许永
编辑:综合办公室     发布时间:2022-04-07

许永 男,研究员,博士生导师,1975年生

简历:

1998.9 – 2001.7 硕士, 辽宁师范大学化学系

2001.9 – 2004.7 博士, 药物发现与设计中心,中国科学院上海药物研究所

2004.8 – 2006.5 博士后,生命有机国家重点实验室,中国科学院上海有机化学研究所

2006.6 – 2011.8 博士后,结构生物学与药物发现中心,美国Van Andel研究所

2011.9 – 至今 研究员,中国科学院广州生物医药与健康研究院,化学生物学与药物研究中心主任,中科院百人计划

研究领域:

运用计算生物学、药物化学和结构生物学等方法研究生物大分子的结构与功能以及生物大分子与小分子间的相互作用,在此基础上针对重要靶标进行药物分子设计研究。

学术奖励:

2018年 广东省自然科学奖二等奖

2020年 国务院政府特殊津贴

 

代表论著:

在国际期刊NatureScienceNature MedicineNature Structural & Molecular BiologyCell ResearchScience SignalingJournal of Medicinal Chemistry等杂志上发表论80余篇。

发表论文

1. Xiang QP, Wang C, Wu TB, Zhang C, Hu QQ, Luo GL, Hu JK, Zhuang XX, Zou LJ, Shen H, Wu XS, Zhang Y, Kong XQ, Liu JS, 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.

2. Wu TB, Xiang QP, Wang C, Wu C, Zhang C, Zhang MF, Liu ZX, Zhang Y, Xiao LJ, Xu Y*. Y06014 is a selective BET inhibitor for the treatment of prostate cancer. Acta Pharmacol Sin, 2021, 42, 2120-2131.

3. Hu QQ, Wang C, Xiang QP, Zhang C, Zhang MF, Xue XQ, Luo GL, Liu XM, Wu XS, Zhang Y, Wu DH, 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, 2020, 94, 103424.

4. 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.

5. Zou LJ#, Xiang QP#, Xue XQ#, Zhang C, Li CC, Wang C, Li Q, Wang R, Wu S, Zhou YL, Zhang Y, Xu Y*. Y08197 is a novel and selective CBP/EP300 bromodomain inhibitor for the treatment of prostate cancer. Acta Pharmacol Sin. 2019, 40, 1436-1447.

6. 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 RORγ Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer. J Med Chem. 2019, 62, 4716-4730.

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 Med Chem Lett, 2018, 9, 262-267.

8. Xue X, Zhang Y, Wang C Zhang M, Xiang Q, Wang J, Wang A, Li C, Zhang C, Zou L, Wang R, Wu X, 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. Eur J Med Chem. 2018, 152, 542-559.

9. 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.

10. 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. Eur J Med Chem. 2018, 147, 238-252.

13. Wu XS, Wang R, Xing YL, Xue XQ, Zhang Y, Lu YZ, Song Y, Luo XY, Wu C, Zhou YL, Jiang JQ*, Xu Y*. Discovery and structural optimization of 4-(4-(benzyloxy)phenyl)-3,4-dihydropyrimidin-2(1H)-ones as RORc inverse agonists.

Acta Pharmacol Sin, 2016, 37: 1516-1524.

14. Song Y, Xue X, Wu X, Wang R, Xing Y, Yan W, Zhou Y, Qian, CN, 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. Eur J Med Chem, 2016, 116, 13-26.

15. Wang J, Zou JX, Xue X, Cai D, Zhang Y, Duan Z, Xiang Q, Yang JC, Louie, MC, Borowsky AD, Gao AC, Evans CP, Lam KS, Xu J, Kung HJ, Evans RM, Xu Y*, Chen HW*. ROR-γ drives androgen receptor expression and represents a therapeutic target in castration-resistant prostate cancer.  Nat Med, 2016, 22: 488-496. (Highlighted by Nature, Nature Review Urology)

18. Cao M, Liu X, Zhang Y, Xue X, Zhou XE, Melcher K, Gao P, Wang F, Zeng L, Zhao Y, Zhao Y, Deng P, Zhong D, Zhu JK, Xu HE*, Xu, Y*. An ABA-mimicking ligand that reduces water loss and promotes drought resistance in plants.  Cell Res, 2013, 23, 1043-1054. (Highlighted by Nature Review Genetics)