学习和工作经历
1983-1987 学士(化学),浙江师范大学。
1987-1990 硕士(有机化学),中国科学院上海药物研究所。
1994-1999 博士(药物化学),美国田纳西大学。
1999-2002 博士后(生物化学,特别是酶学),美国约翰霍普金斯大学医学院。
2002-2004 研究助理(Research Associate)(生物化学,特别是酶学),美国约翰霍普金斯大学医学院。
2004-2011 助理教授(The James L.and Martha J.Foght Assistant Professor,tenure-track),美国Akron大学化学系。
2007-2011 兼职助理教授,美国Akron大学综合生物科学博士点(Integrated Bioscience Ph.D. Program)
2012-至今 教授,江苏大学药学院
主要荣誉和奖励
2009 应邀主持“酶,辅酶,代谢途径”Gordon研究大会中的“染色质重造及转录”会议
2012 入选2012年度江苏特聘教授。
2012 入选2012年度江苏省“双创计划”。
研究兴趣
药物化学和化学生物学:酶促反应的化学调节剂(抑制剂和激活剂)及化学探针的发展及应用。
本课题组在美国Akron大学期间首次在世界范围内开展了发展催化机制导向的蛋白酰化赖氨酸去酰化酶sirtuin抑制剂的工作,并且发展出了三大主类催化机制导向的sirtuin抑制弹头(即硫酰胺类(thioacyl-type),硫脲类(thiourea-type),酰胺类(carboxamide-type))的原型弹头,而且最近几年发展出了迄今最为强效和/或选择性并且酶解稳定及能透过细胞膜的sirtuin抑制剂(参见:Jiang, Yanhong; Liu, Jiajia; Chen, Di; Yan, Lingling; Zheng, Weiping*. Sirtuin inhibition: strategies, inhibitors, and therapeutic potential. Trends in Pharmacological Sciences 2017,38,459-472)。迄今的研究表明该催化机制导向的设计途径代表目前最为简便但是最为有效的sirtuin抑制剂先导化合物产生(Lead Generation)的方法。本课题组在sirtuin的化学生物学、生物有机化学、药物化学领域已经建立了国际学术地位(参见:我应邀为世界著名出版集团Elsevier的系列丛书Progress in Molecular Biology and Translational Science主编了题为“Sirtuins in Health and Disease”的全英文编著(https://www.sciencedirect.com/bookseries/progress-in-molecular-biology-and-tran slational-science/vol/154/suppl/C)(2018年2月出版)。这些学术成果为往后的sirtuin研究奠定了一个扎实的基础。
本课题组的研究对于发展新型的药物(比如代谢及癌症药物)具有深远的意义。参与本课题组的研究可以得到现代药物化学和化学生物学科研理念上的熏陶以及科研技术上的装备。
Sirtuin研究的代表性学术论文(*表示为通讯作者):
1. Zheng, Weiping*. The (patho)physiological roles of the individual deacylase activities of a sirtuin. Chemical Biology & Drug Design 2024, 103, e14460.
2. Wu, Bo; Liu, Tianli; Zheng, Weiping*. A cyclic tripeptide-based human SIRT3 inhibitor. Letters in Drug Design & Discovery 2024, 21, 1611-1616.
3.Li, Renwu; Yan, Lingling; Sun, Xun*; Zheng, Weiping*. A bicyclic pentapeptide-based highly potent and selective pan-SIRT1/2/3 inhibitor harboring N(epsilon)-thioacetyl-lysine. Bioorganic & Medicinal Chemistry 2020, 28, 115356.
4. Jiang, Yanhong; Zheng, Weiping*. Cyclic tripeptide-based potent and selective human SIRT5 inhibitors. Medicinal Chemistry 2020, 16, 358-367.
5. Li, Shengchao; Wu, Bo; Zheng, Weiping*. Cyclic tripeptide-based potent human SIRT7 inhibitors. Bioorganic & Medicinal Chemistry Letters 2019, 29, 461-465.
6. Hu, Xiao; Zheng, Weiping*. Chemical probes in sirtuin research. In: Progress in Molecular Biology and Translational Science, 2018, Volume 154 (Sirtuins in Health and Disease, Edited by Weiping Zheng), Pages 1-24.
7. Li, Shengchao; Zheng, Weiping*. Mammalian sirtuins SIRT4 and SIRT7. In: Progress in Molecular Biology and Translational Science, 2018, Volume 154 (Sirtuins in Health and Disease, Edited by Weiping Zheng), Pages 147-168.
