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郑卫平 教授

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:发展催化机制导向的(catalytic mechanism-based)酶抑制剂;发展酶催化反应的化学探针(activity-based chemical probe)并探索其在生物学和药物化学研究中的应用;新型肽装订(peptide stapling)途径的发展并探索其在药物化学研究中的应用。

本着这些研究兴趣,本课题组在美国Akron大学期间首次在世界范围内开展了针对在生理医学上非常重要的蛋白酰化赖氨酸去酰化酶sirtuin发展催化机制导向的抑制剂的工作,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,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”的专著(https://www.sciencedirect.com/science/bookseries/18771173,2018年2月出版))。

本课题组近年与美国Case Western Reserve大学Zhenghe Wang教授课题组合作成功地鉴定出一个新型的只存在于某些结肠癌细胞内的基于蛋白-蛋白相互作用(protein-protein interaction, PPI)的癌症药物靶点(参见:Hao, Yujun; Wang, Chao; Cao, Bo; Hirsch, Brett M.; Song, Jing; Markowitz, Sanford D.; Ewing, Rob M.; Sedwick, David; Liu, Lili; Zheng, Weiping*; Wang, Zhenghe*. Gain of interaction with IRS1 by p110alpha helical domain mutants is crucial for their oncogenic functions. Cancer Cell 2013, 23, 583-593;评论文章:John E. Burke and Roger L. Williams (MRC Laboratory of Molecular Biology, Cambridge, UK). Connecting with an old partner in a new way. Cancer Cell 2013, 23, 559-561)。虽然在这项研究中运用已知的全碳氢链肽装订(all-hydrocarbon peptide stapling)途径发展出了一个强效且能透过细胞膜的该PPI的抑制剂,我们有兴趣发展新型且更优越的肽装订途径以运用到这项研究中以及整个药物化学的范畴中。

本课题组的研究对于发展新型的药物(特别是抗癌药物)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科研理念上的熏陶以及科研技术上的装备。

 

代表性学术论文(*表示为通讯作者)

 

1.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.

2.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.

3.Hu, Xiao; He, Yanhua; Wu, Liping; Hao, Yujun; Wang, Zhenghe; Zheng, Weiping*. Novel all-hydrocarbon stapled p110alpha[E545K] peptides as blockers of the oncogenic p110alpha[E545K]-IRS1 interaction. Bioorganic & Medicinal Chemistry Letters 2017, 27, 5446-5449.

4.Mukhtar, Yusif M.; Huang, Yajun; Liu, Jiajia; Chen, Di; Zheng, Weiping*. Acetanilide and bromoacetyl-lysine derivatives as activators for human histone deacetylase 8. Bioorganic & Medicinal Chemistry Letters 2017, 27, 2319-2323.

5.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)

6.Wang, Juan; Zang, Wenwen; Liu, Jiajia; Zheng, Weiping*. Bivalent SIRT1 inhibitors. Bioorganic & Medicinal Chemistry Letters 2017, 27, 180-186.

7.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.

8.Liu, Jiajia; Huang, Yajun; Zheng, Weiping*. A selective cyclic peptidic human SIRT5 inhibitor. Molecules 2016, 21, 1217.

9.Liu, Jiajia; Zheng, Weiping*. Cyclic peptide-based potent human SIRT6 inhibitors. Organic & Biomolecular Chemistry 2016, 14, 5928-5935.

10.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.

11.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.

12.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.

13.Zang, Wenwen; Hao, Yujun; Wang, Zhenghe; Zheng, Weiping*. Novel thiourea-based sirtuin inhibitory warheads. Bioorganic & Medicinal Chemistry Letters 2015, 25, 3319-3324.

14.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)

15.He, Yanhua; Chen, Di; Zheng, Weiping*. An enhanced functional interrogation/ manipulation of intracellular signaling pathways with the peptide “stapling” technology. Oncogene 2015, 34, 5685-5698. (Invited)

16.Zheng, Weiping*; Huang, Yajun. The chemistry and biology of the alpha-ketoglutarate- dependent histone N(epsilon)-methyl-lysine demethylases. MedChemComm 2014, 5, 297-313. (Invited for the themed issue on Chemical Biology for Target Identification and Validation, guest edited by Prof. Nathanael Gray (Harvard University, U.S.A.) and Dr. Lyn Jones (Pfizer, Cambridge, U.S.A.).

17.Zheng, Weiping*. Sirtuins as emerging anti-parasitic targets. European Journal of Medicinal Chemistry 2013, 59, 132-140. (Invited)

18.Hao, Yujun; Wang, Chao; Cao, Bo; Hirsch, Brett M.; Song, Jing; Markowitz, Sanford D.; Ewing, Rob M.; Sedwick, David; Liu, Lili; Zheng, Weiping*; Wang, Zhenghe*. Gain of interaction with IRS1 by p110alpha helical domain mutants is crucial for their oncogenic functions. Cancer Cell 2013, 23, 583-593. (Comment by John E. Burke and Roger L. Williams (MRC Laboratory of Molecular Biology, Cambridge, UK) in: Connecting with an old partner in a new way. Cancer Cell 2013, 23, 559-561)

19.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.

20.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.

21.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.

 

 

联系方式

电子信箱: wzheng@ujs.edu.cn

通讯地址:江苏省镇江市学府路301号,江苏大学药学院,邮编 212013。