Gunaratnam, M. and Neidle, S. (2010) An evaluation cascade for G-quadruplex telomere targeting agents in human cancer cells. In: Drug-DNA Interaction Protocols. Methods in molecular biology (613 ). Humana Press, NJ, USA, pp. 303-13. ISBN 978-1-60327-417-3. 10.1007/978-1-60327-418-0_19.
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The targeting of telomerase and telomere maintenance in human cancer cells can be achieved by small molecules that induce the 3'single-stranded ends of telomeric DNA to fold up into four-stranded quadruplex structures that inhibit the action of the telomerase enzyme complex. In this chapter, we describe a series of biochemical, biophysical, and cellular assays that are used to evaluate the activity of new compounds, and so assess whether they are suitable for examination in xenograft models of human cancer. These assays evaluate quadruplex stabilisation properties, short- and long-term cell viability, telomerase enzymatic activity, cellular senescence, and telomere length changes.
|Item Type:||Book Section|
|Uncontrolled Keywords:||Telomere - Telomerase - Quadruplex - Senescence - Small molecule drugs|
|Departments, units and centres:||Department of Pharmaceutical and Biological Chemistry > Cancer Research UK Biomolecular Structure Group|
|Journal or Publication Title:||Drug-DNA Interaction Protocols|
|Deposited By:||Library Staff|
|Deposited On:||04 Feb 2011 09:26|
|Last Modified:||04 Feb 2011 09:26|
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