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Bradykinin (BK) and des-Arg 9 -bradykinin (DBK) of kallikrein-kinin system exert its effects mediated by the B 2 (B 2 R) and B 1 (B 1 R) receptors, respectively. It was already shown that the deletion of kinin B 1 R or of B 2 R induces upregulation of the remaining receptor subtype [10,12,16,28,36]. However studies on overexpression of B ...
To probe the binding of a peptide agonist to a G-protein coupled receptor in native membranes, the spin-labeled amino acid analogue 4-amino-4-carboxy-2,2,6,6-tetramethylpiperidino-1-oxyl (TOAC) was substituted at either position 4 or 9 within the substance P peptide (RPKPQQFFGLM-NH2), a potent agonist of the neurokinin-1 receptor. The affinity of the 4-TOAC analog is comparable to the native peptide...
The present work comparatively analyzes the interaction of α-MSH and its more potent and long-acting analog [Nle 4 , D-Phe 7 ]α-MSH (NDP-MSH) with lipid bilayers. The peptides were spin labeled with Toac (2,2,6,6-tetramethylpiperidine-1-oxyl-4-amino-4-carboxylic acid) at the N-terminal, as those derivatives had been previously shown to keep their full biological activity. Due to the...
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