Exploring the structural requirements for inhibition of the ubiquitin E3 ligase breast cancer associated protein 2 (BCA2) as a treatment for breast cancer

G Brahemi, FR Kona, A Fiasella, D Buac…

Index: Brahemi, Ghali; Kona, Fathima R.; Fiasella, Annalisa; Buac, Daniela; Soukupova, Jitka; Brancale, Andrea; Burger, Angelika M.; Westwell, Andrew D. Journal of Medicinal Chemistry, 2010 , vol. 53, # 7 p. 2757 - 2765

Full Text: HTML

Citation Number: 67

Abstract

The zinc-ejecting aldehyde dehydrogenase (ALDH) inhibitory drug disulfiram (DSF) was found to be a breast cancer-associated protein 2 (BCA2) inhibitor with potent antitumor activity. We herein describe our work in the synthesis and evaluation of new series of zinc- affinic molecules to explore the structural requirements for selective BCA2-inhibitory antitumor activity. An N (C S) S S motif was found to be required, based on selective ...