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Can the 1,5-disubstituted tetrazole ring modify the co-ordinating ability and biological activity of opiate-like peptides?

Lodyga-Chruscinska, Elzbieta and Brzezinska-Blaszczyk, Ewa and Micera, Giovanni and Sanna, Daniele and Kozlowski, Henryk and Olczak, Jacek and Zabrocki, Janusz and Olejnik, Alicja K. (2000) Can the 1,5-disubstituted tetrazole ring modify the co-ordinating ability and biological activity of opiate-like peptides? Journal of Inorganic Biochemistry, Vol. 78 (4), p. 283-291. ISSN 0162-0134. Article.

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DOI: 10.1016/S0162-0134(00)00055-6

Abstract

The copper(II) complexing ability and the biological activity of β-casomorphin-7 tetrazole analogues have been investigated. Potentiometric and spectroscopic (UV–Vis, CD and EPR) studies have been used to establish the thermodynamic stability, speciation and structure of Cu(II) complexes with YP-ψ(CN4)-FPGPI-NH2 (1), YPF-ψ(CN4)-AGPI-NH2 (2) and YPFP-ψ(CN4)-GPI-NH2 (3). Comparison of the binding ability of the tetrazole analogues reveals that the most effective ligand for copper(II) is YPF-ψ(CN4)-AGPI-NH2. The effectiveness of this ligand comes from its particular conformation suited for the Cu(II) 2N co-ordination mode in the physiological pH region. The ability of casomorphin tetrazole analogues to activate rat mast cells to histamine release in vitro in the presence of copper(II) has been studied.

Item Type:Article
ID Code:1413
Status:Published
Refereed:Yes
Uncontrolled Keywords:β-Casomorphin-7-amide tetrazole analogues, Copper(II) complexes, mast cells
Subjects:Area 03 - Scienze chimiche > CHIM/03 Chimica generale e inorganica
Divisions:001 Università di Sassari > 01 Dipartimenti > Chimica
002 Altri enti e centri di ricerca del Nord Sardegna > CNR-Consiglio Nazionale delle Ricerche > Istituto di chimica biomolecolare, Sassari
Publisher:Elsevier Science
ISSN:0162-0134
Additional Information:Pubblicato online il 7 luglio 2000.
Deposited On:18 Aug 2009 10:05

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