2022年1月-至今????? ???中國科學院廣州生物醫(yī)藥與健康研究院? ?副研究員
2021年7月-2021年12月 中國科學院廣州生物醫(yī)藥與健康研究院?? 助理研究員
2019年7月-2021年6月? 中國科學院廣州生物醫(yī)藥與健康研究院?? 博士后
2016年9月-2019年6月? 中國科學院廣州生物醫(yī)藥與健康研究院?? 藥物化學?? 博士
2012年7月-2016年8月 中國科學院廣州生物醫(yī)藥與健康研究院?? 助理研究員
2009年9月-2012年6月? 遼寧師范大學化學系?????????????????? 物理化學?? 碩士
2004年9月-2009年6月? 內蒙古民族大學化學化工學院?????????? 化學教育?? 本科
1. 分子模擬與藥物設計
2. 結構生物學
3. 藥物化學
1. 國家自然科學基金青年基金,21602222,201601-201912,24萬,主持
2. 中科院特別研究助理資助項目,201907-202209,60萬,主持
3. 呼吸疾病國家重點實驗室自主項目,SKLRD-Z-202018,202001-202212,20萬,主持
4. 中國博士后科學基金面上項目,2020M672857,202004-202106,8萬,主持
5. 廣東省自然科學基金面上項目,2020A1515010250,201910-202209,10萬,主持
6. 廣州市基礎研究計劃基礎與應用基礎研究項目,202102080215,202104-202303,5萬,主持
?
2018年度廣東省自然科學獎二等獎(第二完成人)
2019年獲得中國科學院特別研究助理稱號
2019年度中國科學院優(yōu)秀畢業(yè)生
2019年度北京市普通高等學校優(yōu)秀畢業(yè)生
[1]????? Zhang, M#.; Luo, X#.; Zhang, C.; Wang, C.; Wu, X.; Xiang, Q.; Xu, Y*.; Zhang, Y*. Design, synthesis and pharmacological characterization of N-(3-ethylbenzo[d]isoxazol-5-yl) sulfonamide derivatives as BRD4 inhibitors against acute myeloid leukemia. Acta Pharmacologica Sinica 2022, doi: 10.1038/s41401-022-00881-y.
[2]????? Wu, T#.; Xiang, Q#.; Wang, C#.; Wu, C.; Zhang, C.; Zhang, M.; Liu, Z.; Zhang, Y*.; Xiao, L*.; Xu Y*. Y06014 is a selective BET inhibitor for the treatment of prostate cancer. Acta Pharmacologica Sinica 2021, 64, 8775-8797.
[3]????? Song, Y.; Xue, X.; Wu, X.; Wang, R.; Xing, Y.; Yan, W.; Zhou, Y.; Qian, C-N.; Zhang, Y.*; Xu, Y.*; Identification of N-phenyl-2-(N-phenylphenylsulfonamido) Acetamides as New RORγ Inverse Agonists: Virtual Screening, Structure-based Optimization, and Biological Evaluation. European Journal of Medicinal Chemistry2016, 116, 13-26.
[4]????? Wu, X#.; Shen, H#.; Zhang, Y#.; Wang, C.; Li, Q.; Zhang, C.; Zhuang, X.; Li, C.; Shi, Y.; Xing, Y.; Xiang, Q.; Xu, J.; Wu, D.; Liu, J.; Xu, Y*.? Discovery and Characterization of Benzimidazole Derivative XY123 as a Potent, Selective, and Orally Available RORγ Inverse Agonist. Journal of Medicinal Chemistry 2021, 64, 8775-8797.
[5]????? 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, H.; Xu, J.; Xu, Y.* Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable RORγ Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer. Journal of Medicinal Chemistry 2019, 62, 4716-4730.
[6]????? Zhang, M#.; Zhang, Y#.; Song, M#.; Xue, X.; Wang, J.; Wang, C.; Zhang, C.; Li, C.; Xiang, Q.; Zou, L.; Wu, X.; Wu, C.; Dong, B.; Xue, W.; 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 for Potential Treatment of Castration-Resistant Prostate Cancer (CRPC). Journal of Medicinal Chemistry 2018. 61, 3037-3058.
