NDLI: A structure-activity study on the bradykinin B$_{1}$ antagonist desArg$^{10}$-HOE 140: The alanine scan

Content Provider	Springer Nature Link
Author	Galoppini, Claudia Patacchini, Riccardo Meini, Stefania Viganò, Stefania Tancredi, Mariella Quartara, Laura Triolo, Antonio Maggi, Carlo A. Rovero, Paolo
Copyright Year	1999
Abstract	It has recently been shown that the biological activity of the second generation kinin B$_{1}$ receptor selective antagonist, desArg$^{10}$ HOE 140, can be improved by specific amino acid substitutions. Starting from this observation, we undertook a systematic structure-activity relationship study of this antagonist, based on the alanine-scan technique, in order to obtain useful information for the rational design of more analogues. Our data indicate that the sequence of desArg$^{10}$ HOE 140 does not tolerate the replacement by Ala of most of its residues, with the exception of Ser in position 7 and, to a lesser extent, D-Arg in position 1 and Hyp in position 4. The most critical residues appear to be Pro in position 3 and the C-terminal dipeptide Dtic-Oic; Ala replacement at these positions resultes in a total loss of activity. Moreover, replacement by Ala of Gly in position 5 reverts the activity of desArg$^{10}$ HOE 140 to that of an agonist.
Starting Page	123
Ending Page	127
Page Count	5
File Format	PDF
ISSN	09295666
Journal	International Journal of Peptide Research and Therapeutics
Volume Number	6
Issue Number	2-3
e-ISSN	1573496X
Language	English
Publisher	Kluwer Academic Publishers
Publisher Date	1999-01-01
Publisher Place	Dordrecht
Access Restriction	Subscribed
Subject Keyword	B$_{1}$ kinin receptor peptide antagonist Polymer Sciences Biochemistry Animal Anatomy / Morphology / Histology
Content Type	Text
Resource Type	Article
Subject	Biochemistry

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