Strongylophorines: Natural Product Inhibitors of Hypoxia-Inducible Factor-1 Transcriptional Pathway
Journal of Medicinal Chemistry2008Vol. 51(5), pp. 1402–1405
Citations Over TimeTop 22% of 2008 papers
Kaleem A. Mohammed, Raquel C. Jadulco, Tim S. Bugni, Mary Kay Harper, Megan Sturdy, Chris M. Ireland
Abstract
Rapidly increasing experimental and clinical data provides evidence for the role of hypoxia inducible factor-1 (HIF-1) as a crucial mediator of tumor survival and progression. In our effort to identify inhibitors of the HIF-1 activation pathway, we screened fractions from marine invertebrates. Fractions from an extract of Petrosia (Strongylophora) strongylata potently inhibited the HIF-1 activation pathway. Strongylophorines 2, 3, and 8 isolated from the active fractions were found to be responsible for the HIF-1 inhibition with EC 50 values of 8, 13, and 6 microM, respectively.
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