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Qiu Li#, Benqiang Yao#, Shiting Zhao, Zhou Lu, Yan Zhang, Qiuping Xiang, Xishan Wu, Haonan Yu, Cheng Zhang, Junhua Li, Xiaoxi Zhuang, Donghai Wu, Yong Li, Yong Xu. Discovery of a Highly Selective and H435R Sensitive Thyroid Hormone Receptor Agonist. J Med Chem. 2022 May 4. Doi: 10.1021/acs.jmedchem.2c00144.
Li J#, Zhang C#, Xu H, Wang C, Dong R, Shen H, Zhuang X, Chen X, Li Q, Lu J, Zhang M, Wu X, Loomes KM, Zhou Y, Zhang Y, Liu J, Xu Y. Structure- Based Discovery and Optimization of Furo[3,2-c]pyridin-4(5H)-one Derivatives as Potent and Second Bromodomain (BD2)-Selective Bromo and Extra Terminal Domain (BET) Inhibitors. J Med Chem.2022, 65, 5760-5799.
Xiang Q, Wang C, Wu T, Zhang C, Hu Q, Luo G, Hu J, Zhuang X, Zou L, Shen H, Wu X, Zhang Y, Kong X, Liu J, Xu Y. Design, Synthesis, and Biological Evaluation of 1-(Indolizin-3-yl)ethan-1-ones as CBP Bromodomain Inhibitors for the Treatment of Prostate Cancer. J Med Chem. 2022, 65, 785-810
Wu X#, Shen H#, Zhang Y#, Wang C, Li Q, Zhang C, Zhuang X, Li C, Shi Y, Xing Y, Xiang Q, Wu D, Liu J, Xu Y*. Discovery and characterization of benzimidazole derivative XY123 as a selective, and orally available ROR inverse agonist. J Med Chem. 2021, 64, 8775-8797
Wu X, Zhang Y, Xu Y*. Discovery of the First Low Nanomolar Liver Receptor Homolog-1 (LRH-1) Agonist. J Med Chem. 2019, 62, 11019-11021
Zhang Y#, Wu X#, Xue X#, Li C, Wang J, Wang R, Zhang C, Wang C, Shi Y, Zou L, Li Q, Huang Z, Hao X, Loomes K, Wu D, Chen HW, Xu J, Xu Y*. Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable ROR Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer.J Med Chem. 2019, 62, 4716-4730
Zhang M#, Zhang Y#, Song M#, Xue X, Wang J, Wang C, Zhang C, Li C, Xiang Q, Wu X, Wu C, Dong B, Xue We, Zhou Y, Chen H, Wu D, Ding K, Xu Y*. Structure-Based Discovery and Optimization of Benzo[d]isoxazole Derivatives as Potent and Selective BET Inhibitors as Potential Treatment for Castration-Resistant Prostate Cancer (CRPC). J Med Chem, 2018. 61, 3037-3058
Wang, J.; Zou, J.X.; Xue, X.; Cai, D.; Zhang, Y.; Duan, Z.; Xiang, Q.; Yang, J.C.; Louie, M.C.; Borowsky, A.D.; Gao, A.C,; Evans, C.P.; Lam, K.S.; Xu, J.; Kung, H.J.; Evans, R.M.; Xu, Y.*; Chen, H.W.*; ROR- drives androgen receptor expression and represents a therapeutic target in castration-resistant prostate cancer. Nat Med, 2016, 22: 488-496.
Xue, X#.; Zhang, Y#.; Liu, Z#.; Song, M.; Xing, Y.; Xiang, Q.; Wang, Z.; Tu, Z.; Zhou, Y.; Ding, K.; Xu Y*. Discovery of benzo[cd]indol-2(1H)-ones as potent and specific BET bromodomain inhibitors: structure-based virtual screening, optimization, and biological evaluation. J Med Chem, 2016, 59, 1565-1579
Cao, M.; Liu, X.; Zhang, Y.; Xue, X.; Zhou, X. E.; Melcher, K.; Gao, P.; Wang, F.; Zeng, L.; Zhao, Y.; Zhao, Y.; Deng, P.; Zhong, D.; Zhu, J. K.*; Xu, H. E.*; Xu, Y*. An ABA-mimicking ligand that reduces water loss and promotes drought resistance in plants.