title: Targeting HIF2α in Clear-Cell Renal Cell Carcinoma.
abstract: In two recent studies, the HIF2α antagonist, PT2399, decreased HIF2α-dependent transcription and tumor growth in selected VHL-deficient clear-cell renal cell carcinoma (ccRCC) models. These studies validate HIF2α as a therapeutic target in ccRCC, reveal variable sensitivity to HIF2α antagonism, and provide the foundation for predictive biomarker-driven clinical trials.
authors.affiliation: Urologic Oncology Branch, Center for Cancer Research, National Cancer Institute, Bethesda, MD 20892-1107, USA.
authors.forename: Christopher J
authors.initials: CJ
authors.lastname: Ricketts
authors.affiliation: Urologic Oncology Branch, Center for Cancer Research, National Cancer Institute, Bethesda, MD 20892-1107, USA.
authors.forename: Daniel R
authors.initials: DR
authors.lastname: Crooks
authors.affiliation: Urologic Oncology Branch, Center for Cancer Research, National Cancer Institute, Bethesda, MD 20892-1107, USA. Electronic address: wml@nih.gov.
authors.forename: W Marston
authors.initials: WM
authors.lastname: Linehan
mesh_terms: D000818:Animals; D051792:Basic Helix-Loop-Helix Proteins / Q000037:antagonists & inhibitors* / Q000235:genetics*; D002292:Carcinoma, Renal Cell / Q000188:drug therapy* / Q000235:genetics; D006801:Humans; D007189:Indans / Q000494:pharmacology*; D007680:Kidney Neoplasms / Q000188:drug therapy*; D051379:Mice; D008819:Mice, Nude; D058990:Molecular Targeted Therapy; D013450:Sulfones / Q000494:pharmacology*; D000099162:Endothelial PAS Domain-Containing Protein 1
chemical_list: D051792:Basic Helix-Loop-Helix Proteins; D007189:Indans; D013450:Sulfones; D000099162:Endothelial PAS Domain-Containing Protein 1; C000614278:PT2399