Structural and Functional Analysis of the Complex between Citrate and the Zinc Peptidase Carboxypeptidase A
Joint Authors
Avilés, Francesc X.
Vendrell, Josep
Pallarès, Irantzu
Fernández, Daniel
Boix, Ester
Source
Issue
Vol. 2011, Issue 2011 (31 Dec. 2011), pp.1-8, 8 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2011-07-25
Country of Publication
Egypt
No. of Pages
8
Main Subjects
Abstract EN
A high-resolution carboxypeptidase-Zn2+-citrate complex was studied by X-ray diffraction and enzyme kinetics for the first time.
The citrate molecule acts as a competitive inhibitor of this benchmark zinc-dependent peptidase, chelating the catalytic zinc ion in the active site of the enzyme and inducing a conformational change such that carboxypeptidase adopts the conformation expected to occur by substrate binding.
Citrate adopts an extended conformation with half of the molecule facing the zinc ion, while the other half is docked in the S1′ hydrophobic specificity pocket of the enzyme, in contrast with the binding mode expected for a substrate like phenylalanine or a peptidomimetic inhibitor like benzylsuccinic acid.
Combined structural and enzymatic analysis describes the characteristics of the binding of this ligand that, acting against physiologically relevant zinc-dependent proteases, may serve as a general model in the design of new drug-protecting molecules for the oral delivery of drugs of peptide origin.
American Psychological Association (APA)
Fernández, Daniel& Boix, Ester& Pallarès, Irantzu& Avilés, Francesc X.& Vendrell, Josep. 2011. Structural and Functional Analysis of the Complex between Citrate and the Zinc Peptidase Carboxypeptidase A. Enzyme Research،Vol. 2011, no. 2011, pp.1-8.
https://search.emarefa.net/detail/BIM-447931
Modern Language Association (MLA)
Fernández, Daniel…[et al.]. Structural and Functional Analysis of the Complex between Citrate and the Zinc Peptidase Carboxypeptidase A. Enzyme Research No. 2011 (2011), pp.1-8.
https://search.emarefa.net/detail/BIM-447931
American Medical Association (AMA)
Fernández, Daniel& Boix, Ester& Pallarès, Irantzu& Avilés, Francesc X.& Vendrell, Josep. Structural and Functional Analysis of the Complex between Citrate and the Zinc Peptidase Carboxypeptidase A. Enzyme Research. 2011. Vol. 2011, no. 2011, pp.1-8.
https://search.emarefa.net/detail/BIM-447931
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-447931