Dr. Yonghui Wang obtained his Ph.D. from Virginia Polytechnic Institute and State University in 1997 and did his postdoctoral research at Harvard University from 1997 to 2001. He then worked in GlaxoSmithKline Pharmaceutical R&D as a principal scientist, investigator and associate director for more than 12 years. Since 2014, he has become a professor in School of Pharmacy at Fudan University. His current research focuses on small molecular drug discovery for autoimmune diseases and cancer immunotherapy. He earned several honors including GSK Exceptional Science Award in 2004. He published more than 40 SCI papers and is co-inventor of more than 30 PCT international patents.
1. Discovery of novel small molecular drugs for autoimmune diseases and cancer immunotherapy;
2. Design and synthesis of drug-like compound libraries for hit identification and unique chemical probes for MOA studies
Education
1997-1999 Postdoctoral Research Fellow, Organic Chemistry, Harvard University, USA
1993-1997 Ph.D., Organic Chemistry, Virginia Tech, USA
1983-1985 M.S., Analytical Chemistry, Northeast University, China
1979-1983 B.S., Chemistry, Henan Normal University, China
Professional Experiences
2014-present Professor, Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai, China
2008-2013 Manager (10/2008-02/2011);
Associate Director (02/2011-12/2013),
Medicinal Chemistry, R&D Shanghai, GlaxoSmithKline, China
2001-2008 Principal Scientist (08/2001-10/2004);
Investigator (10/2004-03/2007);
Team Leader (03/2007-10/2008),
Medicinal Chemistry, R&D Collegeville, GlaxoSmithKline, PA, USA
1997-2001 Research Associate (08/1999-08/2001);
Postdoctoral Fellow (08/1997-08/1999),
Organic Chemistry, Dept. of Chem. & Chem. Biol., Harvard University, Cambridge, MA, USA
1993-1997 Graduate Research/Teaching Assistant, Organic Chemistry, Dept. of Chem., Virginia Tech, Blacksburg, VA, USA
1985-1993 Assistant professor, Environmental and Analytical Chemistry, School of Environmental and Civil Engineering Xian Univ. of Arch. & Tech., Xian, China
Teaching Activities
Undergraduate course: Medicinal Chemistry II
Graduate courses: Current Progress on Pharmaceutical Research; Modern Drug Discovery
Grants & Projects
1. National Science Foundation of China, Grant 81874287, 2019.01 – 2022.12
2. Fudan University & SIMM Research Collaboration, Grant FU-SIMM20174007, 2017.11 – 2019.10
3. 2017 Shanghai Biopharmaceutical Science and Technology Supporting Plan, Grant 17431902100, 2017.6 – 2020.9
4. National Science Foundation of China, Grant 81573276, 2016.01 – 2019.12
5. 2015 Shanghai Biopharmaceutical Science and Technology Supporting Plan, Grant 17431902100, 2017.6 – 2020.9
6. Fudan University Research Initiation Grant, 2014.1 – 2018.12
Awards & Honors
2013 Silver Recognition Award (Novel lead discovery), GlaxoSmithKline
2007 Silver Recognition Award (China collaboration), GlaxoSmithKline
2005 Silver Recognition Award (program leadership), GlaxoSmithKline
2004 Exceptional Science Award, GlaxoSmithKline
1993-1997 Academic Scholarship, Virginia Tech
1991 Outstanding Young Teacher, Xian Univ. of Arch. & Tech., China
1989 Award for Teaching Excellence, Xian Univ. of Arch. & Tech., China
1984 Outstanding Student Award, Northeast University, China
1980/1/2 Outstanding Student Awards, Henan Normal University, China
Memberships
American Chemical Society
Invited Presentations
1. “From ROR?t agonists to two types of ROR?t inverse agonists”, an invited lecture in the 11th International Symposium for Chinese Medicinal Chemists (ISCMC2018), IL-40, August 24-26, 2018, Zhengzhou, China
