2022年1月-至今betway体育下载 副研究員

2021年7月-2021年12月betway体育下载 助理研究員

2019年7月-2021年6月betway体育下载 博士後

2016年9月-2019年6月betway体育下载 藥物化學博士

2012年7月-2016年8月betway体育下载 助理研究員

2009年9月-2012年6月遼寧師範大學化學係物理化學碩士

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.中國博士後科學基金麵上項目，2020M672857，202004-202106，8萬，主持

5.廣東省自然科學基金麵上項目，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年度中國科學院優秀畢業生

2019年度北京市普通高等學校優秀畢業生

[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 Sinica2022, 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 Sinica2021,64, 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 Chemistry2021, 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 Chemistry2019, 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 Chemistry2018. 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 Letters2018, 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 Chemistry2016. 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 Sinica2015, 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 Chemistry2014, 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 Chemistry2022, 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 Chemistry2022, 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 Chemistry2022, 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 Chemistry2022, 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 Chemistry2022, 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 Chemistry2019, 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 Chemistry2019,94, 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 Letters2019, 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 Sinica2019, 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 Chemistry2018, 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 Chemistry2018,147, 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 MetabolismReports2018,17, 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 Medicine2016,22, 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 Sinica2016, 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 Chemistry2017, 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 Chemistry2013, 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 Research2013, 23, 1043-1054.