报告题目：Structure-based development of novel covalent kinase inhibitors

报 告 人：谭立 研究员（中国科学院生物与化学交叉研究中心）

时    间：2017年5月17日 下午17:00

地    点：重庆大学药学院学术报告厅

邀 请 人：朱峰 教授

报告人简历：

2016年6月至今 中国科学院生物与化学交叉研究中心，研究员，课题组长

2015年4月至2016年5月 哈佛医学院，Dana-Farber Cancer Institute，Research Scientist

2010年4月至2015年3月 哈佛医学院，Dana-Farber Cancer Institute，博士后

2009年7月至2009年12月 中国科学院上海有机化学研究所，助理研究员

2004年9月至2009年6月 中国科学院上海有机化学研究所，博士

2000年9月至2004年6月 南京大学化学化工学院，学士

代表性论文：

1. Li Tan#, Jun Wang#, Junko Tanizaki#, Zhifeng Huang#, Amir R. Aref#, Maria Rusan, Su-Jie Zhu, Yiyun Zhang, Dalia Ercan, Rachel G. Liao, Marzia Capelletti, Wenjun Zhou, Wooyoung Hur, NamDoo Kim, Taebo Sim, Suzanne Gaudet, David A. Barbie, Jing-Ruey Joanna Yeh, Cai-Hong Yun, Peter S. Hammerman*, Moosa Mohammadi*, Pasi A. Jänne*, and Nathanael S. Gray*, Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors, Proceedings of the National Academy of Sciences of the United States of America, 2014, 111(45):E4869-4877.

2. Li Tan#, Koshi Akahane#, Randall McNally, Kathleen M. S. E. Reyskens, Scott B. Ficarro, Suhu Liu, Grit S. Herter-Sprie, Shohei Koyama, Michael J. Pattison, Katherine Labella, Liv Johannessen, Esra A. Akbay, Kwok-Kin Wong, David A. Frank, Jarrod A. Marto, Thomas A. Look, J. Simon C. Arthur, Michael J. Eck, and Nathanael S. Gray*, Development of Selective Covalent Janus Kinase 3 Inhibitors, Journal of Medicinal Chemistry, 2015, 58(16):6589-6606.

3. Li Tan#, Tyzoon Nomanbhoy, Deepak Gurbani, Matthew Patricelli, John Hunter, Jiefei Geng, Lina Herhaus, Jianming Zhang, Eduardo Pauls, Youngjin Ham, Hwan Geun Choi, Ting Xie, Xianming Deng, Sara J. Buhrlage, Taebo Sim, Philip Cohen, Gopal Sapkota, Kenneth D. Westover, and Nathanael S. Gray*, Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2), Journal of Medicinal Chemistry, 2015, 58(1):183-196.

4. Hideki Terai#, Li Tan#, Ellen M. Beauchamp, John M. Hatcher, Qingsong Liu, Matthew Meyerson, Nathanael S. Gray,* and Peter S. Hammerman*, Characterization of DDR2 inhibitors for the treatment of DDR2 mutated non-small cell lung cancer, ACS Chemical Biology, 2015, 10(12):2687–2696.

5. Zhifeng Huang#, Li Tan#, Huiyan Wang#, Yang Liu, Steven Blais, Jingjing Deng, Thomas A. Neubert, Nathanael S. Gray, Xiaokun Li,* and Moosa Mohammadi*, DFG-out mode of inhibition by an irreversible type-1 inhibitor capable of overcoming gate-keeper mutations in FGF receptors, ACS Chemical Biology, 2015, 10(1):299-309.

6. Hyung-Gu Kim#, Li Tan#, Ellen L. Weisberg#, Feiyang Liu#, Peter Canning#, Hwan Geun Choi#, Scott A. Ezell, Hong Wu, Zheng Zhao, Jinhua Wang, Anna Mandinova, James D. Griffin, Alex N. Bullock, Qingsong Liu,* Sam W. Lee,* and Nathanael S. Gray*, Discovery of a Potent and Selective DDR1 Receptor Tyrosine Kinase Inhibitor, ACS Chemical Biology, 2013, 8(10):2145-2150.

7. Li Tan#, Deepak Gurbani#, Ellen L. Weisberg, John C. Hunter, Lianbo Li, Douglas S. Jones, Scott B. Ficarro, Samar Mowafy, Chun-Pong Tam, Suman Rao, Guangyan Du, James D. Griffin, Peter K. Sorger, Jarrod A. Marto, Kenneth D. Westover*, Nathanael S. Gray*, Structure-guided development of covalent TAK1 inhibitors, Bioorganic & Medicinal Chemistry, 2017, 25(3):838-846.

8. Li Tan#, Deepak Gurbani#, Ellen L. Weisberg#, Douglas S. Jones#, Suman Rao, William D. Singer, Faviola M. Bernard, Samar Mowafy, Annie Jenney, Guangyan Du, Atsushi Nonami, James D. Griffin, Douglas A. Lauffenburger, Kenneth D. Westover*, Peter K. Sorger*, Nathanael S. Gray*, Studies of TAK1-centered polypharmacology with novel covalent TAK1 inhibitors, Bioorganic & Medicinal Chemistry, 2017, 25(4):1320-1328.

9. Li Tan#, Dawei Ma*, Total synthesis of salinamide A: a potent anti-inflammatory bicyclic depsipeptide, Angewandte Chemie International Edition, 2008, 47(19):3614-3617.