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Title: Synthesis and pharmacological properties of TOAC-labeled angiotensin and bradykinin analogs
Authors: Nakaie, Clovis Ryuichi [UNIFESP]
Silva, Eneida de Gusmão [UNIFESP]
Cilli, Eduardo Maffud [UNIFESP]
Marchetto, Reinaldo [UNIFESP]
Schreier, Shirley [UNIFESP]
Paiva, Therezinha Bandiera [UNIFESP]
Paiva, Antonio Cechelli de Mattos [UNIFESP]
Universidade Federal de São Paulo (UNIFESP)
Universidade de São Paulo (USP)
Keywords: angiotensin analogs
bradykinin analogs
peptide synthesis
spin labeled peptides
TOAC spin label
electron paramagnetic resonance
Issue Date: 1-Jan-2002
Publisher: Elsevier B.V.
Citation: Peptides. New York: Elsevier B.V., v. 23, n. 1, p. 65-70, 2002.
Abstract: Angiotensin II (AngII) and bradykinin (BK) derivatives containing the TOAC (2,2,6,6-tetramethylpiperidine-N-oxyl-4-amino-4-carboxylic acid) spin label were synthesized by solid phase methodology. Ammonium hydroxide (pH 10, 50degreesC, 1 h) was the best means for reverting nitroxide protonation occurring during peptide cleavage. EPR spectra yielded rotational correlation times for internally labeled analogs that were nearly twice as large as those of N-terminally labeled analogs. Except for TOAC(1)-AngII and TOAC(0)-BK, which showed high intrinsic activities, other derivatives were inactive in smooth muscle preparations. These active paramagnetic analogs may be useful for conformational studies in solution and in the presence of model and biological membranes. (C) 2002 Elsevier Science Inc. All rights reserved.
ISSN: 0196-9781
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Appears in Collections:Em verificação - Geral

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