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Please use this identifier to cite or link to this item: http://acervodigital.unesp.br/handle/11449/19559
Title: 
Determining the structural basis for specificity of ligands using crystallographic screening
Author(s): 
Institution: 
  • Pontifícia Universidade Católica do Rio Grande do Sul (PUCRS)
  • Universidade Federal de Mato Grosso do Sul (UFMS)
  • Universidade Estadual Paulista (UNESP)
ISSN: 
1085-9195
Abstract: 
Crystallographic screening has been used to identify new inhibitors for potential target for drug development. Here, we describe the application of the crystallographic screening to assess the structural basis of specificity of ligands against a protein target. The method is efficient and results in detailed crystallographic information. The utility of the method is demonstrated in the study of the structural basis for specificity of ligands for human purine nucleoside phosphorylase (PNP). Purine nucleoside phosphorylase catalyzes the phosphorolysis of the N-ribosidic bonds of purine nucleosides and deoxynucleosides. This enzyme is a target for inhibitor development aiming at T-cell immune response modulation and has been submitted to extensive structure-based drug design. This methodology may help in the future development of a new generation of PNP inhibitors.
Issue Date: 
1-Jan-2006
Citation: 
Cell Biochemistry and Biophysics. Totowa: Humana Press Inc., v. 44, n. 3, p. 405-411, 2006.
Time Duration: 
405-411
Publisher: 
Humana Press Inc
Keywords: 
  • PNP
  • crystallographic screening
  • structure
  • drug design
  • synchrotron radiation
Source: 
http://dx.doi.org/10.1385/CBB:44:3:405
URI: 
Access Rights: 
Acesso restrito
Type: 
outro
Source:
http://repositorio.unesp.br/handle/11449/19559
Appears in Collections:Artigos, TCCs, Teses e Dissertações da Unesp

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