Curr Pharm Des. 2017 Oct 11; doi: 10.2174/1381612823666171011103551. Epub 2017 Oct 11.
1,N6-ethenoadenine and other Fluorescent Nucleobase Analogues as Substrates for Purine-Nucleoside Phosphorylases: Spectroscopic and Kinetic Studies.
Current pharmaceutical design
Jacek Wierzchowski, Alicja Stachelska-Wierzchowska, Beata Wielgus-Kutrowska, Agnieszka Bzowska
Affiliations
Affiliations
- Department of Biophysics, Faculty of Food Sciences, University of Varmia & Masuria, Olsztyn. Poland.
- Division of Biophysics, Institute of Experimental Physics, Faculty of Physics, University of Warsaw. Poland.
PMID: 29022509
DOI: 10.2174/1381612823666171011103551
Abstract
BACKGROUND: Purine-nucleoside phosphorylase (PNP) is known as a tool for the synthesis of various nucleosides and nucleoside analogues. Mechanism, properties, molecular diversity and inhibitors of PNP, particularly these of pharmacological significance, are briefly characterized.
METHODS: UV and fluorescence spectroscopy was used for kinetic experiments, and HPLC chromatography for product analyses.
RESULTS: Applications of various forms of PNP to synthesis of selected fluorescent nucleosides, particularly ribosides of 1,N6-ethenoadenine and various 8-azapurines (triazolo[4,5-d]pyrimidines) are reviewed. Different specificity of various PNP forms is described towards nucleobase and analogue substrates as well as variable ribosylation sites observed in some reactions, with a possibility to further modify these features via the site-directed mutagenesis.
CONCLUSION: Present and future applications of the fluorescent or fluorogenic ribosides are discussed, with particular emphasis on biochemical and clinical analyses with improved sensitivity.
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Keywords: enzyme assays; enzyme-ligand complexes.
; fluorescence; isozymes; nucleoside analogs; purine-nucleoside phosphorylase
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