Biography

Dr. Luo comprehensively applied theoretical methods including computational biology, bioinformatics, and drug design, combined with various chemical biology validation platforms, to discovery innovative drugs that target novel targets, mainly aimed at epigenetic enzymes and protein-protein interactions, or innovative drugs with novel mechanisms, and also investigate the mechanisms of these drugs. With these strategies, the regulatory mechanism of several important targets were revealed, and a bunch of lead compounds with development prospect were discovered (5 categories for the first time in the world), and two compounds are under clinical trials. More than 240 SCI papers were published, with a total impact factors above 1600, around 10000 citations by others, and the H-index is 47. In the past five years, breakthroughs were published on Nature, Nature Chem, JACS, PNAS, Adv Mater, Nucleic Acids Res, J Med Chem and other famous international journals as corresponding, co-corresponding or first author. 19 patent applications (2 PCT) have been submitted, and 3 domestic and 1 U.S patent applications were granted with a license. 18 graduate students graduated from his lab, and CAS Dean Excellence Award was conferred once, Excellent Graduation Thesis of Shanghai was conferred once, National Award for Graduates was conferred 10 times.

EDUCATION

09/1990-07/1994 Fuzhou University, Department of Chemistry, Bachelor Degree for Structural Chemistry

09/1998-07/2001 Fudan University, Department of Chemistry, Master Degree for Physical Chemistry

09/2001-07/2004 Shanghai Institute of Materia Medica, Ph.D Degree for Organic Chemistry

WORK EXPERIENCE

10/1994-05/1998 Assistant Engineer, Fuzhou Antibiotic Co. Ltd.

07/2004-09/2005 Assistant Professor, Shanghai Institute of Materia Medica, Drug Design

09/2005-03/2008 Postdoctoral Fellow, Ronen Marmorstein Lab, Wistar Institute, University of Pennsylvania, Epigenetics and Chemical Biology

03/2008-10/2008 Assistant Professor, Shanghai Institute of Materia Medica, Drug Design and Chemical Biology

10/2008-10/2012 Associate Professor, Shanghai Institute of Materia Medica, Drug Design and Chemical Biology

10/2012-Present Professor, Shanghai Institute of Materia Medica, Drug Design and Chemical Biology

Research Directions

1. Computational drug design

2. Medicinal chemical biology

3. Medicinal chemistry

Achievements

Dr. Luo’s research field is drug design and chemical biology, his research interests focus on the discoveries of new drug targets of natural products and metabolites as well as the mechanisms of the regulations of the targets using multidisciplinary technologies in biochemistry, structural biology and medicinal chemical biology. Dr. Luo has discovered targets of many important natural products or endogenous metabolites, and revealed the regulation mechanisms of the important targets. In addition, he also developed a series of promising lead compounds including the copper transporter inhibitor DC-AC50 and the small G protein Rho subfamily inhibitor DC-Rhoin. Among them 3 compounds are in pre-clinical evaluation and some compounds have been transferred successfully. Dr. Luo has published more than 130 peer-viewed paper including Nature, Cancer Cell, Nat. Chem., Adv. Sci., JACS, PNAS, Nucleic Acid Res. with about 10000 citations. He also applied 56 patents and 5 of them have been authorized and transferred successfully. Dr. Luo has presided over more than 10 projects, such as the "863" project, the key projects of the National Natural Science Foundation of China and Distinguished Young Scholars Fund Project. Dr. Luo has also received many honors, including leader in innovation of the Ministry of Science and Technology, leader in the "Ten Thousand Talents Program" of the Organization Department of the Central Committee, and an outstanding academic leader in Shanghai. Dr. Luo has trained more than 50 graduate students, some of whom have been engaged in post-doctoral research in the world-famous universities such as Harvard University, University of Chicago, University of Pennsylvania, European Center for Molecular Biology, and some of whom have been funded by a number of talent programs including the Hundred Talents Program of the Chinese Academy of Sciences.

Publications

1. Ping Guo, Shijia Zu, Shilong Han, Wendan Yu, Guoqing Xue, Xiaona Lu, Hua Lin, Xinrui Zhao, Haibo Lu ,Chunyu Hua,Xinyu Wan,Liyuan Ru,Ziyue Guo,Hanxiao Ge, Kuan Lv, Guohui Zhang, Wuguo Deng, Cheng Luo*,Wei Guo*. BPTF inhibition antagonizes colorectal cancer progression by transcriptionally inactivating Cdc25A. Redox Biol. 2022 Jul 22;55:102418.

