Pharmacological exploitation of the α1-adrenoreceptor antagonist doxazosin to develop a novel class of antitumor agents that block intracellular protein kinase B/Akt …

…, YT Yang, JB Garrison, N Kyprianou…

Index: Shaw, Yeng-Jeng; Yang, Ya-Ting; Garrison, Jason B; Kyprianou, Natasha; Chen, Ching-Shih Journal of medicinal chemistry, 2004 , vol. 47, # 18 p. 4453 - 4462

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Citation Number: 51

Abstract

The α1-adrenoreceptor antagonist doxazosin induces apoptosis in malignant cells with moderate potency via an α1-adrenoreceptor-independent mechanism. Here, we demonstrate that the ability of doxazosin to induce apoptosis in PC-3 prostate cancer cells was, in part, attributable to the inhibition of protein kinase B (PKB)/Akt activation. The separation of the effect of doxazosin on apoptosis from its original pharmacological activity ...