On-target efficacy of a HIF-2α antagonist in preclinical kidney cancer models

@article{Cho2016OntargetEO,
  title={On-target efficacy of a HIF-2α antagonist in preclinical kidney cancer models},
  author={Hyejin Cho and Xinlin Du and James P. Rizzi and Ella Liberzon and Abhishek A Chakraborty and Wenhua Gao and Ingrid Carvo and Sabina Signoretti and Richard K. Bruick and John A. Josey and Eli M. Wallace and William G Kaelin},
  journal={Nature},
  year={2016},
  volume={539},
  pages={107-111}
}
Clear cell renal cell carcinoma, the most common form of kidney cancer, is usually linked to inactivation of the pVHL tumour suppressor protein and consequent accumulation of the HIF-2α transcription factor (also known as EPAS1). Here we show that a small molecule (PT2399) that directly inhibits HIF-2α causes tumour regression in preclinical mouse models of primary and metastatic pVHL-defective clear cell renal cell carcinoma in an on-target fashion. pVHL-defective clear cell renal cell… CONTINUE READING
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