8. Jiang, Yanhong; Liu, Jiajia; Chen, Di; Yan, Lingling; Zheng, Weiping*. Sirtuin inhibition: strategies, inhibitors, and therapeutic potential. Trends in Pharmacological Sciences 2017, 38, 459-472.(Invited)
9. Chen, Di; Zheng, Weiping*. Cyclic peptide-based potent and selective SIRT1/2 dual inhibitors harboring N(epsilon)-thioacetyl-lysine. Bioorganic & Medicinal Chemistry Letters 2016, 26, 5234-5239.
10. Liu, Jiajia; Huang, Yajun; Zheng, Weiping*. A selective cyclic peptidic human SIRT5 inhibitor. Molecules 2016, 21, 1217.
11. Liu, Jiajia; Zheng, Weiping*. Cyclic peptide-based potent human SIRT6 inhibitors. Organic & Biomolecular Chemistry 2016, 14, 5928-5935.
12. Huang, Yajun; Liu, Jiajia; Yan, Lingling; Zheng, Weiping*. Simple N(epsilon)-thioacetyl-lysine-containing cyclic peptides exhibiting highly potent sirtuin inhibition. Bioorganic & Medicinal Chemistry Letters 2016, 26, 1612-1617.
13. He, Yanhua; Yan, Lingling; Zang, Wenwen; Zheng, Weiping*. Novel sirtuin inhibitory warheads derived from the N(epsilon)-acetyl-lysine analog L-2-amino-7-carboxamidoheptanoic acid. Organic & Biomolecular Chemistry 2015, 13, 10442-10450.
14. Chen, Bing; Wang, Juan; Huang, Yajun; Zheng, Weiping*. Human SIRT3 tripeptidic inhibitors containing N(epsilon)-thioacetyl-lysine. Bioorganic & Medicinal Chemistry Letters 2015, 25, 3481-3487.
15. Zang, Wenwen; Hao, Yujun; Wang, Zhenghe; Zheng, Weiping*. Novel thiourea-based sirtuin inhibitory warheads. Bioorganic & Medicinal Chemistry Letters 2015, 25, 3319-3324.
16. Chen, Bing; Zang, Wenwen; Wang, Juan; Huang, Yajun; He, Yanhua; Yan, Lingling; Liu, Jiajia; Zheng, Weiping*. The chemical biology of sirtuins. Chemical Society Reviews 2015, 44, 5246-5264.(Invited)
17. Zheng, Weiping*. Sirtuins as emerging anti-parasitic targets. European Journal of Medicinal Chemistry 2013, 59, 132-140.(Invited)
18. Hirsch, Brett M.; Hao, Yujun; Li, Xiaopeng; Wesdemiotis, Chrys; Wang, Zhenghe; Zheng, Weiping*. A mechanism-based potent sirtuin inhibitor containing N(epsilon)-thiocarbamoyl-lysine (TuAcK). Bioorganic & Medicinal Chemistry Letters 2011, 21, 4753-4757.
19. Hirsch, Brett M.; Du, Zhanwen; Li, Xiaopeng; Sylvester, Jorge A.; Wesdemiotis, Chrys; Wang, Zhenghe; Zheng, Weiping*. Potent sirtuin inhibition bestowed by L-2-amino-7-carboxamidoheptanoic acid (L-ACAH), a N(epsilon)-acetyl-lysine analog. MedChemComm 2011, 2, 291-299.
20. Fatkins, David G.; Monnot, Andrew D.; Zheng, Weiping*. N(epsilon)-thioacetyl-lysine: a multi-facet functional probe for enzymatic protein lysine N(epsilon)-deacetylation. Bioorganic & Medicinal Chemistry Letters 2006, 16, 3651-3656.
出版的论著:
1.“Sirtuins in Health and Disease”, Elsevier系列丛书Progress in Molecular Biology and Translational Science第154 卷,全英文编著(主编)(https://www.sciencedirect.com/bookseries/progress-in-molecular-biology-and-tran slational-science/vol/154/suppl/C);出版日期:2018年2月。
2.“Active Site-directed Enzyme Inhibitors: Design Concepts”,全英文独著(7.3万字) (https://books.rsc.org/books/edited-volume/2112/Active-Site-directed-Enzyme-Inhi bitorsDesign?searchresult=1);出版社:Royal Society of Chemistry;出版日期:2023年9月。