2. “Discovery of ROR?t modulators for autoimmune diseases and cancer immunotherapy”, an invited talk in BioTOP-Huya seminar series, July 25, 2018, Suzhou, China
3. “Discovery of ROR?t agonists for cancer immunotherapy”, an invited talk in 2017 Chinese Medicinal Chemistry Symposium (CMCS2017), August 27-30, 2017, Beijing, China
4. “Discovery of ROR?t inverse agonists for autoimmune diseases and agonists for cancer immunotherapy”, an invited talk in BIT’s 6th Annual International Congress of Medchem-2016 (ICM-2016), November 16-19, 2016, Nanjing, China
5. “Discovery of ROR?t modulators”, an invited lecture in 2016 Queenstown Molecular Biology Meetings in Shanghai, March 17-18, 2016, Shanghai, China
6. “Discovery of ROR?t modulators”, an invited lecture in School of Pharmacy, Nantong University, March 18, 2016, Nantong, China
7. “Discovery of ROR?t inverse agonists for autoimmune diseases”, an invited lecture in 2015 Chinese Medicinal Chemistry Symposium (CMCS2015), IL-46, August 23-26, 2015, Lanzhou, China
8. “Discovery of ROR?t inverse agonists”, an invited lecture in China Pharmaceutical University, November 17, 2014, Nanjing, China
9. “Discovery of ROR?t inverse agonists for autoimmune diseases”, an invited lecture in the 9th International Symposium for Chinese Medicinal Chemists (ISCMC2014), IL-08, August 17-20, 2014, Shenyang, China
10. “Discovery of ROR?t inverse agonists for inflammatory and autoimmune diseases”, an invited lecture in the Department of Chemistry and Chemical Engineering, Henan Normal University, April, 2014, Xinxiang, China
Selected Publications
1. Ruomeng Qiu, Yonghui Wang.* Retinoic acid receptor-related orphan receptor-gamma-t (ROR?t) agonists as potential small molecular therapeutics for cancer immunotherapy. J. Med. Chem., 2018, 61, 5794-5804
2. Yafei Huang, Mingcheng Yu, Nannan Sun, Ting Tang, Fazhi Yu, Xiaoxia Song, Qiong Xie*, Wei Fu, Liming Shao, Yonghui Wang.* Discovery of Carbazole Carboxamides as Novel ROR?t Inverse Agonists. Eur. J. Med. Chem., 2018, 148, 465-476
3. Yonghui Wang,* Wei Cai, Ting Tang, Qian Liu, Ting Yang, Liuqing Yang, Yingli Ma, Guifeng, Zhang, Yafei Huang, Xiaoxia Song, Lisa A. Orband-Miller, Qianqian Wu, Ling Zhou, Zhijun Xiang, Jia-Ning Xiang, Stewart Leung, Liming Shao, Xichen Lin, Mercedes Lobera, and Feng Ren.* From ROR?t Agonist to Two Types of ROR?t Inverse Agonists. ACS Med. Chem. Lett. 2018, 9, 120-124
4. Yan Zhu, Juwen Gong, Yonghui Wang.* Free-radical-promoted copper-catalyzed decarboxylative alkylation of α,β-unsaturated carboxylic acids with ICH2CF3 and its analogs. J. Org. Chem., 2017, 82, 7428-7436
5. Ruomeng Qiu, Wenli Shi, Ting Cai, Siyu Pei, Ting Tang, Yafei Huang, Huan Wang, Liming Shao, Ju Qiu? and Yonghui Wang.? Design, synthesis and phenotypic evaluation of N-biaryl amides for IL-17A suppression. Med. Chem. Commun., 2016, 7, 2344 - 2348
6. Yonghui Wang,* Ting Yang, Qian Liu, Yingli Ma, Liuqing Yang, Ling Zhou, Zhijun Xiang, Ziqiang Cheng, Sijie Lu, Lisa A. Orband-Miller, Wei Zhang, Qianqian Wu, Kathleen Zhang, Yi Li, Jia-Ning Xiang, John D. Elliott, Stewart Leung, Feng Ren, Xichen Lin.* Discovery of N-(4-aryl-5-aryloxy-thiazol-2-yl)-amides as potent ROR?t inverse agonists. Bioorg. Med. Chem 2015, 23, 5293-5302
7. Yonghui Wang,* Wei Cai, Yaobang Cheng, Ting Yang, Qian Liu, Guifeng Zhang, Qinghua Meng, Fangbin Han, Yafei Huang, Ling Zhou, Zhijun Xiang, Yong-Gang Zhao, Yan Xu, Ziqiang Cheng, Sijie Lu, Qianqian Wu, Jia-Ning Xiang, John D. Elliott, Stewart Leung, Feng Ren, Xichen Lin.* Discovery of Biaryl Amides as Potent, Orally Bioavailable, and CNS Penetrant ROR?t Inhibitors. ACS Med. Chem. Lett. 2015, 6, 787-792
