姓名：叶向阳，哲学博士，研究员（博士生/硕士生导师）
办公电话：0571-28860236
指导专业：药物化学，生物学（生物化学与合成生物学）
二、研究领域
药物化学、天然产物化学、药物合成及有机方法学、化学生物学、合成生物学、创新药物的研究与开发
三、主讲课程
药物合成新技术、药学导论（药物化学，药物分析学），专利撰写概要
四、教育和工作经历
1985年9月-1989年6月，华东师范大学，理学学士
1989年9月-1992年6月，厦门大学，理学硕士学位
1992年-1995年任教厦门大学化学系
1999年获香港大学哲学博士
1999-2002年普林斯顿大学从事博士后工作
2002-2016年在美国施贵宝(Bristol-Myers Squibb) 从事创新药研发和管理15年，位至主任科学家
2018年12月起，任杭州师范大学药学院特聘研究员
五、学术简介
创新药物发明专利授权和发明申请40多项；发表SCI论文70+篇，其中以第一作者或通讯作者在药物化学及有机化学Top期刊如J. Am. Chem. Soc.,J. Med. Chem. Eur. J. Med. Chem., J. Org. Chem. Biochem. Pharma.等发表多篇论文。叶向阳是浙江省第10批省级特聘专家，杭州市级人才。2018年底入职杭州师范大学药学院，组建药学院药物化学团队。
六、主持教学科研项目
1. 杭州师范大学卓越人才启动基金：100万
2. 国家自然科学基金面上项目：82073686, 55万（2021.1.1-2024.12.31）
3. 中国科技部外国专家局项目（2020年）：G20200217005, 8万
4. 中国科技部外国专家局项目（2021年）：G2021017004, 30万
5. 中国科技部外国专家局项目（2022年）：G2022017007L， 40万
6. 杭州市“115”引进国（境）外智力项目计划项目：2020年, 20万
7. 杭州市“115”引进国（境）外智力项目计划项目：2021年, 20万
8. 杭州市“115”引进国（境）外智力项目计划项目：2022年, 30万
9. 浙江省卫生健康委项目：2023KY210，3万
10.浙江省科技厅中央引导地方科技发展基金项目：2023ZY1014，300万
11.杭州市高层次人才创新创业项目：3万
七、代表性论著
1. Yuan Gao, Jilong Duan, Xiawen Dang, Yinghui Yuan, Yu Wang, Xingrui He, Renren Bai*, Xiang-Yang Ye*, Tian Xie*. Design, synthesis and biological evaluation of novel histone deacetylase (HDAC) inhibitors derived from β-elemene scaffold. Journal of Enzyme Inhibition and Medicinal Chemistry. 2023, 38(1), 2195991.
2. Nian-Dong Mao, Yuan Gao, Xia-Wen Dang, Ji-Long Duan, Zi Hui, Hao Che, Yueying Xu, Hang Zhang, Xingrui He, Carmen Garrido, Xiang-Yang Ye*. Design, synthesis and biological evaluation of novel HDACs inhibitors based on pyrrolo [2, 3-d] pyrimidine and pyrrolo [2, 3‐b] pyridine scaffolds. ChemMedChem. 2023, e202200683.
3. Li Xu, Yuan Wang, Xingrui He, Yuan Gao, Frédéric Lirussi, Yi Zhou, Carmen Garrido*, Hang Zhang*, Tian Xie*, Xiang-Yang Ye*. Discovery of second generation heat shock protein 110 (HSP110) inhibitors for potential treatment of colorectal cancer. European Journal of Medicinal Chemistry Reports. 2023, 7, 100103.
4. Haowen Deng, Yang Ye, Renren Bai, Xuelei Zhang, Xiang-Yang Ye*, Tian Xie*, Zi Hui*. Microwave-assisted rapid synthesis of chiral oxazolines. Organic & Biomolecular Chemistry. 2023, 21(11), 2312-2319.
5. Jinyun Dong, Jilong Duan, Zi Hui, Carmen Garrido, Zhangshuang Deng, Tian Xie, Xiang-Yang Ye*. An updated patent review of protein arginine N-methyltransferase inhibitors. Expert Opinion on Therapeutic Patents. 2022, 32(12), 1185-1205.
