Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1364572 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
Abstract
The natural product salicylihalamide is a potent inhibitor of the Vacuolar ATPase (V-ATPase), a potential target for antitumor chemotherapy. We generated salicylihalamide-resistant tumor cell lines typified by an overexpansion of lysosomal organelles. We also found that many tumor cell lines upregulate tissue-specific plasmalemmal V-ATPases, and hypothesize that tumors that derive their energy from glycolysis rely on these isoforms to maintain a neutral cytosolic pH. To further validate the potential of V-ATPase inhibitors as leads for cancer chemotherapy, we developed a multigram synthesis of the potent salicylihalamide analog saliphenylhalamide.
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Related Topics
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Organic Chemistry
Authors
Sylvain Lebreton, Janis Jaunbergs, Michael G. Roth, Deborah A. Ferguson, Jef K. De Brabander,