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- W2902287192 abstract "Significance Constitutive HIF-2α activity has been well demonstrated to promote cancer progression. A newly designed small molecule (PT2399) has been proven to inhibit HIF-2α through binding its PAS-B domain in recent studies. In the present study, we generated a mouse model featuring a cavity-filling point mutation (S305M), which fails to bind PT2399 in vivo. In addition to response to hypoxia stress, we show that HIF-2α PAS-B domain also mediates response to metabolic stress such as high fat diet, and PT2399 could ameliorate metabolic condition in obese animals, suggesting potential therapeutic applications for HIF-2α antagonists in metabolic disorders." @default.
- W2902287192 created "2018-12-11" @default.
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- W2902287192 date "2018-12-06" @default.
- W2902287192 modified "2023-09-23" @default.
- W2902287192 title "Modulation of HIF-2α PAS-B domain contributes to physiological responses" @default.
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- W2902287192 doi "https://doi.org/10.1073/pnas.1810897115" @default.
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