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Chemical Syntheses of Cart (Human, 55-102) Analogues and their Anorectic Effect on Food Intake in Rats Induced by Neuropeptide Y

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Abstract:

To understand the comparative effect on the anorectic property of the replacement of two Tyr residues at positions 58 and 62 in CART(55-102) by two Tyr(Me) or Phe(NO2) residues, [Tyr(Me)58,62]CART55-102 and [Phe(NO2)58,62]CART55-102 were synthesized. In vivo inhibitory activity on the food intake induced by NPY was compared with that of the parent peptide. [Phe(NO2)58,62]CART55-62 exhibited 2-fold higher anorectic activity on the food intake induced by NPY as compared with the parent peptide. [Tyr(Me)58,62]CART55-102 exhibited less potent anorectic activity than the parent peptide. These results indicate that aromaticity of two Tyr residues in CART55-102 is important for anorectic activity on the food intake induced by NPY and an electrophilic group on aromatic rings such as -NO2 enhanced anorectic activity more than that of the parent peptide. On the contrary, an electron-donating group on aromatic rings (Tyr58,62) such as CH3O- influenced to reduce anorectic activity as compared with the parent peptide.

Keywords: ANORECTIC EFFECT; CART (HUMAN,55-102); NEUROPEPTIDE Y; Solid-phase peptide synthesis; inhibitory activity

Document Type: Review Article

DOI: https://doi.org/10.2174/0929866013409382

Publication date: 2001-08-01

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  • Protein & Peptide Letters publishes short papers in all important aspects of protein and peptide research, including structural studies, recombinant expression, function, synthesis, enzymology, immunology, molecular modeling, drug design etc. Manuscripts must have a significant element of novelty, timeliness and urgency that merit rapid publication. Reports of crystallisation, and preliminary structure determinations of biologically important proteins are acceptable. Purely theoretical papers are also acceptable provided they provide new insight into the principles of protein/peptide structure and function.
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