6. Li Xu, Bing Xu, Yuan Gao, Jianshe Wang, Xingrui He*, Tian Xie*, Xiang-Yang Ye*. Recent advances of novel fourth generation EGFR inhibitors in overcoming C797S mutation of lung cancer therapy. European Journal of Medicinal Chemistry. 2023, 245(Pt 1), 114900.
7. Yuan Gao, Nian-Dong Mao, Hao Che, Li Xu, Renren Bai, Li-Wei Wang, Xiang-Yang Ye*, Tian Xie*. Novel hydroxyl carboximates derived from β-elemene: design, synthesis and anti-tumour activities evaluation. Journal of Enzyme Inhibition and Medicinal Chemistry. 2022, 37(1): 2403-2416.
8. Xiang Qi , Songwei Jiang , Zi Hui , Yuan Gao, Yang Ye, Fred´eric Lirussi, Carmen Garrido, Li Xu , Xingrui He*, Renren Bai *, Xiang-Yang Ye*, Tian Xie*. Design, synthesis and antitumor efficacy evaluation of a series of novel -elemene-based macrocycles. Bioorganic & Medicinal Chemistry Letters. 2022, 74:117049.
9. Li-Wei Wang, Songwei Jiang, Ying-Hui Yuan, Jilong Duan, Nian-Dong Mao, Zi Hui, Renren Bai*, Tian Xie*, Xiang-Yang Ye *. Recent Advances in Synergistic Antitumor Effects Exploited from the Inhibition of Ataxia Telangiectasia and RAD3-Related Protein Kinase (ATR). Molecules. 2022; 27(8):2491.
10. Suwen Hu, Zi Hui, Jilong Duan, Carmen Garrido, Tian Xie*, Xiang-Yang Ye *. Discovery of small-molecule ATR inhibitors for potential cancer treatment: a patent review from 2014 to present. Expert Opin Ther Pat. 2022; 32(4):401-421.
11. Wendremaire M, Lopez TE, Barrichon M, Hang Zhang, Hadi T, Xiang-Yang Ye, Neiers F, Bardou M, Sagot P, Garrido C, Lirussi F*. Leptin-Induced HLA-G Inhibits Myometrial Contraction and Differentiation. Cells. 2022; 11(6):954.
12. Xingrui He, Hang Zhang, Yingqian Zhang, Yang Ye, Shou Wang, Renren Bai*, Tian Xie*, Xiang-Yang Ye*. “Drug discovery of histone lysine demethylases (KDMs) inhibitors (progress from 2018 to present)”. European Journal of Medicinal Chemistry 2022, 231, 114143.
13. Xingrui He, Zi Hui, Li Xu, Renren Bai, Yuan Gao, Zongcheng Wang*, Tian Xie*, Xiang-Yang Ye*. “Medicinal chemistry updates of novel HDACs inhibitors (2020 to present)”. European Journal of Medicinal Chemistry 2022, 227, 113946.
14. Suwen Hu, Songwei Jiang, Xiang Qi, Renren Bai*, Xiang-Yang Ye*, Tian Xie*.Races of small molecule clinical trials for the treatment of COVID-19: An up-to-date comprehensive review”. Drug Development Research 2022, 83(1), 16-54. DOI:10.1002/ddr.21895.
15. Suwen Hu, Zi Hui ,Frédéric Lirussi, Carmen Garrido, Xiang-Yang Ye*, Tian Xie*. “Small molecule DNA-PK inhibitors as potential cancer therapy: a patent review (2010-present).” Expert Opinion on Therapeutic Patents 2021, 31(5), 435-452.
16. Han Zou, Tingyue Wu, Yuan Wang, Yanhua Kang, Qingye Shan, Liqing Xu, Zheyi Jiang, Xiaohan Lin, Xiang-Yang Ye*, Tian Xie,* and Hang Zhang* “5-Hydroxymethylfurfural Enhances the Antiviral Immune Response in Macrophages through the Modulation of RIG-I-Mediated Interferon Production and the JAK/STAT Signaling Pathway.” ACS Omega.2021, 6(42), 28019-28030.