2. Jiacheng Li, Ting Liu, Yuanli Song, Mingyu Wang, Liling Liu, Hongwen Zhu, Jin Lin, Kaixian Chen, Hualiang Jiang, Hu Zhou*, Hua Lin*, and Cheng Luo,*Discovery of small-molecule degraders of the CDK9-cyclin T1 complex for targeting transcriptional addiction in prostate cancer. J Med Chem. 2022 Aug 25;65(16):11034-11057.

3. Liping Liao, Wenzhen Dang, Tingting Lin, Wen Li, Senhao Xiao, Lei Feng, Jing Huang, Rong Fu, Jiacheng Li, Liping Liu, Mingchen Wang, Hungru Tao, Hualiang Jiang, Kaixian Chen, Bing Zhou*, Xiaoyan Shen*, and Cheng Luo*. A potent PGK1 antagonist reveals PGK1 regulates the production of IL-1β and IL-6. APSB 2022, in press.

4. Mingming Sun, Leilei Li, Jiaqi Song, Yaya Qiao, Fei Xie, Yingzhi Wang, Huanran Sun, Jiyan Wang, Zhen Li, Sizhen Lai, Hongkai Chang, Han Zhang, Chenxin Yang, Huifang Zhao, Junzhen Tan, Yanping Li, Shuangping Liu, Bin Lu, Min Liu, Guangyao Kong, Yujun Zhao, Chunze Zhang, Cheng Luo*, Changliang Shan*. PRMT6-medaited 6PGD and ENO1 methylation regulates cell metabolism, tumorigenicity, and chemotherapy response of lung cancer. APSB 2021; in press.

5. Jing Huang, Xiaobo Wang, Shiyu Shen, Ruina Wang, Bing, Li, Hongru Tao, Junchi Hu, Jin Yu,Hualiang Jiang, Kaixian Chen, Cheng Luo*，Yongjun Dang*, Yuanyuan Zhang*, L-5-hydroxytryptophan promotes Antitumor Immunity by Inhibiting PD-L1 Inducible Expression. J Immunother Cancer. 2022 Jun;10(6):e003957.

6. Xiaotong Diao, Fei Ye, Meina Zhang, Xintong Ren, Xiaoxu Tian, Jingping Lu, Xiangnan Sun, Zeng Hou, Xiaoyu Chen, Fengwei Li, Jingjing Zhuang, Hong Ding, Chao Peng, Fraydoon Rastinejad*, Cheng Luo*, Dalei Wu*. Identification of oleoylethanolamide as an endogenous ligand candidate for HIF-3α. Nat Commun. 2022 May 9;13(1):2529.

7. Jianhua Mao^#, Kongkai Zhu^#, Zhangbiao Long^#, Huimin Zhang^#, Bing Xiao, Wenda Xi, Yun Wang, Jiansong Huang, Jingqiu Liu, Xiaofeng Shi, Hao Jiang, Tian Lu, Yi Wen, Naixia Zhang, Qian Meng, Hu Zhou, Zheng Ruan, Jin Wang, Cheng Luo^*, Xiaodong Xi*, Small molecule DCDBS84 regulates platelet  thrombus  formation by targeting c-Src SH3 domain, SH3, Adv Sci 2022;e2103228.

8. Liping Liu, Rui Zhua, Jiacheng Li, Yuan Pei, Shuanshuan Wang, Pan Xu, Mingyu Wang, Hao Zhang, Daohai Du, Hong Ding, Hualiang Jiang, Kaixian Chen, Bing Zhou, Lifang Yu*, Cheng Luo,*Computational and Structure-based development of high potent cell-active covalent Inhibitor targeting the peptidyl-prolyl isomerase NIMA-interacting-1 (Pin1). J Med Chem 2022;65(3):2174-2190.

9. Mao J, Zhu K, Long Z, Zhang H, Xiao B, Xi W, Wang Y, Huang J, Liu J, Shi X, Jiang H, Lu T, Wen Y, Zhang N, Meng Q, Zhou H, Ruan Z, Wang J, Luo C*, Xi X*. Targeting the RT loop of Src SH3 in Platelets Prevents Thrombosis without Compromising Hemostasis. Adv Sci (Weinh). 2022 Mar;9(7):e2103228.

2021年

10. Lu T, Li Y, Lu W, Spitters T, Fang X, Wang J, Cai S, Gao J, Zhou Y, Duan Z, Xiong H, Liu L, Li Q, Jiang H, Chen K, Zhou H, Lin H, Feng H, Zhou B*, Antos CL*, Luo C*. Discovery of a subtype-selective, covalent inhibitor against palmitoylation pocket of TEAD3. Acta Pharm Sin B. 2021 Oct;11(10):3206-3219.

