Abstract
Abstract The thiosemicarbazone NSC73306 is one of several agents identified in a screen for agents that selectively kill cells expressing the multidrug resistance transporter P-glycoprotein (MDR1, ABCB1, P-gp). Prolonged exposure of P-gp expressing cells to NSC73306 down-regulates P-gp, re-sensitizing the cells to conventional chemotherapeutics. Given the exciting potential for NSC73306 as a potential therapy for previously intractable multidrug resistant cancer cells, in vitro and in vivo validation is underway. A series of NSC73306 analogs have been synthesized in order to examine the structural requirements for MDR1-selectivity of this family of compounds, and a proposed pharmacophore for MDR1-selectivity has been generated. In parallel, new MDR1-selective chemotypes are being discovered and validated through a number of strategies, including bioinformatic, high throughput screening and drug design approaches. Citation Format: {Authors}. {Abstract title} [abstract]. In: Proceedings of the 101st Annual Meeting of the American Association for Cancer Research; 2010 Apr 17-21; Washington, DC. Philadelphia (PA): AACR; Cancer Res 2010;70(8 Suppl):Abstract nr 3533.
Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
