A structure-based site-directed mutagenesis study on the neurolysin (EC 3.4.24.16) and thimet oligopeptidase (EC 3.4.24.15) catalysis

Neurolysin (EP24.16) and thimet oligopeptidase (EP24.15) are closely related metalloendopeptidases. Site-directed mutagenesis of Tyr(613) (EP24.16) or Tyr(612) (EP24.15) to either Phe or Ala promoted a strong reduction of k(cat)/K-M for both enzymes. These data suggest the importance of both hydroxy...

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Bibliographic Details
Authors: Oliveira, Vitor [UNIFESP], Araujo, M. C., Rioli, V, Camargo, Antonio Carlos Martins de [UNIFESP], Tersariol, Ivarne Luis dos Santos [UNIFESP], Juliano, Maria Aparecida [UNIFESP], Juliano, Luiz [UNIFESP], Ferro, Emer Suavinho [UNIFESP]
Format: article
Status:Published version
Publication Date:2003
Country:Brasil
Institution:Universidade Federal de São Paulo (UNIFESP)
Repository:Repositório Institucional da UNIFESP
Language:English
OAI Identifier:oai:repositorio.unifesp.br:11600/27211
Online Access:http://dx.doi.org/10.1016/S0014-5793(03)00310-7
http://repositorio.unifesp.br/handle/11600/27211
Access Level:Open access
Keyword:enzyme specificity
catalytic mechanism
site-directed mutagenesis
Description
Summary:Neurolysin (EP24.16) and thimet oligopeptidase (EP24.15) are closely related metalloendopeptidases. Site-directed mutagenesis of Tyr(613) (EP24.16) or Tyr(612) (EP24.15) to either Phe or Ala promoted a strong reduction of k(cat)/K-M for both enzymes. These data suggest the importance of both hydroxyl group and aromatic ring at this specific position during substrate hydrolysis by these peptidases. Furthermore, the EP24.15 A607G mutant showed a k(cat)/K-M of 2x10(5) M-1 s(-1) for the Abz-GFSIFRQ-EDDnp substrate, similar to that of EP24.16 (k(cat)/K-M = 3x10(5) M-1 s(-1)) which contains Gly at the corresponding position; the wild type EP24.15 has a k(cat)/K-M of 2.5x10(4) M-1 s(-1) for this substrate. (C) 2003 Federation of European Biochemical Societies. Published by Elsevier Science B.V. All rights reserved.