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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:发展机制导向的(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。

本着这些研究兴趣,本课题组在美国Akron大学期间首次在全球范围内开展了发展机制导向的蛋白酰化赖氨酸去酰化酶sirtuin抑制剂的工作,并且发现了首例也是迄今为止最为有效的sirtuin催化活性的机制导向抑制弹头硫乙酰赖氨酸。现已证明该机制导向的研究途径代表目前最为简便且最为有效的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(主要参考文献是应邀的CSR文章: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)。 

本课题组近年与美国Case Western Reserve大学Zhenghe Wang教授课题组成功地鉴定出一个新型的癌症药物靶点(参考文献: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 p110α helical domain mutants is crucial for their oncogenic functions. Cancer Cell 2013, 23, 583-593)。此项研究得到了世界癌症研究同行的普遍关注(主要参考文献: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)。

 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。

 

本课题组现已发表的学术论文(*表示为通讯作者)

  1. He, Yanhua; Yan, Lingling; Zang, Wenwen; Zheng, Weiping*. Novel sirtuin inhibitory warheads derived from the N(ε)-acetyl-lysine analog l-2-amino-7-carboxamidoheptanoic acid. Organic & Biomolecular Chemistry 2015, 13, 10442-10450.
  2. Chen, Bing; Wang, Juan; Huang, Yajun; Zheng, Weiping*. Human SIRT3 tripeptidic inhibitors containing N(ε)-thioacetyl-lysine. Bioorganic & Medicinal Chemistry Letters 2015, 25, 3481-3487. 
  3. Zang, Wenwen; Hao, Yujun; Wang, Zhenghe; Zheng, Weiping*. Novel thiourea-based sirtuin inhibitory warheads. Bioorganic & Medicinal Chemistry Letters 2015, 25, 3319-3324. 
  4. 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.(应邀)
  5. 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.(应邀)
  6. Zheng, Weiping*. Mechanism-based modulator discovery for sirtuin-catalyzed deacetylation reaction. Mini Reviews in Medicinal Chemistry 2013, 13, 132-154.(应邀)
  7. Zheng, Weiping*. Sirtuins as emerging anti-parasitic targets. European Journal of Medicinal Chemistry 2013, 59, 132-140.(应邀)
  8. 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 p110α helical domain mutants is crucial for their oncogenic functions. Cancer Cell 2013, 23, 583-593. (Comment (评论) 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)
  9. Zheng, Weiping*. Sulfur-based mechanistic probes for enzyme-catalyzed reactions. Current Medicinal Chemistry 2013, 20, 3743-3758.(应邀)
  10. Zheng, Weiping*; Huang, Yajun. The chemistry and biology of the a-ketoglutarate-dependent histone Ne-methyl-lysine demethylases. MedChemComm 2014, 5, 297-313. (应邀, for the themed issue(特刊)on Chemical Biology for Target Identification and Validation, guest edited by Dr. Nathanael Gray (a professor at Harvard University, USA) and Dr. Lyn Jones (a scientist at Pfizer, Cambridge, USA).
  11. Hirsch, Brett M.; Hao, Yujun; Li, Xiaopeng; Wesdemiotis, Chrys; Wang, Zhenghe; Zheng, Weiping*. A mechanism-based potent sirtuin inhibitor containing Ne-thiocarbamoyl-lysine (TuAcK). Bioorganic & Medicinal Chemistry Letters 2011, 21, 4753-4757.
  12. 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 Ne-acetyl-lysine analog. MedChemComm 2011, 2, 291-299.
  13. Hirsch, Brett M.; Zheng, Weiping*. Sirtuin mechanism and inhibition: explored with Ne-acetyl-lysine analogs. Molecular Biosystems 2011, 7, 16-28. (应邀, for the themed issue(特刊)on Post-translational Modifications, guest edited by Dr. Hening Lin (a professor at Cornell University, USA) and Dr. Tadhg Begley (a professor at Texas A&M University, USA).
  14. Hirsch, Brett M.; Gallo, Caroline A.; Du, Zhanwen; Wang, Zhenghe; Zheng, Weiping*. Discovery of potent, proteolytically stable, and cell permeable human sirtuin peptidomimetic inhibitors containing Ne-thioacetyl-lysine. MedChemComm 2010, 1, 233-238.
  15. Zhao, Yiqing; Zhang, Xiaodong; Guda, Kishore; Lawrence, Earl; Sun, Qun; Watanabe, Toshio; Iwakura, Yoichiro; Asano, Masahide; Wei, Lanlan; Yang, Zhirong; Zheng, Weiping; Dawson, Dawn; Willis, Joseph; Markowitz, Sanford; Satake, Masanobu; Wang, Zhenghe*. Identification and functional characterization of paxillin as a target of protein tyrosine phosphatase receptor T. Proceedings of the National Academy of Sciences of USA 2010, 107, 2592-2597.
  16. Jamonnak, Nuttara; Hirsch, Brett M.; Pang, Yi; Zheng, Weiping*. Substrate specificity of SIRT1-catalyzed lysine Ne-deacetylation reaction probed with the side chain modified Ne-acetyl-lysine analogs. Bioorganic Chemistry 2010, 38, 17-25.
  17. Hawse, William F.; Hoff, Kevin G.; Fatkins, David G.; Daines, Alison; Zubkova, Olga V.; Schramm, Vern L.; Zheng, Weiping; Wolberger, Cynthia*. Structural insights into intermediate steps in the Sir2 deacetylation reaction. Structure 2008, 16, 1368-1377.
  18. Wei, Lanlan; Jamonnak, Nuttara; Choy, Jeremy; Wang, Zhenghe; Zheng, Weiping*. Differential binding modes of the bromodomains of CREB-binding protein (CBP) and p300 with acetylated MyoD. Biochemical and Biophysical Research Communications 2008, 368, 279-284.
  19. Fatkins, David G.; Zheng, Weiping*. Substituting Ne-thioacetyl-lysine for Ne-acetyl-lysine in peptide substrates as a general approach to inhibiting human NAD+-dependent protein deacetylases. International Journal of Molecular Sciences 2008, 9, 1-11.
  20. Fatkins, David G.; Zheng, Weiping*. A spectrophotometric assay for histone deacetylase 8. Analytical Biochemistry 2008, 372, 82-88.
  21. Liu, Qin*; Londraville, Richard; Marrs, James A.; Wilson, Amy L.; Mbimba, Thomas; Murakami, T.; Kubota, F.; Zheng, Weiping; Fatkins, David G. Cadherin-6 function in zebrafish retinal development. Developmental Neurobiology 2008, 68, 1107-1122.
  22. Zhang, Xiaodong; Guo, Ailan; Yu, Jianshi; Possemato, Anthony;Chen, Yueting;Zheng, Weiping; Polakiewicz, Roberto D.; Kinzler, Kenneth W.; Vogelstein, Bert; Velculescu, Victor E.; Wang, Zhenghe John*. Identification of STAT3 as a substrate of receptor protein tyrosine phosphatase T. Proceedings of the National Academy of Sciences of USA 2007, 104, 4060-4064.
  23. Jamonnak, Nuttara; Fatkins, David G.; Wei, Lanlan; Zheng, Weiping*. Ne-methanesulfonyl-lysine as a non-hydrolyzable functional surrogate for Ne-acetyl-lysine. Organic & Biomolecular Chemistry 2007, 5, 892-896.
  24. Fatkins, David G.; Monnot, Andrew D.; Zheng, Weiping*. Ne-thioacetyl-lysine: a multi-facet functional probe for enzymatic protein lysine Ne-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。