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Proceedings Paper

Combined SERS and flow linear dichroism approach to monitoring the interaction of pharmaceuticals with their target
Author(s): Anatoli I. Ianoul; Fabrice Fleury; Olivier Duval; Jean-Claude Jardillier; Alain J.P. Alix; Igor R. Nabiev
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Paper Abstract

Surface-Enhanced Raman Scattering (SERS) spectroscopy and Flow Linear Dichroism (FLD) technique have been employed to study the anticancer agent fagaronine and its derivative ethoxidine - double inhibitors of DNA topoisomerases I and II. Cooperative use of two methods permitted (i) to determine the molecular determinants of the drug-DNA interactions; (ii) to monitor in real time the process of topo I inhibition by these anticancer agents. FLD technique allowed us to identify the mode of drug interactions with the DNA as a 'major groove intercalation' and to determine orientation of the drugs chromophores within the complexes. Using SERS spectroscopy we have determined the drugs molecular determinants interacting with the DNA. FLD was also used for real time monitoring of the process of sc DNA relaxation by topo I and of inhibition of relaxation with the pharmaceuticals. Ethoxidine was found to exhibit the same activity of inhibition of sc DNA relaxation as fagaronine at the 10-fold less concentration. The proposed SERS-FLD combined approach demonstrates the new perspectives for screening new pharmaceuticals due to its relative simplicity and low expense, high sensitivity and selectivity, and, finally, possibility of real-time monitoring of the structure-function correlation within the series of drug derivatives.

Paper Details

Date Published: 21 April 1999
PDF: 11 pages
Proc. SPIE 3603, Systems and Technologies for Clinical Diagnostics and Drug Discovery II, (21 April 1999); doi: 10.1117/12.346747
Show Author Affiliations
Anatoli I. Ianoul, Univ. de Reims Champagne-Ardenne and Shemyakin & Ovchinnikov Institute of Bioorganic Chem (Canada)
Fabrice Fleury, Univ. de Reims Champagne-Ardenne (France)
Olivier Duval, Univ. d'Angers (France)
Jean-Claude Jardillier, Univ. de Reims Champagne-Ardenne (France)
Alain J.P. Alix, Univ. de Reims Champagne-Ardenne (France)
Igor R. Nabiev, Univ. de Reims Champagne-Ardenne (France)


Published in SPIE Proceedings Vol. 3603:
Systems and Technologies for Clinical Diagnostics and Drug Discovery II
Gerald E. Cohn; John C. Owicki, Editor(s)

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