Inhibition of Hypoxia Inducible Factor-2 Transcription: Isolation of Active Modulators from Marine Sponges

Journal of Natural Products
2012.0

Abstract

Renal or kidney cancer accounts for about 3% of all cancer cases reported each year in the U.S. Molecular signatures that define the cancer, such as the loss of functional VHL, are found in both sporadic and familial cases of cancer. In clear cell renal cancer, the transcription factor HIF-2α has been shown to have a distinct role in tumorigenesis. Our laboratories developed a cell-based screen to identify modulators of HIF-2α. Screening of the NCI's Natural Product Extract Repository resulted in the identification of 10 sponge extracts, from which 12 compounds were isolated. The biological evaluation of these compounds will be discussed including evaluation of HIF-1α vs HIF-2α selectivity and the isolated compounds' effects on mRNA from several pathways regulated by HIF.

Knowledge Graph

Similar Paper

Inhibition of Hypoxia Inducible Factor-2 Transcription: Isolation of Active Modulators from Marine Sponges
Journal of Natural Products 2012.0
Molecular-Targeted Antitumor Agents. 19. Furospongolide from a Marine <i>Lendenfeldia</i> sp. Sponge Inhibits Hypoxia-Inducible Factor-1 Activation in Breast Tumor Cells
Journal of Natural Products 2008.0
Molecular-Targeted Antitumor Agents. 15. Neolamellarins from the Marine Sponge <i>Dendrilla nigra</i> Inhibit Hypoxia-Inducible Factor-1 Activation and Secreted Vascular Endothelial Growth Factor Production in Breast Tumor Cells
Journal of Natural Products 2007.0
Screening and Biological Effects of Marine Pyrroloiminoquinone Alkaloids: Potential Inhibitors of the HIF-1α/p300 Interaction
Journal of Natural Products 2016.0
Cytotoxic Metabolites from an Indonesian Sponge <i>Lendenfeldia</i> sp.
Journal of Natural Products 2007.0
Lipophilic 2,5-Disubstituted Pyrroles from the Marine Sponge <i>Mycale</i> sp. Inhibit Mitochondrial Respiration and HIF-1 Activation
Journal of Natural Products 2009.0
Structures and Potential Antitumor Activity of Sesterterpenes from the Marine Sponge Hyrtios communis
Journal of Natural Products 2013.0
Lipophilic 2,5-Disubstituted Pyrroles from the Marine Sponge <i>Mycale</i> sp. Inhibit Mitochondrial Respiration and HIF-1 Activation
Journal of Natural Products 2009.0
Sodwanone and Yardenone Triterpenes from a South African Species of the Marine Sponge <i>Axinella</i> Inhibit Hypoxia-Inducible Factor-1 (HIF-1) Activation in Both Breast and Prostate Tumor Cells
Journal of Natural Products 2006.0
Benzochromenones from the Marine Crinoid Comantheria rotula Inhibit Hypoxia-Inducible Factor-1 (HIF-1) in Cell-Based Reporter Assays and Differentially Suppress the Growth of Certain Tumor Cell Lines
Journal of Natural Products 2007.0