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Yancheng Yu, Fulai Yang, Quanwei Yu, Simeng Liu, Chenyang Wu, Kaijun Su, Le Yang, Xiaoqian Bao, Zhihong Li, Xiang Li,* Xiaojin Zhang.* Discovery of a potent and orally bioavailable hypoxia-inducible factor 2α (HIF-2α) agonist and its synergistic therapy with prolyl hydroxylase inhibitors for the treatment of renal anemia. Journal of Medicinal Chemistry 2021, 64 (23), 17384–17402. (supplementary cover)
Yue Wu, Zhihong Li, Michael A. McDonough, Christopher J. Schofield,* Xiaojin Zhang.* Inhibition of the oxygen-sensing asparaginyl hydroxylase factor inhibiting hypoxia-inducible factor: A potential hypoxia response modulating strategy. Journal of Medicinal Chemistry 2021, 64 (11), 7189–7209.
Pengfei Wang, Qijie Gong, Jiabo Hu, Xiang Li,* Xiaojin Zhang.* Reactive oxygen species (ROS)-responsive prodrugs, probes, and theranostic prodrugs: applications in the ROS-related diseases. Journal of Medicinal Chemistry 2021, 64 (1), 298–325.
Yancheng Yu, Quanwei Yu, Simeng Liu, Chenyang Wu, Xiaojin Zhang.* Insight into the binding mode of HIF-2 agonists through molecular dynamic simulations and biological validation. European Journal of Medicinal Chemistry 2021, 211, 112999.
Qijie Gong, Fulai Yang, Jiabao Hu, Pengfei Wang, Tian Li, Xiang Li,* Xiaojin Zhang.* Rational designed highly sensitive NQO1-activated near-infrared fluorescent probe combined with NQO1 substrates in vivo: an innovative strategy for NQO1-overexpressing cancer theranostics. European Journal of Medicinal Chemistry 2021, 224, 113707.
Qijie Gong, Quanwei Yu, Nan Wang, Jiabao Hu, Pengfei Wang, Fulai Yang, Tian Li, Qidong You,* Xiang Li,* Xiaojin Zhang.* Application of cation-π interactions in enzyme-substrate binding: design, synthesis, biological evaluation, and molecular dynamics insights of novel hydrophilic substrates for NQO1. European Journal of Medicinal Chemistry 2021, 221, 11351.
Qijie Gong, Jiabao Hu, Pengfei Wang, Xiang Li,* Xiaojin Zhang.* A comprehensive review on β-lapachone: Mechanisms, structural modifications, and therapeutic potentials. European Journal of Medicinal Chemistry 2021, 210, 112962.
Kaijun Su, Zhihong Li, Yancheng Yu, Xiaojin Zhang.* The prolyl hydroxylase inhibitor roxadustat: Paradigm in drug discovery and prospects for clinical application beyond anemia. Drug Discovery Today 2020, 25 (7), 1262–1269.
Xiaojin Zhang,* Yonghua Lei, Tianhan Hu, Yue Wu, Zhihong Li, Zhensheng Jiang, Changyong Yang, Lianshan Zhang, Qidong You.* Discovery of clinical candidate (5-(3-(4-chlorophenoxy)prop-1-yn-1-yl)-3-hydroxypicolinoyl)glycine, an orally bioavailable prolyl hydroxylase inhibitor for the treatment of anemia. Journal of Medicinal Chemistry 2020, 63 (17), 10045–10060.
Zhihong Li, Shuai Zhen, Kaijun Su, Anthony Tumber, Quanwei Yu, Ying Dong, Michael McDonough, Christopher J. Schofield,* Xiaojin Zhang.* A small-molecule probe for monitoring binding to prolyl hydroxylase domain 2 by fluorescence polarisation. Chemical Communications 2020, 56 (91), 14199–14202
Zhihong Li, Kaijun Su, Zhensheng Jiang, Yancheng Yu, Qidong You,* Xiaojin Zhang.* Photoactivatable prolyl hydroxylase 2 inhibitors for stabilizing the hypoxia-inducible factor with light. Journal of Medicinal Chemistry 2019, 62 (16), 7583−7588. (front cover)
Zhihong Li, Qidong You,* Xiaojin Zhang.* Small-molecule modulators of the hypoxia-inducible factor pathway: Development and therapeutic applications. Journal of Medicinal Chemistry 2019, 62 (12), 5725−5749.
Yancheng Yu, Quanwei Yu, Xiaojin Zhang.* Allosteric inhibition of HIF-2α as a novel therapy for clear cell renal cell carcinoma. Drug Discovery Today 2019, 24 (12), 2332−2340.
Zhensheng Jiang, Qidong You,* Xiaojin Zhang.* Medicinal chemistry of metal chelating fragments in metalloenzyme active sites: A perspective. European Journal of Medicinal Chemistry 2019, 165, 172−197.
Xingsen Wu, Xiang Li, Zhihong Li, Yancheng Yu, Qidong You,* Xiaojin Zhang.* Discovery of nonquinone substrates for NAD(P)H: quinone oxidoreductase 1 (NQO1) as effective intracellular ROS generators for the treatment of drug-resistant non-small cell lung cancer. Journal of Medicinal Chemistry 2018, 61 (24), 11280−11297. (supplementary cover)
Yue Wu, Zhensheng Jiang, Zhihong Li, Jing Gu, Qidong You,* Xiaojin Zhang.* Click chemistry–based discovery of [3-hydroxy-5-(1H-1,2,3-triazol-4-yl)picolinoyl]glycines as orally active hypoxia inducing factor prolyl hydroxylase inhibitors with favorable safety profiles for the treatment of anemia. Journal of Medicinal Chemistry 2018, 61 (12), 5332−5349.
Xian Zhang, Xiang Li, Zhihong Li, Xingsen Wu, Yue Wu, Qidong You,* Xiaojin Zhang.* An NAD(P)H: quinone oxidoreductase 1 responsive and self-immolative prodrug of 5-fluorouracil for safe and effective cancer therapy. Organic Letters 2018, 20 (12), 3635−3638.
Jinlei Bian, Xiang Li, Nan Wang, Xingsen Wu, Qidong You,* Xiaojin Zhang.* Discovery of quinone-directed antitumor agents selectively bioactivated by NQO1 over CPR with improved safety profile. European Journal of Medicinal Chemistry 2017, 129, 27−40.
Jinlei Bian, Xiang Li, Lili Xu,Nan Wang, Xue Qian, Qidong You,* Xiaojin Zhang.* Affinity-based small fluorescent probe for NAD(P)H:quinone oxidoreductase 1 (NQO1). Design, synthesis and pharmacological evaluation. European Journal of Medicinal Chemistry 2017, 127, 828−839.
Xian Zhang, Xiang Li, Qidong You,* Xiaojin Zhang.* Prodrug strategy for cancer cell-specific targeting: a recent overview. European Journal of Medicinal Chemistry 2017, 139, 542−563.