Design of new and sensitive fluorogenic substrates for human kallikrein hK3 (prostate-specific antigen) derived from semenogelin sequences

Design of new and sensitive fluorogenic substrates for human kallikrein hK3 (prostate-specific antigen) derived from semenogelin sequences

Autor Rehault, S. Google Scholar
Brillard-Bourdet, M. Google Scholar
Bourgeois, L. Google Scholar
Frenette, G. Google Scholar
Juliano, L. Google Scholar
Gauthier, F. Google Scholar
Moreau, T. Google Scholar
Instituição Univ Tours
CHUL
Univ Laval
Universidade Federal de São Paulo (UNIFESP)
Resumo Human kallikrein hK3 (prostate-specific antigen) is a chymotrypsin-like serine protease which is widely used in the diagnosis of prostate cancer. Assays of the enzymatic activity of hK3 in extracellular fluids have been limited by a lack of sensitive synthetic substrates. This report describes the design of a series of internally quenched fluorescent peptides containing an amino acid sequence based on preferential hK3 cleavage sites in semenogelins. Those were identified by 2-D gel electrophoresis analysis and N-terminal sequencing of semenogelin fragments generated by ex vivo proteolysis in freshly ejaculated semen. These peptides were cleaved by hK3 at the C-terminal of certain tyrosyl or glutaminyl residues with k(cat)/K-m values of 15 000-60 000 M-1 s(-1). the substrate Abz-SSIYSQTEEQ-EDDnp was cleaved at the Tyr-Ser bond with a specificity constant k(cat)/K-m of 60000 M-1 s(-1), making it the best substrate for hK3 described to date. (C) 2002 Elsevier Science B.V. All rights reserved.
Palavra-chave human kallikrein
prostate-specific antigen
semenogelin
substrate specificity
chymotrypsin-like enzyme
Idioma Inglês
Data de publicação 2002-04-01
Publicado em Biochimica Et Biophysica Acta-protein Structure and Molecular Enzymology. Amsterdam: Elsevier B.V., v. 1596, n. 1, p. 55-62, 2002.
ISSN 0167-4838 (Sherpa/Romeo, fator de impacto)
Publicador Elsevier B.V.
Extensão 55-62
Fonte http://dx.doi.org/10.1016/S0167-4838(02)00204-2
Direito de acesso Acesso restrito
Tipo Artigo
Web of Science WOS:000175657300007
Endereço permanente http://repositorio.unifesp.br/handle/11600/26814

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