[7]????? Xiang, Q#.; Zhang, Y#.; Li, J#.; Xue, X.; Wang, C.; Song, M.; Zhang, Z.; Wang, R.; Li, C.; Wu, C.; Zhou, Y.; Yang, X.; Li, G.; Ding, K.; Xu, Y.* Y08060: A selective BET inhibitor for treatment of prostate cancer. ACS Medicinal Chemistry Letters 2018, 9, 262-267.
[8]????? 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. Journal of Medicinal Chemistry 2016. 59, 1565-1579.
[9]????? Zhang, Y.; Luo, X. Y.; Wu, D. H.*; Xu, Y.* ROR nuclear receptors: structures, related diseases, and drug discovery. Acta Pharmacologica Sinica 2015, 36, 71-87.
[10]?? Zhang, Y#.; Xue, X#.; Jin, X.; Song, Y.; Li, J.; Luo, X.; Song, M.; Yan, W.; Song, H.; Xu, Y.* Discovery of 2-oxo-1,2-dihydrobenzo[cd]indole-6-sulfonamide derivatives as new RORgamma inhibitors using virtual screening, synthesis and biological evaluation. European Journal of Medicinal Chemistry 2014, 78, 431-441.
[11]?? 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. Journal of Medicinal Chemistry 2022, 65, 5760-5799.
[12]?? Li, W#.; Zhang, C#.; Zhang, H.; Dong, R.; Liu, J.; Wang, C.; Wang, M.; Wang, Y.; Wang, C.; Zhang, Y.; Shi, L.; Xu, Y*.; Sun, L*. Design, synthesis, and anticancer evaluation of ammosamide B with pyrroloquinoline derivatives as novel BRD4 inhibitors. Bioorganic Chemistry 2022, 127, 105917.
[13]?? Xiang, Q#.; Luo, G#.; Zhang, C.; Hu, Q.; Wang, C.; Wu, T.; Xu, H.; Hu, J.; Zhuang, X.; Zhang, M.;Wu, S.; Xu, J.; Zhang, Y.; Liu, J.; Xu, Y*. Discovery, optimization and evaluation of 1-(indolin-1-yl)ethan-1-ones as novel selective TRIM24/BRPF1 bromodomain inhibitors. European Journal of Medicinal Chemistry 2022, 236, 114311.
[14]?? 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. Journal of Medicinal Chemistry 2022, 65, 785-810.
[15]?? Li, Q#.; Yao, B#.; Zhao, S.; Lu, Z.; Zhang, Y.; Xiang, Q.; Wu, X.; Yu, H.; Zhang, C.; Li, J.; Zhuang, X.; Wu, D.; Li, Y*.; Xu, Y*. Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist. Journal of Medicinal Chemistry 2022, 65, 7193-7211.
[16]?? Wu, X.; Zhang, Y.; Xu, Y.* Discovery of the First Low Nanomolar Liver Receptor Homolog-1 (LRH-1) Agonist. Journal of Medicinal Chemistry 2019, 62, 11019-11021.
[17]?? Hu Q.; Wang C.; Xiang Q.; Wang R.; Zhang C.; Zhang M.; Xue X.; Luo G.; Liu X.; Wu X.; Zhang, Y.; Wu, D.; Xu, Y.* Discovery and optimization of novel N-benzyl-3,6-dimethylbenzo [d] isoxazol-5-amine derivatives as potent and selective TRIM24 bromodomain inhibitors with potential anti-cancer activities. Bioorganic Chemistry 2019, 94, 103424.
[18]?? Peng, L.; Zhang, Z.; Lei, C.; Li, S.; Zhang, Z.; Ren, X.; Chang, Y.; Zhang, Y.; Xu, Y.; Ding, K. Identification of New Small-Molecule Inducers of Estrogen-related Receptor α (ERRα) Degradation. ACS Medicinal Chemistry Letters 2019, 10, 767-772.
