CLC number: O657.63
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Received: 2004-03-02
Revision Accepted: 2004-04-30
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ZHANG Hong, PAN Yuan-jiang. Affinity ultrafiltration of DNA topoisomerases-targeted compounds determined with HPLC/ESI-MS for drug candidate screening[J]. Journal of Zhejiang University Science A, 2004, 5(8): 900-905.
@article{title="Affinity ultrafiltration of DNA topoisomerases-targeted compounds determined with HPLC/ESI-MS for drug candidate screening",
author="ZHANG Hong, PAN Yuan-jiang",
journal="Journal of Zhejiang University Science A",
volume="5",
number="8",
pages="900-905",
year="2004",
publisher="Zhejiang University Press & Springer",
doi="10.1631/jzus.2004.0900"
}
%0 Journal Article
%T Affinity ultrafiltration of DNA topoisomerases-targeted compounds determined with HPLC/ESI-MS for drug candidate screening
%A ZHANG Hong
%A PAN Yuan-jiang
%J Journal of Zhejiang University SCIENCE A
%V 5
%N 8
%P 900-905
%@ 1869-1951
%D 2004
%I Zhejiang University Press & Springer
%DOI 10.1631/jzus.2004.0900
TY - JOUR
T1 - Affinity ultrafiltration of DNA topoisomerases-targeted compounds determined with HPLC/ESI-MS for drug candidate screening
A1 - ZHANG Hong
A1 - PAN Yuan-jiang
J0 - Journal of Zhejiang University Science A
VL - 5
IS - 8
SP - 900
EP - 905
%@ 1869-1951
Y1 - 2004
PB - Zhejiang University Press & Springer
ER -
DOI - 10.1631/jzus.2004.0900
Abstract: A method of screening assay is demonstrated. The approach is based on the affinity of antitumor candidates for topoi-somerases. In this method, antitumor candidates are fished out using topoisomerases as targets. Traditional analysis of complex compounds typically encounters signal suppression due to the relatively low concentrations, but enzyme-affinity screening for the active compounds can effectively concentrate the desired analysts into a small volume of high concentration. Active compounds are separated from non-affinity compounds by ultrafiltration. The molecules-enzymes complexes that are retained on the filter are subsequently separated by acidification to obtain the topoisomerases-affinity compounds for analysis on High Performance Liquid Chromatography coupled with electrospray ionization mass spectrometric detection (ESI-MS). This enzyme-affinity based screening assay provides a highly specific and efficient method that can directly screen, identify, and acquire drug candidates thus improving the accuracy and speed of high-throughput screening activities.
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