5UFP の概要
| エントリーDOI | 10.2210/pdb5ufp/pdb |
| 分子名称 | Endothelial PAS domain-containing protein 1, Aryl hydrocarbon receptor nuclear translocator, 3-({(1S)-7-[(difluoromethyl)sulfonyl]-2,2-difluoro-1-hydroxy-2,3-dihydro-1H-inden-4-yl}oxy)-5-fluorobenzonitrile, ... (4 entities in total) |
| 機能のキーワード | hif2 inhibitor hif2 ligand pas-b hypoxia inducible factor 2 epas1, transcription |
| 由来する生物種 | Homo sapiens (Human) 詳細 |
| 細胞内の位置 | Nucleus : Q99814 P27540 |
| タンパク質・核酸の鎖数 | 2 |
| 化学式量合計 | 27467.92 |
| 構造登録者 | |
| 主引用文献 | Cho, H.,Du, X.,Rizzi, J.P.,Liberzon, E.,Chakraborty, A.A.,Gao, W.,Carvo, I.,Signoretti, S.,Bruick, R.K.,Josey, J.A.,Wallace, E.M.,Kaelin, W.G. On-target efficacy of a HIF-2 alpha antagonist in preclinical kidney cancer models. Nature, 539:107-111, 2016 Cited by PubMed Abstract: 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 carcinoma cell lines display unexpectedly variable sensitivity to PT2399, however, suggesting the need for predictive biomarkers to be developed to use this approach optimally in the clinic. PubMed: 27595393DOI: 10.1038/nature19795 主引用文献が同じPDBエントリー |
| 実験手法 | X-RAY DIFFRACTION (1.9 Å) |
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