17. Nian-Dong Mao#, Yang Ye#, Xiao-Tao Zhuo, Xiang-Yang Ye*, Tian Xie*.“Recent advances of the site-specifific direct methylation on aromatic rings.”Tetrahedron 2021, 96, 132402.
18. Yuan Gao, Hang Zhang, Frédéric Lirussi, Carmen Garrido, Xiang-Yang Ye*, Tian Xie* “Dual inhibitors of histone deacetylases and other cancer-related targets: A pharmacological perspective” Biochemical Pharmacology, 2020, 182:114224.
19. Zi Hui, Songwei Jiang, Xiang Qi, Xiang-Yang Ye*, Tian Xie* “Investigating the microwave-accelerated Claisen rearrangement of allyl aryl ethers: Scope of the catalysts, solvents, temperatures, and substrates” Tetrahedron Lett., 2020, 61(24), 151995.
20. Xingrui He, Xiao-Tao Zhuo, Xiang-Yang Ye*, Tian Xie* “-Elemene analogs derived from SeO2-mediated oxidative reaction” Royal Society of Open Science, 2020;7(5):200038.
21. He, Xingrui; Gao, Yuan; Hui, Zi; Shen, Guodong; Wang, Shuo; Xie, Tian*; Ye, Xiang-Yang*; 4-Hydroxy-3-methylbenzofuran-2-carbohydrazones as novel LSD1 inhibitors, Bioorganic & Medicinal Chemistry Letters, 2020, 30(10), 127109.
22. Xingrui He, Zhen Li, Tian Xie*, Xiang-Yang Ye* “Novel selective histone deacetylase 6 (HDAC6) inhibitors: a patent review (2016-2019)” Recent Patents on Anti-Cancer Drug Discovery, 2020, 15, 1-17.
23. Xingrui He#, Xiabin Chen#, Hancheng Zhang, Tian Xie*, Xiang-Yang Ye* “Selective Tyk2 inhibitors as potential therapeutic agents: a patent review (2015–2018)” Expert Opinion On Therapeutic Patents 2019, 29(2), 137-149.(被引用近40次)
24. Xiang-Yang Ye,* Stephanie Chen, Jeffrey A Robl “Discovery of Clinical Candidate 2-((2S,6S)-2-phenyl-6-hydroxyadamantan-2-yl)-1-(3'-hydroxyazetidin-1-yl)ethanone [BMS-816336], an orally active novel selective 11b-hydroxysteroid dehydrogenase type 1 inhibitor” Journal Medicinal Chemistry 2017, 60(12), 4932-4948.
25. Xiang-Yang Ye, Mei-Chu Lo, Livia Brunner, Deborah Walker, Daniel Kahne, and Suzanne Walker;* “Better Substrate for Bacterial Transglycosylases” Journal of American Chemical Society, 2001, 123, 3155−3156.
26. Dan Yang,* Xiang-Yang Ye, and Ming Xu; “Enantioselective Total Synthesis of (−)-Triptolide, (−)-Triptonide, (+)-Triptophenolide, and (+)-Triptoquinonide” Journal Organic Chemistry, 2000, 65(7), 2208−2217.
27. Dan Yang,* Xiang-Yang Ye, Ming Xu, Kwan-Wah Pang, and Kung-Kai Cheung; “Investigation of Mn(III)-Based Oxidative Free Radical Cyclization Reactions toward the Synthesis of Triptolide: The Effects of Lanthanide Triflates and Substituents on Stereoselectivity” Journal of American Chemical Society, 2000, 122(8), 1658−1663.
28. Dan Yang,* Xiang-Yang Ye, Shen Gu, and Ming Xu; “Lanthanide Triflates Catalyze Mn(III)-Based Oxidative Radical Cyclization Reactions. Enantioselective Synthesis of (−)-Triptolide, (−)-Triptonide, and (+)-Triptophenolide” Journal of American Chemical Society, 1999, 121(23), 5579−5580.
