时间：2021年11月4日（周四）下午16:00-17:30

Time：16:00-17:30, Thursday, Nov 4, 2021

主持人: 西湖大学理学院PI 吴明轩 博士

Host: Dr. Mingxuan Wu, PI of School of Science, Westlake University

地址：西湖大学云栖校区5号楼一楼学术报告厅

Venue: Lecture Hall, 1F, Building 5, Yunqi Campus

陈弓 教授

南开大学化学学院

Prof. Gong Chen

State Key Laboratory of Elemento-organic Chemistry, Nankai University, China

主讲人/Speaker：

Dr. Gong Chen received his Bachelor from Nanjing University in 1998 and Ph.D. from Columbia University in 2004. After postdoctoral training at Memorial Sloan-Kettering Cancer Center in USA, he joined the Department of Chemistry, the Pennsylvania State University in 2008, where he acquired the position of Associate professor in 2014. He joined State Key Laboratory of Elemento-organic Chemistry, Nankai University in 2015. The main focus of his research is on organic synthesis and chemical biology study of complex peptides and oligosaccharides.

讲座摘要/Abstract:

Peptide macrocycles have emerged as a powerful platform for drug discovery, especially for biological targets that are difficult to modulate by conventional small molecule drugs. To realize the full potential of this platform, new strategies are needed to streamline the synthesis of peptide macrocycles with novel structures. We will discuss 1) exploration of palladium-catalyzed C−H functionalization strategy for total synthesis of complex peptide natural products and construction of cyclophane-braced peptide macrocycles; 2) a metal-free cooperative stapling method of native peptides at lysine and tyrosine or arginine with formaldehyde; 3) a recent development of Pd-catalyzed intramolecular S-Arylation reaction to assemble complex peptide structures for synthesis and biological screening of DNA-encoded library.

References:

[1]   Zhang, X.; Lu, G.; Sun, M.; Hahankali, M.; Ma, Y.; Zhang, M.; Hua, W.; Hu, Y.; Wang, Q.; Chen, J.; He, G.; Qi, X.; Shen, W.; Liu, P.; Chen, G. A General Strategy for Synthesis of Cyclophane-Braced Peptide Macrocycles via Palladium-Catalyzed Intramolecular sp³ C−H Arylation. Nat. Chem. 2018, 10, 543.

[2]   Li, B.; Li, X.; Han, B.; Chen, Z.; Zhang, X.; He, G.; Chen, G. Construction of Natural-Product-Like Cyclophane-Braced Peptide Macrocycles via sp³ C−H Arylation. J. Am. Chem. Soc. 2019, 141, 9401.

[3]   Li, B.; Tang, H.; Turlik, A.; Wan, Z.; Xue, X.-S.; Li, L.; Yang, X.; Li, J.; He，G.; Houk, K.N.; Chen, G. Cooperative Stapling of Native Peptides at Lysine and Tyrosine or Arginine with Formaldehyde. Angew. Chem., Int. Ed. 2021, 60, 6646.

[4]   Yang, P.; Wang, X.; Li, B.; Yang, Y.; Yue, J.; Suo, Y.; Tong, H.; He, G.; Lu, X.; Chen, G. Streamlined Construction of Peptide Macrocycles via Palladium-catalyzed Intramolecular S-Arylation in Solution and on DNA. Chem. Sci. 2021, 12, 5804.

讲座联系人/Contact:

理学院，邹坤，zoukun@westlake.edu.cn

School of Science, Kun Zou, zoukun@westlake.edu.cn