Principal Investigator
Small-Molecule Drug Research Center;Zhongshan Branch of Drug Discovery & Development Institute
Personal Homepage
CONTACT
zhaoguilong@simm.ac.cn
0760- 85281521
528400
Room 5513, Building 5, Zhongshan Life Science Park, Cuiheng New District, Zhongshan 528400, Guangdong Province, P. R. China
Dr. Zhao received his Ph.D. degree in synthetic organic chemistry from Shandong University in 2008. He then joined Tianjin Institute of Pharmaceutical Research (TIPR) as an assistant professor and principal investigator (PI), a prestigious research institute in pharmaceutical academia and industry in China, where he focused on drug discovery and development of novel drugs for the treatment of metabolic diseases. He became an associate professor in 2010 and then a full professor in 2015. Prior to leaving TIPR, Dr. Zhao served as the director of Tianjin Key Laboratory of Molecular Design and Drug Discovery for years in TIPR. During the stay in TIPR, Dr. Zhao joined Dr. Peng George Wang’s Laboratory in Department of Chemistry at Georgia State University (GSU) as a postdoctoral fellow in 2011-2012. In 2018, Dr. Zhao left TIPR and worked as R&D director in two pharmaceutical companies, Hangzhou Dingzhi Biopharmaceuticals Inc. and Guangzhou Lixin Pharmaceuticals, Inc. In 2020, Dr. Zhao joined Shanghai Institute of Materia Medica (SIMM), Chinese Academy of Sciences (CAS), as a Professor and PI.
Dr. Zhao’s group has discovered and developed three investigational new drugs, i.e. tianagliflozin, tininurad and EP-0226. Tianagliflozin is a potent SGLT2 inhibitor and is currently being developed in phase I clinical trials in China, while tininurad is a potent selective URAT1 inhibitor under development and has finished phase IIb clinical trials in China. EP-0226 is potent and selective voltage-gated calcium channel α2δ ligand, which is now being developed in phase I clinical trials in China for the treatment of neuropathic pain. Dr. Zhao has published 130 peer-reviewed papers, and has 35 authorized patents (including 4 PCT authorizations).
Education Experience
2005.09-2008.06 Ph.D. in synthetic organic chemistry, School of Chemistry and Chemical Engineering, Shandong University
2002.09-2005.06 Master in synthetic organic chemistry, School of Chemistry and Molecular Engineering, Qingdao University of Science and Technology
1999.09-2002.06 Bachelor in Chemistry, School of Chemistry and Chemical Engineering, Liaocheng University (graduated 1 year ahead)
Work Experience
2020.05-Present Professor, PI, Shanghai Institute of Materia Medica, Chinese Academy of Sciences
2019.04-2020.05 Research & Development Director, Guangzhou Lixin Pharmaceuticals, Inc.
2018.07-2019.03 Research & Development Director, Hangzhou Dingzhi Biopharmaceuticals, Inc.
2011.11-2012.11 Postdoctoral fellow, Department of Chemistry at Georgia State University
2008.07-2018.06 Professor, PI and Director of Tianjin Key Laboratory of Molecular Design and Drug Discovery, Tianjin Institute of Pharmaceutical Research
With 18 years of experience of drug discovery and development, Dr. Zhao’s research interest mainly focuses on the discovery and development of novel drugs for the treatment of metabolic and central nervous system diseases as well as the novel organic process development involved in the drug development. Dr. Zhao has a multidisciplinary background of synthetic organic chemistry, pharmacology, medical science, regulatory affairs and intellectual property and a unique experience of running drug R&D program from beginning all the way to the stage of clinical trials.
1. Discovery and development of tianagliflozin, a SGLT2 inhibitor, for the treatment of type 2 diabetes
2. Discovery and development of tininurad, a potent selective URAT1 inhibitor, for the treatment of hyperuricemia and gout
3. Discovery and development of EP-0226, a potent selective voltage-gated calcium channel α2δ ligand, for the treatment of neuropathic pain.
1. China Patent Excellence Award, 2022.
2. Tianjin Municipal Science and Technology Award for Young Talents, 2017.
3. China Patent Excellence Award, 2016.
Selected Publications
1. Mengyan Hou#, Xia Li#, Yan Li#, Wenhao Shi#, Haotian Tang, Fang Feng, Xuan Wan, Hua Xie*, Guilong Zhao*. Design, synthesis, and biological activity of boron-bearing sugar derivatives for boron neutron capture therapy (BNCT). Molecules, 2026, 31(8), 1230.
2.Wang, Qiang; Khan, Maaz; Chen, Shuangyuan; Wu, Qingqing; Zhao, Guilong*; Jadhav, Pankaj*. Rh(III)-catalyzed (benz)imidazole-directed [4+2] cyclization of indoles with maleimides: Facile access to C6-fused indole polyheterocyclic compounds. European Journal of Organic Chemistry, 2026, 29(4), e202500924.
3. Hu, Xinwei; Huang, Wenqian; Lin, Xiaotong; Zhang, Hao; Huang, Yishu; Wu, Jiang*; Zhao, Guilong*. Structure-activity relationship study on soticlestat derivatives for the discovery of CYP46A1 (CH24H) inhibitors. Molecules, 2026, 31(3), 460.
4.Zhang, Tao#; Pan, Zilu#; Gao, Jing#; Wu, Qingqing#; Bai, Gang; Li, Yan; Tong, Linjiang; Feng, Fang; Lai, Mengzhen; Liu, Yingqiang; Song, Peiran; Ning, Yi; Tang, Haotian; Luo, Wen; Chen, Yi; Fang, Yan; Zhang, Hui; Liu, Qiupei; Zhang, Yudi; Wang, Hua; Chen, Zhiwei; Chen, Yi; Geng, Meiyu; Ji, Hongbin; Zhao, Guilong*; Zhou, Hu*; Ding. Jian*; Xie, Hua*. Branched-chain amino acid transaminase 1 confers EGFR-TKI resistance through epigenetic glycolytic activation. Signal Transduction and Targeted Therapy, 2024, 9, 216.
5.Chen, Shuangyuan#; Wei, Feifei#; Cheng, Xinqiang#; Luo, Ying; Meng, Fancui; Zhang, Yuanwen; Huang, Wenqian; Lv, Jun; Pan, Hong*; Wu, Qingqing*; Zhao, Guilong*. Regioselective deacetylation of peracetylated deoxy-C-glycopyranosides by boron trichloride (BCl3). The Journal of Organic Chemistry, 2024, 89(7), 4802-4817.
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