29. Dan Yang,* Xiang-Yang Ye, Ming Xu, Kwan-Wah Pang, Ning Zou, and Roy M. Letcher; A “Concise Total Synthesis of Triptolide” Journal Organic Chemistry, 1998, 63 (19), 6446–6447.
专著：
Xiang-Yang Ye & Pratik Devasthale; Chapter 6. Carboxylic Acids and Lactones as HMG-CoA Reductase Inhibitors, “Bioactive Carboxylic Compound Classes - Pharmaceuticals and Agrochemicals”, Wiley Publisher 2016.
八、专利
中国和国际专利申请和授权40项
1. 叶向阳，毛念栋，高园，车昊，张航，徐月莹，段吉隆，袁滢惠，谢恬 一种AAK1抑制剂及其制备和应用, CN202310035762.4
2. 叶向阳，谢恬，许丽，白仁仁，高园，惠子，叶杨，章映茜，王丽薇，刘丰瑞 一种组蛋白去乙酰化酶和热休克蛋白110 KDa双靶点抑制剂及应用, CN202210588856.X
3. 叶向阳，许丽，谢恬，张航，白仁仁，何兴瑞，徐月莹，谢玉娟，杜晓利，王媛一种靶向热休克蛋白110 kDa（HSP110）抑制剂及其应用, CN202210588860.6
4. 段吉隆，袁滢惠，高园，毛念栋，叶向阳，谢恬，张航，王臣臣 一种靶向降解PARP7的PROTAC化合物及其制备方法与应用, CN202211414193.6
5. 段吉隆，袁滢惠，叶向阳，谢恬，高园，惠子 具有PARP7/HDAC双靶点抑制活性的哒嗪酮衍生物及其制备方法和应用, CN202211084323.4
6. Ye, Xiang-Yang; Morales, Christian; Higgins, Mendi A.; Mull, Eric Indazole derivatives as αV integrin antagonists and their preparation WO 2018089357.
7. Ye, Xiang-Yang; Ellsworth, Bruce; Jurica, Elizabeth Preparation of pyrrolidine derivatives as GPR40 modulators WO 2015171757 A1.
8. Ye, Xiang-Yang; Wacker, Dean; Robl, Jeffrey A. Benzofuranyl Analogues as GPR119 Modulators WO2011/140161A.
9. Ye, Xiang-Yang; Wacker, Dean; Robl, Jeffrey A.; Wang, Ying Bicyclic Heteroaryl Compounds as GPR119 Modulator WO2011/140160A.
10. Ye, Xiang-Yang; Robl, Jeffrey A. Cyclic 11-β-Hydroxysteroid Dehydrogenase Type 1 Inhibitors. US7727978 (issued on June 1, 2010).
11. Ye, Xiang-Yang; Robl, Jeffrey A.; Hanson, Ronald; Guo, Zhiwei; Patel, Ramesh. Cyclic Compounds as 11-β-Hydroxysteroid Dehydrogenase Type 1 Inhibitors and Their Preparation, Pharmaceutical Compositions and Use in The Treatment of Diseases WO 2008024892 A2.
九、国际会议
2023: “Design, synthesis and structure-activity relationship of novel 2-aminopyrazine-based ATR/HDACs dual inhibitors for potential cancer therapy” American Chemical Society Fall National Meeting, San Francisco, USA, August 13-17, 2023 (presenter: Xiang-Yang Ye)
2023: “Design, synthesis and structure-activity relationship of novel pyridazinone-based PARP7/HDACs dual inhibitors for cancer treatment” American Chemical Society Fall National Meeting, San Francisco, USA, August 13-17, 2023 (presenter: Xiang-Yang Ye)
2023: “Nickel-Catalyzed Thioetherification of Vinyl Bromides and Thiols” 23rd Tetrahedron Symposium, Gothenburg, Sweden, June 27-30, 2023 (presenter: Xiang-Yang Ye)
2023: “Design, Synthesis and Biological Evaluation of Novel AAK1 Inhibitors Based on Pyrrolo[2,3-b]pyridine Scaffolds for Suppressing SARS-CoV-2 Infection” 57th RICT International Conference on Medicinal Chemistry, Lille, France, July 5-7, 2023 (presenter: Xiang-Yang Ye)