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專家人才

  • 姓名：吳錫山
  • 性別：男
  • 職稱：副研究員
  • 學曆：博士
  • 電話：
  • 傳真：
  • 電子郵件:wu_xishan@gibh.ac.cn
  • 通訊地址廣州市黃埔區開源大道190號

    簡曆：

  • 2023.01-至今betway体育下载 副研究員

    2020.07-2022.06betway体育下载 博士後

    2017.09-2020.06betway体育下载 博士

    研究領域：

  • 1、計算機輔助藥物設計

    2、藥物化學

    承擔科研項目情況：

  • 1.國家自然科學基金青年基金，22107102，2022.01-2024.12，30萬，主持

    2.廣東省區域聯合基金青年基金，2020A1515110793，2020.10-2023.09，10萬，主持

    3.廣東省自然科學基金麵上項目，2023A1515010418，2023.01-2025.12，10萬，主持

    4.中國科學院青年創新促進會，2023.01-2026.12，80萬，主持

    社會任職：

    獲獎及榮譽：

  • 2018年度廣東省自然科學獎二等獎（第八完成人）

    2020年中國科學院大學優秀畢業生

    2020年北京市普通高等學校優秀畢業生

    代表論著：

  • [1]Wu, X. S#.; Shen, H#.; Zhang, Y#.; Wang, C.; Li, Q.; Zhang, C.; Zhuang, X. X.; Li, C. C.; Shi, Y. D.; Xing, Y. L.; Xiang, Q. P.; Xu, J. X.; Wu, D. H.; Liu, J. S.; Xu, Y*. Discovery and characterization of benzimidazole derivative XY123 as a potent, selective, and orally available RORγ inverse agonist.J Med Chem2021, 64, 8775-8797.

    [2]Wu, X. S.; Zhang, Y.; Xu, Y*. Discovery of the first low nanomolar liver receptor homolog-1 (LRH-1) agonist.J Med Chem2019, 62, 11019-11021.

    [3]Zhang, Y#.;Wu, X. S#.; Xue, X. Q#.; Li, C. C.; Wang, J. J.; Wang, R.; Zhang, C.; Wang, C.; Shi, Y. D.; Zou, L. J.; Li, Q.; Huang, Z. H.; Hao, X. J.; Loomes, K.; Wu, D. H.; Chen, H. W.; Xu, J. X.; Xu, Y*. Discovery and characterization of XY101, a potent, selective, and orally bioavailable RORγ inverse agonist for treatment of castration-resistant prostate cancer.J Med Chem2019, 62, 4716-4730.

    [4]Wu, X. S#.; Wang, R#.; Xing, Y. L#.; Xue, X, Q.; Zhang, Y.; Lu, Y. Z.; Song, Y.; Luo, X. Y.; Wu, C.; Zhou, Y. L.; Jiang, J. Q*.; Xu, Y*. Discovery and structural optimization of 4-(4-(benzyloxy)phenyl)-3,4-dihydropyrimidin- 2(1H)-ones as RORc inverse agonists.Acta Pharmacol Sin2016, 37, 1516-1524.

    [5]Li, Q#.; Yao, B. Q#.; Zhao, S. T.; Lu, Z.; Zhang, Y.; Xiang, Q. P.;Wu, X. S.; Yu, H. N.; Zhang, C.; Li, J. H.; Zhuang, X. X.; Wu, D. H.; Li, Y*.; Xu, Y*. Discovery of a highly selective and H435R-sensitive thyroid hormone receptor β agonist.J Med Chem2022, 65, 7193-7211.

    [6]Xiang, Q. P#.; Wang, C#.; Wu, T. B#.; Zhang, C.; Hu, Q. Q.; Luo, G. L.; Hu, J. K.; Zhuang, X. X.; Zou, L. J.; Shen, H.;Wu, X. S.; Zhang, Y.; Kong, X. Q.; Liu, J. S.; 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 Chem2022, 65, 785-810.

    [7]Li, J. H#.; Zhang, C#.; Xu, H. R.; Wang, C.; Dong, R. B.; Shen, H.; Zhuang, X. X.; Chen, X. S.; Li, Q.; Lu, J. B.; Zhang, M. F.;Wu, X. S.; Loomes, K. M.; Zhou, Y. L.; Zhang, Y.; Liu, J. S.; 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 Chem2022, 65, 5760-5799.

    [8]Zhang, M. F#*.; Luo, X. Y#.; Zhang, C.; Wang, C.;Wu, X. S.; Xiang, Q. P.; 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 Pharmacol Sin2022, 0, 1-14.

    [9]Xu, H. R.; Luo, G. L.; Wu, T. B.; Hu, J. K.; Wang, C.;Wu, X. S.;Zhang, Y*.; Xu, Y*.; Xiang, Q. P*. Structural insights revealed by the cocrystal structure of CCS1477 in complex with CBP bromodomain.Biochem Biophys Res Commun2022, 623, 17-22.

    [10]Hu, Q. Q.; Wang, C.; Xiang, Q. P.; Wang, R.; Zhang, C.; Zhang, M. F.; Xue, X. Q.; Luo, G. L.; Liu, X. M.;Wu, X. S.; Zhang, Y.; Wu, D. H.; Xu Y*. Discovery and optimization of novel N-benzyl-3,6-dimethyl benzo[d]isoxazol-5-amine derivatives as potent and selective TRIM24 bromodomain inhibitors with potential anti-cancer activities.Bioorg Chem2020, 94, 103424.

    [11]Zhang, M. F#.; Zhang, Y#.; Song, M#.; Xue, X. Q.; Wang, J. J.; Wang, C.; Zhang, C.; Li, C. C.; Xiang, Q. P.; Zou, L. J.;Wu, X. S.; Wu, C.; Dong, B. J.; Xue, W.; Zhou, Y. L.; Chen, H. W.; Wu, D. H.; 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).J Med Chem2018, 61, 3037-3058.

    [12]Song, Y.; Xue, X. Q.;Wu, X. S.; Wang, R.; Xing, Y. L.; Yan, W. Q.; Zhou, Y. L.; Qian, C. N.; Zhang, Y*.; Xu Y*. Identification of N-phenyl-2-(N-phenyl phenylsulfonamido)acetamides as new RORγ inverse agonists: Virtual screening, structure-based optimization, and biological evaluation.EurJ Med Chem2016, 116, 13-26.

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