Faculty |
Gang LIU, Ph.D.

Gang LIU, Tenured Full Professor

Prof. Gang Liu got his Ph.D. from School of Pharmaceutical Sciences, Beijing Medical University in 1994. Then he had two postdoctoral fellowships in Institute of Pharmacology and Toxicology, AMMS and The Scripps Research Institute, respectively, from 1994 to 1997. After a senior scientist career for three years in University of California at Davis, he established his own laboratory in 2000 at Institute of Materia Medica, CAMS & PUMC, when he was awarded “Peking Union” Scholar and then “Chang Jiang” Scholar in 2005. In 2011, he moved to School of Medicine, Tsinghua University as chair of Department of Pharmacology and Pharmaceutical Sciences (renamed School of Pharmaceutical Sciences).

Honors and Awards

Science and technology award of Chinese Pharmaceutical Association, the first place, 2019.

Cathay Award of 12th Chinese International Peptide Symposium, 2012.

Published Books


Research Interests

Prof. Gang Liu’s lab is interested in developing synthetic methodologies of small molecule heterocyclic compound libraries, natural products, peptide/glycopeptide mimics and “synergistic therapy” compounds. His lab is also interested in analytic and/or assay methodologies for qualification, quantization and high throughput screening of libraries to understand the molecular interactions, coding and decoding the small molecules that interrupt the biological actions. The goals in this lab are to discover and optimize the lead compounds and develop drug candidates to prevent from cancer and certain infectious diseases.

Major scientific contributions

Prof. Gang Liu is one of the scientists firstly engaged in combinatorial chemistry and chemical biology research in China. He successfully constructed the combinatorial chemistry technology platform consisting of high-throughput synthetic technology, high-throughput modern analysis technology, medicinal chemistry, organic chemistry, polymer chemistry (resin), CADD, automation technology, biological screening technology, data management system and sample preservation and analysis of quality control methods, which is evaluated by experts as "overall in international advanced level”. Over the years, he accumulated fully experience in heterocyclic compounds library design, combinatorial synthesis, peptide chemistry, organic chemistry, medicinal chemistry, and also immunotherapy, anti-tumor and anti-infection drug discovery.

His laboratory had successfully developed drug candidates Conmutaxol and Salutaxel, which are conjugates of paclitaxel or docetaxel and MDP derivatives, designed to be inhibiting inflammatory cytokines from tumor microenvironment trough antagonize NOD1/2 signaling, thereby inhibiting tumor metastasis and tumor growth. Salutaxel is now under phase I trial investigation.

1. Antagonists of pattern recognition receptor NOD1/2 inhibited both tumor growth and metastasis via reversing chemo-therapeutic resistance via (J Extracell Vesicles, 2022; 11: e12264. https://doi.org/10.1002/jev2.12264.;J. Med. Chem. 2018, 61, 1519-1540; J. Med. Chem. 2017, 60 (12), 5162–5192.; J. Med. Chem. 2017, 60, 1219-1224; J. Med. Chem. 2011, 54(8): 2767-77; Glycoconj J 2008, 25: 415–425.)

2. Synthetic calanolides with anti HIV-1 activity, bactericidal activity against replicating and Non-replicating mycobacterium tuberculosis and target identification(Chem Commun (Camb). 2021, 57, 13174-13177;ACS Infect. Dis. 2018, Jan. 2018, online; J. Med. Chem., 2014, 57, 3755-3772.; Antimicrob. Agents Chemother. 2012, 56(1): 341-351.; J. Med. Chem. 2010, 53, 1397–1401.; J. Med. Chem. 2008, 51, 1432–1446.)

3. Total synthesis of natural product and medicinal chemistry (J. Med. Chem., 2022, 2022, 65(21), 14891-14915, https://doi.org/10.1021/acs.jmedchem.2c01431.; Angew. Chem. Int. Ed., 2016, 55(24): 6992-6; Org Lett 2015, 17(16): 4110-3)