11. Hu L, Chen F, Wu C, Wang J, Chen SS, Li XR, Wang J, Wu L, Ding JP, Wang JC, Huang C, Zheng H, Rao Y, Sun Y, Chang Z, Deng W*, Luo C*, Chin YE*. Rapamycin recruits SIRT2 for FKBP12 deacetylation during mTOR activity modulation in innate immunity. iScience. 2021 Sep 27;24(11):103177

12. Zhang H, He J, Hu G, Zhu F, Jiang H, Gao J, Zhou H, Lin H, Wang Y, Chen K, Meng F, Hao M, Zhao K, Luo C*, Liang Z. Dynamics of Post-Translational Modification Inspires Drug Design in the Kinase Family. J Med Chem. 2021 Oct 28;64(20):15111-15125.

13. Fan S, Yue L, Wan W, Zhang Y, Zhang B, Otomo C, Li Q, Lin T, Hu J, Xu P, Zhu M, Tao H, Chen Z, Li L, Ding H, Yao Z, Lu J, Wen Y, Zhang N, Tan M, Chen K, Xie Y, Otomo T, Zhou B*, Jiang H*, Dang Y*, Luo C*. Inhibition of Autophagy by a Small Molecule through Covalent Modification of the LC3 Protein. Angew Chem Int Ed Engl. 2021 Sep 29. doi: 10.1002/anie.202109464

14. Lu T, Lu H, Duan Z, Wang J, Han J, Xiao S, Chen H, Jiang H, Chen Y, Yang F, Li Q, Chen D, Lin J, Li B, Jiang H, Chen K, Lu W, Lin H*, Luo C*. Discovery of High-Affinity Inhibitors of the BPTF Bromodomain. J Med Chem. 2021 Aug 26;64(16):12075-12088.

15. Youyi Zhang, Fei Ye, Tongtong Zhang, Shiyun Lv, Liping Zhou, Fei Guo, Daohai Du, Cheng Luo*, Shujia Zhu* Structural basis of ketamine action on human NMDA receptors. Nature. 2021 Aug;596(7871):301-305.

16. Du D, Xu D, Zhu L, Stazi G, Zwergel C, Liu Y, Luo Z, Li Y, Zhang Y, Zhu K, Ding Y, Liu J, Fan S, Zhao K, Zhang N, Kong X, Jiang H, Chen K, Zhao K, Valente S*, Min J*, Duan W*, Luo C*. Structure-Guided Development of Small-Molecule PRC2 Inhibitors Targeting EZH2-EED Interaction. J Med Chem. 2021 Jun 2. doi: 10.1021/acs.jmedchem.0c02261.

17. Lin T, Li J, Liu L, Li Y, Jiang H, Chen K, Xu P*, Luo C*, Zhou B*. Design, synthesis, and biological evaluation of  4-benzoylamino-1H-pyrazole-3- carboxamide derivatives as potent CDK2 inhibitors.  Eur J Med Chem. 2021 Apr 5;215:113281.

18. Wang J, Wang C, Xu P, Li X, Lu Y, Jin D, Yin X, Jiang H, Huang J, Xiong H, Ye F, Jin J, Chen Y, Xie Y, Chen Z, Ding H, Zhang H, Liu R, Jiang H, Chen K, Yao Z, Luo C*, Huang Y*, Zhang Y*, Zhang J*. PRMT1 is a novel molecular therapeutic target for clear cell renal cell carcinoma. Theranostics. 2021 Mar 12;11(11):5387-5403.

19. Tian Lu, Yong Li, Wenchao Lu, TWGM Spitters, Jun Wang, Simian Cai, Jing Gao,  Yanting Zhou, Zhe Duan, Huan Xiong, Qi Li, Hualiang Jiang, Kaixian Chen, Hu Zhou, Hua Lin, Huijin Feng, Bing Zhou, * Christopher L. Antos, * Cheng Luo*Discovery of a subtype-selective, covalent inhibitor against palmitoylation pocket of TEAD3. Acta Pharmaceutica Sinica B, 2021 in press.

20. Li W, Liao LP, Song N, Liu YJ, Ding YL, Zhang YY, Zhou XR, Sun ZY, Xiao SH, Wang HB, Lu J, Zhang NX, Jiang HL, Chen KX, Liu CP, Zheng J*, Zhao KH*, Luo C*. Natural product 1,2,3,4,6-penta-O-galloyl-β-D-glucopyranose is a reversible inhibitor of glyceraldehyde 3-phosphate dehydrogenase. Acta Pharmacol Sin. 2021 Apr 13. doi: 10.1038/s41401-021-00653-0.