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

  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},
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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Development of inhibitors of the PASB domain of the HIF2 alpha transcription factor

  • J. L. Rogers
  • J Med Chem
  • 2013

HIF 2 alpha inhibition promotes p 53 pathway activity , tumor cell death , and radiation responses

  • A. M. Roberts
  • Proc Natl Acad Sci U S A
  • 2009

Suppression of hypoxiainducible factor 2 alpha restores p 53 activity via Hdm 2 and reverses chemoresistance of renal carcinoma cells

  • A. P. Fay
  • Cancer Res
  • 2009

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