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: Christopher J Ricketts, Daniel R Crooks, W Marston Linehan
• Journal: Cancer cell (Cancer Cell) Vol. 30 Issue 4 Pg. 515-517 (10 10 2016) ISSN: 1878-3686 [Electronic] United States
• PMID: 27728802 (Publication Type: Journal Article, Comment)
• Copyright: Published by Elsevier Inc.

Chemical References

• Basic Helix-Loop-Helix Transcription Factors
• Indans
• PT2399
• Sulfones
• endothelial PAS domain-containing protein 1

Topics

• Animals
• Basic Helix-Loop-Helix Transcription Factors (antagonists & inhibitors, genetics)
• Carcinoma, Renal Cell (drug therapy, genetics)
• Humans
• Indans (pharmacology)
• Kidney Neoplasms (drug therapy)
• Mice
• Mice, Nude
• Molecular Targeted Therapy
• Sulfones (pharmacology)