8. Sheng Xiao, Nir Yosef, Jianfei Yang, Yonghui Wang, Ling Zhou, Chen Zhu, Chuan Wu, Erkan Baloglu, Darby Schmidt, Radha Ramesh, Mercedes Lobera, Mark S. Sundrud, Pei-Yun Tsai, Zhijun Xiang, Jinsong Wang, Yan Xu, Xichen Lin, Karsten Kretschmer, Peter B. Rahl, Richard A. Young, Zhong Zhong, David A. Hafler, Aviv Regev, Shomir Ghosh, Alexander Marson,* Vijay K. Kuchroo.* “Small molecule ROR?t antagonists inhibit T helper 17 cell transcriptional network by divergent mechanisms”. Immunity 2014, 40, 477-489
9. Yonghui Wang,* Wei Cai, Guifeng Zhang, Ting Yang, Qian Liu, Yaobang Cheng, Ling Zhou, Yingli Ma, Ziqiang Cheng, Sijie Lu, Yong-Gang Zhao, Wei Zhang, Zhijun Xiang, Shuai Wang, Liuqing Yang, Qianqian Wu, Lisa A. Orband-Miller, Yan Xu, Jing Zhang, Ruina Gao, Melanie Huxdorf, Jia-Ning Xiang, Zhong Zhong, John D. Elliott, Stewart Leung, Xichen Lin. “Discovery of novel N-(5-(arylcarbonyl)thiazol-2-yl)amides and N-(5-(arylcarbonyl)thiophen-2-yl)amides as potent ROR?t inhibitors”. Bioorg. Med. Chem. 2014, 22, 692-702
10. Ting Yang, Qian Liu, Yaobang Cheng, Wei Cai, Yingli Ma, Liuqing Yang, Qianqian Wu, Lisa A. Orband-Miller, Ling Zhou, Zhijun Xiang, Melanie Huxdorf, Wei Zhang, Jing Zhang, Jia-Ning Xiang, Stewart Leung, Yang Qiu, Zhong Zhong, John D. Elliott, Xichen Lin and Yonghui Wang.* “Discovery of tertiary amine and indole derivatives as potent ROR?t inverse agonists”. ACS Med. Chem. Lett. 2014, 5, 65-68
Selected PCT Patents
1. Wang, Y., Huang, Y., Yu, M., Xie, Q. “Preparation of carbazole derivatives useful as RORγt modulators” International Patent Application No. PCT/CN2018/093715, Applied: 06/29/2018
2. Wang, Y., Huang, Y., Qiu, R., Tang, T. “Preparation of biaryl derivatives useful as RORγt agonists” International Patent No. WO2018145653A1, Published: 08/16/2018
3. Wang, Y., Huang, Y., Yu, F., Tang, T. “Preparation of biaryl urea derivatives useful as RORγt inhibitors” International Patent No. WO2017219935A1; Published 12/28/2017
4. Wang, Y., Cai, W., Liu, Q., Meng, Q., Cheng, Y., Yang, T., Zhang, G., Xiang, J., Wu, C. “Preparation of N-substituted 2-[4-(ethylsulfonyl)phenyl]acetamides as retinoid-related orphan receptor gamma modulators” International Patent No. WO2013029338A1; Published 03/07/2013
5. Wang, Y., Yang, T. “Preparation of N-thiazolyl phenylacetamides as retinoid-related orphan receptor gamma modulators” International Patent No. WO2012100734A1; Published 08/02/2012
6. Wang, Y., Yang, T. “Preparation N-thienyl phenylacetamides as retinoid-related orphan receptor gamma modulators” International Patent No. WO2012100732A1; Published 08/02/2012
7. Wang, Y., Yang, T.; Liu, Q.; Xiang, J.-N. “Preparation of N-thiazolyl acetamides as retinoid-related orphan receptor gamma (ROR) modulators” International Patent No. WO2012028100A1; Published 03/08/2012
8. Wang, Y., Cai, W.; Liu, Q.; Xiang, J.-N. “Preparation of thiazole derivatives as modulators of retinoid-related orphan receptor gamma” International Patent No. WO2012027965A1; Published 03/08/2012
9. Adams, G. L.; Brackley, J. A. III; Busch-Petersen, J.; deng, J.; Fu, W.; Li, H.; Taggart, J. J.; Wang, F.; Wang, Y.; Widdowson, K. L.; Yu, H. “Preparation of aminosulfonyl-N-thiadiazolylbenzamide for use as IL-8 receptor Antagonists” International Patent No. WO2008070707A1 ; Published 06/12/2008; US8044075B2 (granted on 10/25/2011)
10. Budzik, B.; Jin, J.; Laine, D.; Mccleland, B.; Palovich, M.; Rivero, R.; Wang, Y.; Xie, H.; Zhu, C.; Cooper, A. “Preparation of N-[(piperazinylmethyl)biphenyl]benzamide derivatives as M3 muscarinic acetylcholine receptor antagonists” International Patent No. WO2006055553A2, Published 05/26/2006; US7932247B2 (granted on 04/26/2011)
