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Targeting transcription factors HIF‐2 is currently considered to be the most direct way for the therapy of clear cell renal cell carcinoma. The preclinical inhibitor PT2399 and artificial inhibitor 0X3 have been identified as promising on‐target inhibitors to inhibit the heterodimerization of HIF‐2. However, the inhibition mechanism of PT2399 and 0X3 on HIF‐2 remains unclear. To this end, molecular...
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