Rational Design and Optimization of a Potent IDO1 Proteolysis Targeting Chimera (PROTAC).

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Tác giả: Jacob M Allen, Payton Berardi, Prashant V Bommi, Sara F Dunne, Michael Egozi, Sean W Fanning, Arabela A Grigorescu, Sonam Jha, Hong Jiang, Taylor Koch, Steven Kregel, Kristen L Lauing, Rimas V Lukas, Yingyu Mao, Paige J Monsen, Oluwatomilayo Ojo, Manon Penco-Campillo, Pilar Sanchez-Gomez, Gary E Schiltz, Guiqin Song, Ali Vaziri-Gohar, Derek A Wainwright, Bakhtiar Yamini, Lijie Zhai, Fang Zhang

Ngôn ngữ: eng

Ký hiệu phân loại: 912.01 Philosophy and theory

Thông tin xuất bản: United States : Journal of medicinal chemistry , 2025

Mô tả vật lý:

Bộ sưu tập: NCBI

ID: 179688

Indoleamine 2,3-dioxygenase 1 (IDO1) is an immunosuppressive protein that inhibits antitumor immunity through both tryptophan metabolism and nonenzymatic functions. Drugs targeting IDO1 enzyme activity have failed to improve the overall survival of patients with cancer. Developing new therapeutics that neutralize both enzyme- and nonenzyme-derived immunosuppressive IDO1 effects is therefore of high interest. We previously described a novel proteolysis targeting chimera (PROTAC), NU223612, that degrades IDO1 in cultured human glioblastoma (GBM) cells, as well as in well-established brain tumors,
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