Selected Publications

1. Xiduan Wei, Jingjia Ye, Yamen Pei, Chunting Wang, Hongzhen Yang, Jingyuan Tian, Guangxu Si, Yao Ma*, Kun Wang*, Gang Liu*, Extracellular vesicles from colorectal cancer cells promote metastasis via the NOD1 signaling pathway, J Extracell Vesicles, 2022; 11: e12264. https://doi.org/10.1002/jev2.12264.
2. Wenjun YU, Yao Ma, Xilei Xie, Shiping Fang, Yi Dong*, Gang LIU*, Identification of 1,4-Benzodiazepine-2,5-dione Derivatives as Protein Synthesis Inhibitors with Highly Potent Anticancer Activity, J. Med. Chem. 2022, 65(21), 14891-14915,  https://doi.org/10.1021/acs.jmedchem.2c01431.
3. Xueyuan Li, Pengfei Geng, Xiaoqiao Hong, Zhaogang Sun, Gang Liu*, Detecting Mycobacterium Tuberculosis using a nitrofuranyl calanolide–trehalose probe based on nitroreductase Rv2466c, Chem Commun (Camb). 2021, 57, 13174-13177.
4. Chunting Wang, Yameng Pei, Lei Wang, Ye Xiang, Yao Ma*, Gang Liu*, Constrain the Conformation: Discovery of (1H-pyrazolo[3,4-c]pyridin-5-yl)sulfonamide Analogues as Hepatitis B Virus Capsid Assembly Modulator, J. Med. Chem., 2020, 63, 6066-6089.
5. Yao Ma, Dawei Yin, Hai Qian*, Gang Liu*, Discovery of potent inhibitors against P-glycoprotein-mediated multidrug resistance aided by late-stage functionalization of 2-(4-(pyridin-2-yl)phenoxy)pyridine analogue, J. Med. Chem. 2020, 63, 5458-5476.
6. Ran Mu, Chengcheng Kong, Wenjun Yu, Hongyao Wang, Jie Wu, Xueyuan Li, Selin Somersan-Karakaya, Haitao Li, Zhaogang Sun*, Gang LIU*, Nitrooxidoreductase Rv2466c-Dependent Fluorescent Probe for Mycobacterium tuberculosis Diagnosis and Drug Susceptibility Testing, ACS Infect. Dis. 2019, 5(6), 949-961.
7. Xiaoming Wen, Purong Zheng, Yao Ma, Yingye Ou, Weixin Huang, Shuo Li, Shoujia Liu, Xuan Zhang, Ziyu Wang, Qianli Zhang, Wenming Cheng, Ruwen Lin, Hongzu Li, Youyou Cai, Chunyun Hu, Ningbin Wu, Long Wan, Tingting Pan, Jinlong Yao, Xuelu Bei, Wei-Bin Wu, Jian Jin, Jie Yan*, and Gang Liu*, Salutaxel, a conjugate of docetaxel and a muramyl dipeptide (MDP) analogue, acts as multi-functional prodrug that inhibits tumor cell growth and metastasis, J. Med. Chem. 2018, 61, 1519-1540.
8. Ana Negri, Prisca Javidnia, Ran Mu, Xiaojie Zhang, Jeremie Vendome, Ben Gold, Julia Roberts, Dipti Barman, Thomas Ioerger, James Sacchettini, Xiuju Jiang, Kristin Burns-Huang, Thulasi Warrier, Yan Lin, David Warren, Thijs Beuming, Hongyao Wang, Jie Wu, Haitao Li, Kyu Rhee, Carl F. Nathan, Gang Liu*, Selin Somersan-Karakaya*, Identification of a mycothiol-dependent nitro-oxidoreductase from Mycobacterium tuberculosis, ACS Infect. Dis. Jan. 2018, online.
9. Suhua Wang, Jingshu Yang, Xueyuan Li, Zijie Liu, Youzhen Wu, Guangxu Si, Yiran Tao, Nan Zhao, Xiao Hu, Yao Ma*, Gang Liu*, Discovery of 1,4-Benzodiazepine-2,5-dione (BZD) Derivatives as Dual Nucleotide Binding Oligomerization Domain Containing 1 /2 (NOD1/NOD2) Antagonists Sensitizing Paclitaxel (PTX) to Suppress Lewis Lung Carcinoma (LLC) Growth In Vivo, J. Med. Chem. 2017, 60 (12), 5162–5192.
10. Yi Dong, Suhua Wang, Chunting Wang, Zihua Li, Yao Ma*, Gang Liu*, Antagonizing NOD2 Signaling with Conjugates of Paclitaxel and Muramyl Dipeptide Derivatives Sensitizes Paclitaxel Therapy and Significantly Prevents Tumor Metastasis, J. Med. Chem. 2017, 60, 1219-1224.
