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Structure-activity studies of bradykinin analogues on rat mast cell histamine release
Bueb, Jean-Luc; Mousli, M.; Landry, Y. et al.
1993In Peptides, 14 (4), p. 685-9
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Keywords :
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
Abstract :
[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.
Disciplines :
Biochemistry, biophysics & molecular biology
Identifiers :
UNILU:UL-ARTICLE-2008-199
Author, co-author :
Bueb, Jean-Luc ;  University of Luxembourg > Faculty of Science, Technology and Communication (FSTC) > Life Science Research Unit
Mousli, M.
Landry, Y.
Regoli, D.
Language :
English
Title :
Structure-activity studies of bradykinin analogues on rat mast cell histamine release
Publication date :
1993
Journal title :
Peptides
ISSN :
0196-9781
Publisher :
Elsevier Science, New York, United States - New York
Volume :
14
Issue :
4
Pages :
685-9
Peer reviewed :
Peer reviewed
Available on ORBilu :
since 09 September 2013

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