Inhibition of dihydroorotate dehydrogenase overcomes differentiation blockade in acute myeloid leukemia

Sykes, David B., Kfoury, Youmna S., Mercier, François E., Wawer, Mathias J., Law, Jason M., Haynes, Mark K., Lewis, Timothy A., Schajnovitz, Amir +22 more·2016·Cell

DOI 10.1016/j.cell.2016.08.057

Cited by (516)

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Gergana Popova, Marcus J.G.W. Ladds, Lars Johansson, Aljona Saleh, Johanna Larsson, Lars Sandberg, Sara Häggblad Sahlberg, Weixing Qian, Hjalmar Gullberg, Neeraj Kumar Garg et al. · 2020 · Journal of Medicinal Chemistry
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Feng Qin Yin, Yonghua Ling, Jason N. Martin, Rohini Narayanaswamy, Lisa McIntosh, Fumin Li, Guowen Liu · 2020 · Journal of Pharmaceutical and Biomedical Analysis
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Donglin Ding, Alexandra M. Blee, Jianong Zhang, Yunqian Pan, Nicole A. Becker, Louis James Maher, Rafael E. Jiménez, Liguo Wang, Haojie Huang · 2023 · Nature Communications
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Siying Lyu, Nina Gildor, Qing Hua Zhang, Chengheng Liao · 2025 · Science China Life Sciences
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James F. Demarest, Maryline Kienle, RuthMabel Boytz, Mary Ayres, Eun‐Jung Kim, J. J. Patten, Donghoon Chung, Varsha V. Gandhi, Robert A. Davey, David B. Sykes et al. · 2022 · Antiviral Research
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Chunyang Yi, Jiacheng He, Dan Feng Huang, Yumiao Zhao, Chan Zhang, Xiyun Ye, Ying Huang, Ruth Nussinov, Junke Zheng, Mingyao Liu et al. · 2022 · Cell Death and Disease
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Jing Yang, Jinshuai Lan, Hongzhi Du, Xiaoling Zhang, Aiyun Li, Xinyu Zhang, Yun Liu, Jieyi Zhang, Chaochao Zhang, Yue Ding et al. · 2018 · European Journal of Pharmacology
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