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 302, Building A, Sino-Swiss (Euro) Industrial 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 investigational (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 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 ever 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 two investigational new drugs, i.e. tianagliflozin and tininurad. Tianagliflozin is a SGLT1/SGLT2 dual inhibitor and is currently being developed in phase II clinical trials in China, while tininurad is a potent selective URAT1 inhibitor under development in phase I clinical trials in China. Dr. Zhao’s group discovered a cocatalyst in 2014, SrCl2, which is capable of efficiently catalyzing acidic hydrolysis of methyl glycosides. Before that, the acidic hydrolysis of methyl glycosides remained an intractable problem both in laboratory and industry. The efficiency of this cocatalyst has been confirmed by other laboratories when other currently available methods don’t work and also proved efficient on industrial scales. Dr. Zhao has published 115 peer-reviewed papers, among which 66 ones, Dr. Zhao are as corresponding authors or first author. Dr. Zhao also filed 53 patents (7 PCT applications), with 34 being already authorized (3 PCT authorizations).
Education
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)
Professional History
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 12 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 SGLT1/SGLT2 dual 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 industrial application of SrCl2, an efficient cocatalyst for the acidic hydrolysis of methyl glycosides
4. Discovery of synthetic approaches to 1-S-cycloprpanecarboxylic acids as novel moieties for the SAR study in medicinal chemistry
1. Tianjin Municipal Science and Technology Award for Young Talents, 2017.
2. China Patent Excellence Award, 2016.
3. Tianjin Municipal May 1 Labor Medal. 2016.
4.“Outstanding Young Scholar” of Tianjin Municipal Talent Development Special Support Program. 2015.
5.“Young Talent of Science and Technology” of Tianjin Municipal Innovative Talent Promotion Program. 2014.
6. First Level of Tianjin Municipal “131” Innovative Talent Promotion Program. 2013
Full Publication List
Selected Publications
1.Zhang, Shuo; Shi, Xinhua; Li, Jichao; Hou, Zitong; Song, Zihe; Su, Xiaofeng; Peng, Dan*; Wang, Feng; Yu, Yitao and Zhao, Guilong*. Nickel-catalyzed amidoalkylation reaction of γ-hydroxy lactams: an access to 3?substituted isoindolinones. ACS Omega, 2019, 4(21), 19420-19436.
2.Wu, Jingwei; Yin, Ling; Liu, Yuqiang; Zhang, Huan; Xie, Yafei; Wang, Runling*; Zhao, Guilong*. Synthesis, biological evaluation and 3D-QSAR studies of 1,2,4-triazole-5-substituted carboxylic acid bioisosteres as uric acid transporter 1 (URAT1) inhibitors for the treatment of hyperuricemia associated with gout. Bioorganic & Medicinal Chemistry Letters, 2019, 29(3), 383-388.
3.Cai, Wenqing; Wu, Jingwei; Liu, Wei; Xie, Yafei; Liu, Yuqiang; Zhang, Shuo; Xu, Weiren; Tang, Lida; Wang, Jianwu*; Zhao, Guilong*. Systematic structure-activity relationship (SAR) exploration of diarylmethane backbone and discovery of a highly potent novel uric acid transporter 1 (URAT1) inhibitor. Molecules, 2018, 23(2), 252.
4.Zhang, Xiansheng; Wu, Jingwei; Liu, Wei; Liu, Yuqiang; Xie, Yafei; Shang, Qian; Zhou, Zhixing; Xu, Weiren; Tang, Lida; Wang, Jianwu*; Zhao, Guilong*. Discovery of flexible naphthyltriazolylmethane-based thioacetic acids as highly active uric acid transporter 1 (URAT1) inhibitors for the treatment of hyperuricemia of gout. Medicinal Chemistry, 2017, 13(3), 260-281.
5.Tian, He; Liu, Wei; Zhou, Zhixing; Shang, Qian; Liu, Yuqiang; Xie, Yafei; Liu, Changying; Xu, Weiren; Tang, Lida; Wang, Jianwu*; Zhao, Guilong*. Discovery of a flexible triazolylbutanoic acid as a highly potent uric acid transporter 1 (URAT1) inhibitor. Molecules, 2016, 21(11), 1543.
Back