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dc.contributor.authorGrkovic, Tanjaen_US
dc.contributor.authorL. Whitson, Emilyen_US
dc.contributor.authorC. Rabe, Danielen_US
dc.contributor.authorS. Gardella, Robertaen_US
dc.contributor.authorP. Bottaro, Donalden_US
dc.contributor.authorMarston Linehan, W.en_US
dc.contributor.authorB. McMahon, Jamesen_US
dc.contributor.authorR. Gustafson, Kirken_US
dc.contributor.authorC. McKee, Tawnyaen_US
dc.date.accessioned2017-04-24T13:36:32Z
dc.date.available2017-04-24T13:36:32Z
dc.date.issued2011en_US
dc.date.modified2011-09-22T06:52:41Z
dc.identifier.issn0960894Xen_US
dc.identifier.doi10.1016/j.bmcl.2011.01.127en_AU
dc.identifier.urihttp://hdl.handle.net/10072/40966
dc.description.abstractKidney cancer was the cause of almost 13,000 deaths in the United States in 2009. Loss of function of the VHL tumor suppressor gene (von Hippel-Lindau disease) dramatically increases the risk of developing clear cell kidney cancer. The VHL protein is best understood for its regulation of hypoxia inducible factor (HIF). HIF responds to changes in oxygen levels in the cell and is responsible for mediating the transcriptional response to hypoxia. Of the three known HIFalpha gene products, HIF-2alpha appears to play a fundamental role in renal carcinoma. A high throughput screen was developed to identify small molecule inhibitors of HIF-2 gene expression. The screen was performed and yielded 153 confirmed active natural product extracts. Three of the active extracts were from marine soft corals of the order Alcyonacea: Sarcophyton sp., Lobophytum sarcophytoides and Asterospicularia laurae. Bioassay-guided fractionation led to the isolation of two new cembrane diterpenes, (4Z,8S*,9R*,12E,14E)-9-hydroxy-1-(prop-1-en-2-yl)-8,12-dimethyl-oxabicyclo[9.3.2]-hexadeca-4,12,14-trien-18-one (1), and (1E,3E,7R*,8R*,11E)-1-(2-methoxypropan-2-yl)-4,8,12-trimethyloxabicyclo[12.1.0]-pentadeca-1,3,11-triene (7), as well as eight known compounds, 2-6 and 8-10.en_US
dc.description.peerreviewedYesen_US
dc.description.publicationstatusYesen_AU
dc.languageEnglishen_US
dc.language.isoen_AU
dc.publisherElsevieren_US
dc.publisher.placeUnited Kingdomen_US
dc.relation.ispartofstudentpublicationNen_AU
dc.relation.ispartofpagefrom2113en_US
dc.relation.ispartofpageto2115en_US
dc.relation.ispartofissue7en_US
dc.relation.ispartofjournalBioorganic & Medicinal Chemistry Lettersen_US
dc.relation.ispartofvolume21en_US
dc.rights.retentionYen_AU
dc.subject.fieldofresearchBiologically Active Moleculesen_US
dc.subject.fieldofresearchcode030401en_US
dc.titleIdentification and evaluation of soft coral diterpenes as inhibitors of HIF-2α induced gene expressionen_US
dc.typeJournal articleen_US
dc.type.descriptionC1 - Peer Reviewed (HERDC)en_US
dc.type.codeC - Journal Articlesen_US
gro.date.issued2011
gro.hasfulltextNo Full Text


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