Reference : Structure-activity studies of bradykinin analogues on rat mast cell histamine release
Scientific journals : Article
Life sciences : Biochemistry, biophysics & molecular biology
Structure-activity studies of bradykinin analogues on rat mast cell histamine release
Bueb, Jean-Luc mailto [University of Luxembourg > Faculty of Science, Technology and Communication (FSTC) > Life Science Research Unit >]
Mousli, M. [> >]
Landry, Y. [> >]
Regoli, D. [> >]
Elsevier Science
Yes (verified by ORBilu)
New York
[en] Amino Acid Sequence ; drug effects ; pharmacology ; analogs and derivatives ; Structure-Activity Relationship ; Rats, Wistar ; Rats ; Molecular Sequence Data ; Mast Cells ; Male ; Histamine Release ; Bradykinin ; Animals ; metabolism
[en] Bradykinin (BK), kallidin (KD), and various analogues induced histamine release from rat mast cells. The results obtained with substituted analogues of BK indicated that: 1) the presence of both Arg residues at position 1 and 9 of kinins was favorable to confer histamine-releasing activity, 2) acetylation of the N-terminal amino acid residue led to a drastic reduction of this activity, 3) addition of a D-Arg residue at the N-terminus reduced their activity, as well as trans-4-hydroxyproline (Hyp) substitutions at position 2 or 3,4) D-Arg0 addition and Hyp3 substitution were synergistic in lowering activity, and 5) D-Phe7 substitution led to enhanced histamine-releasing activity.

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