Treatment of renal cell carcinoma: HIF antagonists

Kidney cancer. Principles and practice. Second edition. Primo N. Lara, Jr. Eric Jonasch (Editors). Springer International Publishing (2015)


The preclinical data outlined above suggest that drugs that inhibit HIF, and particularly HIF2a, would have antitumor activity in kidney cancer. Unfortunately, DNA-binding transcription factors, with the exception of the steroid hormone receptors, have historically been difficult to target with drug-like small molecules. Nonetheless, a number of approaches to targeting HIF are being explored in the laboratory, including the use of DNA-binding polyamides [172–174] and short interfering RNAs [175]. Moreover, HIF2a, but not HIF1a, has a potentially druggable pocket, and lead compounds have been identified that can inhibit HIF2a in biochemical, cell-based, and animal models [176–178].

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