[19]?? Zou, L#.; Xiang, Q.; Xue, X.; Zhang, C.; Li, C.; Wang, C.; Li, Q.; Wang, R.; Wu, S.; Zhou, Y.; Zhang, Y.; Xu, Y.* Y08197 is a Novel and Selective CBP and EP300 Bromodomain Inhibitor for Treatment of Prostate Cancer. Acta Pharmacologica Sinica 2019, 40, 1436-1447.
[20]?? Xue, X.; Zhang, Y.; Wang, C.; Zhang, M.; Xiang, Q.; Wang, J.; Wang, A.; Li, C.; Zhang, C.; Zou, L.; Wang, R.; Wu, S.; Lu, Y.; Chen, H.; Ding, K.; Li, G.; Xu, Y.* Benzoxazinone-containing 3,5-Dimethylisoxazole Derivatives as BET Bromodomain Inhibitors for Treatment of Castration-Resistant Prostate Cancer. European Journal of Medicinal Chemistry 2018, 152, 542-559.
[21]?? Xiang, Q#.; Wang, C#.; Zhang, Y.; Xue, X.; Song, M.; Zhang, C.; Li, C.; Wu, C.; Li, K.; Hui, X.; Zhou, Y.; Smaill, JB.; Patterson, AV.; Wu, D.; Ding, K.; Xu, Y.* Discovery and optimization of 1-(1H-indol-1-yl)ethanone derivatives as CBP/EP300 bromodomain inhibitors for the treatment of castration-resistant prostate cancer.European Journal of Medicinal Chemistry 2018, 147, 238-252.
[22]?? Li, H.; Zhao, L.; Singh, R.; Ham, JN.; Fadoju, DO.; Bean, LJH.; Zhang, Y.; Xu, Y.; Xu, HE.; Gambello MJ. The First Pediatric Case of Glucagon Receptor Defect Due to Biallelic Mutations in GCGR is Identified by Newborn Screening of Elevated Arginine. Molecular Genetics and Metabolism Reports 2018, 17, 46-52.
[23]?? 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-γ drives androgen receptor expression and represents a therapeutic target in castration-resistant prostate cancer. Nature Medicine 2016, 22, 488-496.
[24]?? Wu, X#.; Wang, R#.; Xing, Y#.; Xue, X.; Zhang, Y.; Lu, Y.; Song, Y.; Luo, X.; Wu, C.; Zhou, Y.; Jiang, J.*; Xu, Y.* Discovery and structural optimization of 4-(4-(benzyloxy)phenyl)-3,4-dihydropyrimidin-2(1H)-ones as RORc inverse agonists. Acta Pharmacologica Sinica 2016, 37, 1516-1524.
[25]?? Zhou, Y#.; Nie, T#.; Zhang, Y.; Song, M.; Li, K.; Ding, M.; Ding, K.; Wu, D.*; Xu, Y.* The discovery of novel and selective fatty acid binding protein 4 inhibitors by virtual screening and biological evaluation. Bioorganic & Medicinal Chemistry2016, 24, 4310-4317.
[26]?? Chang, Y.; Lu, X.; Shibu, MA.; Dai, YB.; Luo, J.; Zhang, Y.; Li, Y.; Zhao, P.; Zhang, Z.; Xu, Y.; Tu, ZC.; Zhang, QW.; Yun, CH.; Huang, CY.; Ding, K. Structure based design of N-(3-((1H-Pyrazolo[3,4-b]pyridin-5-yl)ethynyl)benzenesulfonamides as selective leucine-zipper and sterile-α motif kinase (ZAK) inhibitors. Journal of Medicinal Chemistry 2017, 60, 5927-5932.
[27]?? Gao, M.; Duan, L.; Luo, J.; Zhang, L.; Lu, X.; Zhang, Y.; Zhang, Z.; Tu, Z.; Xu, Y.; Ren, X.; Ding, K. Discovery and optimization of 3-(2-(Pyrazolo[1,5-a] pyrimidin-6-yl)ethynyl)benzamides as novel selective and orally bioavailable discoidin domain receptor 1 (DDR1) inhibitors. Journal of Medicinal Chemistry 2013, 56, 3281-3295.
[28]?? 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. Cell Research 2013, 23, 1043-1054.