Chemical Syntheses of Cart (Human, 55-102) Analogues and their Anorectic Effect on Food Intake in Rats Induced by Neuropeptide Y
Authors: Abiko T.; Ogawa R.
Source: Protein and Peptide Letters, Volume 8, Number 4, August 2001 , pp. 289-295(7)
Publisher: Bentham Science Publishers
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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: CART (HUMAN,55-102); ANORECTIC EFFECT; NEUROPEPTIDE Y; inhibitory activity; Solid-phase peptide synthesis
Language: English
Document Type: Review article
DOI: 10.2174/0929866013409382
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