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Novel analogues of bradykinin conformationally restricted in the C-terminal part of the molecule
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SYSNO ASEP 0360968 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Novel analogues of bradykinin conformationally restricted in the C-terminal part of the molecule Author(s) Sleszynska, M. (PL)
Wierzba, T. H. (PL)
Malinowski, K. (PL)
Borovičková, Lenka (UOCHB-X)
Maluch, I. (PL)
Sobolewski, D. (PL)
Lammek, B. (PL)
Slaninová, Jiřina (UOCHB-X)
Prahl, A. (PL)Number of authors 9 Source Title Journal of Peptide Science - ISSN 1075-2617
Roč. 17, č. 5 (2011), s. 366-372Number of pages 7 s. Language eng - English Country GB - United Kingdom Keywords bradykinin analogues ; B2 receptor antagonists ; sterically restricted residue ; in vivo rat blood pressure test ; in vitro rat uterus Subject RIV CC - Organic Chemistry CEZ AV0Z40550506 - UOCHB-X (2005-2011) UT WOS 000289441200011 DOI 10.1002/psc.1351 Annotation Achiral non-coded amino acids (N-benzylglycine, 2-aminomethylphenylacetic acid or 3-aminophenylacetic acid) were substituted at position 7 of the B-2 receptor antagonist [D-Arg(0), Hyp(3), Thi(5,8), D-Phe(7)]-BK. The N-terminal amino group of the analogues was either free or acylated with 1-Aca or Aaa. Biological activity of the compounds was assessed in the in vitro rat uterus test and the in vivo rat blood pressure test. Substitution in position 7 resulted in a decrease in antagonistic potency or change of the activity into agonistic one. Acylation of the N-terminus enhanced antagonistic properties of the resulting peptides in the rat blood pressure test. Workplace Institute of Organic Chemistry and Biochemistry Contact asep@uochb.cas.cz ; Kateřina Šperková, Tel.: 232 002 584 ; Viktorie Chládková, Tel.: 232 002 434 Year of Publishing 2012
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