11. Yameng Pei, Chunting Wang, S. Frank Yan*, Gang Liu*,Past, Current, and Future Developments of Therapeutic Agents for Treatment of Chronic Hepatitis B Virus Infection,J. Med. Chem. 2017, 60, 6461-6479. Invited perspective.
12. Chong Tian, Xiaoqiang Lei, Yuanhao Wang, Zhen Dong, Gang Liu* and Yefeng Tang*, Total Syntheses of Periconiasins A-E, Angew. Chem. Int. Ed., 2016, 55(24): 6992-6.
13. Nan Zhao, Mingna Sun, Kristin E. Burns-Huang, Xiuju Jiang, Yan Ling, Crystal M. Darby, Sabine Erht, Gang Liu* and Carl F. Nathan*, Identification of Rv3852 as an Agrimophol-Binding Protein in Mycobacterium tuberculosis, PLoS One 2015, 10(5): e0126211.
14. Yi Dong, Nana Du, Xueyuan Li, Litao Zheng, Gang Liu*, Tandem Chloropalladation/Cyclization and Dearomative Cyclization toward Functionalized Tricyclic Bridged [3.2. 1] Skeleton Compounds, Org. Lett. 2015, 17(16):4110-3.
15. Purong Zheng, Selin Somersan Karakaya, Shichao Lu, Julia Roberts, Maneesh Pingle, Thulasi Warrier, David Little, Xiaoyong Guo, Steven Brickner, Carl F. Nathan*, Ben Gold*, Gang Liu* Synthetic Calanolides with Bactericidal Activity Against Replicating and Non-replicating Mycobacterium tuberculosiss, J. Med. Chem. 2014, 57(9), 3755–3772.
16. Yi Dong, Gang Liu*,Rh-Catalyzed Sulfonic Acid Group Directed C-H Olefination of Arenes, Chem. Comm. 2013, 49, 8066-8068.
17. Shichao Lu, Purong Zheng, Gang Liu*, Iodine(III)-Mediated Tandem Oxidative Cyclization for Construction of 2-Nitrobenzo[b]furans, J. Org. Chem. 2012, 77, 7711-7717.
18. Xiaofan Lu, Li Liu, Xu Zhang, Terrence Lau, Stephen Kwok-Wing Tsui,   Yuanxi Kang,  Purong Zheng, Gang Liu* and Zhiwei Chen*, F18, a novel small molecule NNRTI, inhibits HIV-1 replication using distinct binding motifs, Antimicrob. Agents Chemother. 2012, 56(1): 341-351.
19. Rui Liu, Zhuhui Huang, Michael G. Murray, Xiaoyong Guo, Gang Liu*, Quinoxalin-2(1H)-One Derivatives As Inhibitors Against Hepatitis C Virus, J. Med. Chem. 2011, 54, 5747–5768.
20. Yao Ma, Nan Zhao, Gang Liu*, Conjugate (MTC-220) of Muramyl Dipeptide Analogue and Paclitaxel Prevents Both Tumor Growth and Metastasis in Mice, J. Med. Chem., 2011, 54 (8), 2767–2777.
21. Gang Li, Dongmei Wang, Mingna Sun, Guangyan Li, Jinfeng Hu, Yun Zhang, Yuhe Yuan, Haijie Ji, Naihong Chen*, Gang Liu*. Discovery and Optimization of Novel 3-Piperazinyl Coumarin Antagonist of Chemokine – like factor 1 with oral Anti-asthma activity in mice. J. Med. Chem. 2010, 53 (4), 1741–1754.
22. Hai Xue, Xiaofan Lu, Purong Zheng, Li LIU, Chunyan Han, Jinping HU, Zijie Liu, Tao MA, Yan LI, Lin WANG , Zhiwei CHEN*, Gang LIU*, Highly suppressing wide type HIV-1 and Y181C mutation by 10-Chloromethyl-11-Demethyl-12-oxo calanolide A with druggable profile. J. Med. Chem. 2010, 53, 1397–1401.
23. Leilei Zhang, Yu Yan, Zijie Liu, Abliz Zeper, Gang Liu*, Identification of Peptide Substrate and Small Molecule Inhibitors of Testis-specific Serine/Threonine Kinase1 (TSSK1) By the Developed Assays, J. Med. Chem. 2009, 52, 4419-4428.
24. Fa Zhang, Wei Zhang, Yan Zhang,  Dennis P. Curran, and Gang Liu*, Synthesis and Applications of Light-Fluorous Glycosyl Donor, J. Org. Chem. 2009, 74 (6), 2594-2597.
25. Tao MA, Li LIU, Hai XUE, Li LI, Chunyan HAN, Lin WANG, Zhiwei CHEN, Gang LIU*, The Chemical Library and Structure-Activity Relationship of Calanolide-A Analogues against HIV-1, J. Med. Chem. 2008, 51, 1432-1446.