Research Areas

Our lab focused on the design, synthesis, and evaluation of anti-cancer chemical small molecules by comprehensive utilization of various approaches including high throughput screening, organic synthesis, chemical biology, cell biology, molecular genetics, and molecular pharmacology, aiming to development of innovative anti-cancer drugs targeting transcription factors.

Highlights

Xiaoguang Lei is a professor in the College of Chemistry and Molecular Engineering at Peking University, senior investigator at Peking-Tsinghua Center for Life Sciences, winner of National Distinguished Young Investigator Award, and 973 chief scientist. Prof. Lei is a world-renowned organic synthetic chemist, chemical biologist, and pharmaceutical chemist, and has made a series of original scientific achievements in the fields of natural product function-oriented total synthesis, chemical biology, synthetic biology, and innovative drug development. He has published more than 80 papers in Cell, Nature, Science, and other journals, and obtained more than 10 patents of innovative drug invention. To date, two candidate drug molecules of them have achieved scientific research transformation, and clinical research will be carried out soon. He has won 18 academic awards at home and abroad, including Tetrahedron Young Investigator Award in Bioorganic and Medicinal Chemistry, Young Chemical Biologist Award by the International Chemical Biology Society (ICBS), Shulan Medical Youth Award, CCS-BASF Young Investigator Award, Wei Shan Natural Product Synthesis Award by Chinese Chemical Society, IUPAC Young Chemist Award, and Servier Young Investigator Award by Chinese Pharmaceutical Association. Currently, Prof. Lei is an executive chief editor of the international pharmaceutical core journal《Bioorganic & Medicinal Chemistry》. 

We have completed more than 60 complex natural product function-oriented total synthesis

Kinase DYRK2 acts as an upstream regulator of the proteasome and can promote tumor growth. Metal carrier pseudopalin is a small molecule that actively pass through the bacterial cell membrane and can be connected to antibiotics to promote its transmembrane transport. 

Honors

• • IUPAC Young Chemist Award, 2009

• • WuXi PharmaTech 2010 Life Science and Chemistry Award, 2010

• • New Century Excellent Talents in University Award, 2010

• • Outstanding Young Investigator Award by National Natural Science Foundation of China, 2012

• • Asian Core Program Lectureship Award, 2012

• • Thieme Chemistry Journal Award, 2013

• • Servier Young Investigator Award by Chinese Pharmaceutical Association, 2013

• • Young Chemical Biologist Award by the International Chemical Biology Society (ICBS), 2013

• • Chinese Chemical Society Prize for Young Scientists, 2013

• • National Leading Young Scientific Investigator Award, 2013

• • Roche Chinese Young Investigator Award, 2014

• • Outstanding Young Talent Award of Beijing, 2014

• • Chemical Society of Japan Distinguished Lectureship Award, 2015

• • Wei Shan Natural Product Synthesis Award by Chinese Chemical Society, 2015

• • National Distinguished Young Investigator Award, 2016

• • Organic Chemistry Frontier Emerging Investigator Award, 2016

• • Asian Core Program Lectureship Award, 2016

• • KAIST School of Molecular Science Lectureship Award, 2017

• • Swiss Chemical Society Distinguished Lectureship Award, 2017

• • Tetrahedron Young Investigator Award in Bioorganic and Medicinal Chemistry, 2017

• • CCS-BASF Young Investigator Award, 2018

• • David Ginsburg Memorial Lectureship Award, 2018

• • Shulan Medical Youth Award, 2019

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Related News

1. Tetrahedron Young Investigator Award in Bioorganic and Medicinal Chemistry, 2017

2. International Year of Periodic Table of Chemical Elements 2019

Selected Publications

1. Lei Gao, Cong Su, Xiaoxia Du, Ruishan Wang, Shuming Chen, Yu Zhou, Chengwei Liu, Xiaojing Liu, Runze Tian, Liyun Zhang, Kebo Xie, She Chen, Qianqian Guo, Lanping Guo, Yoshio Hano, Manabu Shimazaki, Atsushi Minami, Hideaki Oikawa, Niu Huang, K. N. Houk, Luqi Huang*, Jungui Dai*, Xiaoguang Lei* "FAD-dependent Enzyme-Catalysed Intermolecular [4+2] Cycloaddition in Natural Product Biosynthesis" Nature Chemistry, 2020, 1, 620-628;

2. Weilong Liu, Benke Hong, Jin Wang, Xiaoguang Lei* “New Strategies in the Efficient Total Syntheses of Polycyclic Natural Products” Acc. Chem. Res. 2020, 53, 2569-2586;

3. Yingjie Bai, Hiu C Lam, Xiaoguang Lei* “Dissecting Programmed Cell Death with Small Molecules” Acc. Chem. Res. 2020, 53, 1034-1045;

4. Sourav Banerjee, Tiantian Wei, Jue Wang, Jenna J. Lee, Haydee L. Gutierrez, Owen Chapman, Sandra E. Wiley, Joshua E. Mayfield, Vasudha Tandon, Edwin F. Juarez, Lukas Chavez, Ruqi Liang, Robert L. Sah, Caitlin Costello, Jill P. Mesirov, Laureano de la Vega, Kimberly L. Cooper, Jack E. Dixon*, Junyu Xiao*, and Xiaoguang Lei* “Inhibition of dual-specificity tyrosine phosphorylation-regulated kinase 2 perturbs 26S proteasome-addicted neoplastic progression” Proc. Natl Acad. Sci. USA 2019, 116, 24881-24891;

5. Alexander X. Jones, Yong Cao, Yu-Liang Tang, Jian-Hua Wang, Yue-He Ding, Hui Tan, Zhen-Lin Chen, Run-Qian Fang, Jili Yin, Rong-Chang Chen, Xing Zhu, Yang She, Niu Huang, Feng Shao , Keqiong Ye , Rui-Xiang Sun, Si-Min He , Xiaoguang Lei* & Meng-Qiu Dong* “Improving mass spectrometry analysis of protein structures with arginine-selective chemical cross-linker” Nature Comm. 2019, 10, 3911;