přehledy 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.
Citace poskytuje Crossref.org
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