Professor of Medicinal Chemistry
Department of Medicinal Chemistry
School of Pharmacy
Phone: 13951619649
Email: haiyings1969@163.com
Research Summary
Professor Sun’s research interest is in the design, synthesis and biological evaluation of novel small molecular agents targeting crucial proteins in human diseases. He played a leading role in a project to identify small molecular inhibitors of IAPs. Two clinical candidates have been identified in this project and are currently in Phase I/II studies. He has been awarded 9 US Patents and published 30+ papers on top journals in the fields of Medicinal Chemistry and Organic Chemistry.
Education
2000 Ph.D., Organic Chemistry, Shanghai Institute of Organic Chemistry
1997 M.S., Organic Chemistry, Lanzhou University
1991 B.S., Applied Chemistry, Lanzhou University
Academic Experience
2014- Professor of Medicinal Chemistry, China Pharmaceutical University
2008-2014 Research Assistant Professor, University of Michigan
2003-2008 Research Investigator, University of Michigan
2002-2003 Postdoctoral Research Fellow, University of Michigan
2000-2002 Postdoctoral Research Fellow, Georgetown University
Awards and Honors
2013 Specially Appointed Professor of Jiangsu Province
Representative Publications
Haiying Sun, Jianfeng Lu, Liu Liu, Han Yi, Su Qiu, Chao-Yie Yang and Shaomeng Wang; Potent and Selective Small-Molecule Inhibitors of cIAP1/2 Proteins Reveal That the Binding of Smac Mimetics to XIAP BIR3 Is Not Required for Their Effective Induction of Cell Death in Tumor Cells; ACS Chem. Bio.; 2014, 9(4); 994-1002.
Rong Sheng, Haiying Sun, Liu Liu, Jianfeng Lu, Donna McEachern, Guanfeng Wang, Jianfeng Wen, Ming Guo, Dajun Yang and Shaomeng Wang. A Potent Bivalent Smac Mimetic (SM-1200) Achieving Rapid, Complete, and Durable Tumor Regression in Mice; J. Med. Chem., 2013, 56(10), 3969-3979.
Yuefeng Peng, Haiying Sun, Jianfeng Lu, Liu Liu, Han Yi, Su Qiu, Chao-Yie Yang and Shaomeng Wang*; Bivalent Smac mimetics with a diazabicyclic core as highly potent antagonists of XIAP and cIAP1/2 and novel anticancer agents; J. Med. Chem.;2012, 55(1), 106-114.
Haiying Sun, Liu Liu, Jianfeng Lu, Longchuan Bai, Xiaoqin Li, Zaneta Nikolovska-Coleska,Chao-Yie Yang, Su Qiu, Han Yi, Duxin Sun and Shaomeng Wang*; PotentbivalentSmacmimetics: effect of the linker on binding to inhibitor of apoptosis proteins (IAPs) and anticancer activity; J. Med. Chem.; 2011; 54(9); 3306-3318.
Qian Cai, Haiying Sun (co-first author), Yuefeng Peng, Jianfeng Lu, Zaneta Nikolovska-Coleska, Donna McEachern, Liu Liu, Su Qiu, Chao-Yie Yang, Rebecca Miller, Han Yi, Tao Zhang, Duxin Sun, Sanmao Kang, Ming Guo, Dajun Yang, Shaomeng Wang. A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment; J. Med. Chem.; 2011; 54(8);2714-2726.
Haiying Sun, Jianfeng Lu, Liu Liu, Han Yi, Su Qiu, Chao-Yie Yang, Jeffrey R. Deschamps and Shaomeng Wang. Nonpeptidic and potentsmall-moleculeinhibitors of cIAP-1/2 and XIAPproteins; J. Med. Chem., 2010, 53(17), 6361-6367.
Haiying Sun, Liu Liu, Jianfeng Lu, Su Qiu, Chao-Yie Yang, Han Yi, Shaomeng Wang*; Cyclopeptide Smac mimetics as antagonists of IAP proteins; Bioorg. Med. Chem. Lett. 2010, 20 (10); 3043-3046.
Chao-Yie Yang, Haiying Sun, Jianyong Chen, Zaneta Nikolovska-Coleska, Shaomeng Wang; Importance of Ligand Reorganization Free Energy in Protein-Ligand Binding-Affinity Prediction; Journal of the American Chemical Society; 2009, 131(38), 13709-13721.
Haiying Sun, Zaneta Nikolovska-Coleska, Chao-Yie Yang, Dongguang Qin, Jianfeng Lu, Su Qiu, Longchuan Bai, Yuefeng Peng, Qian Cai, and Shaomeng Wang. Design of Small-Molecule Peptidic and Non-Peptidic Smac Mimetics. Accounts of Chemiscal Research (article); 2008, 41(10), 1264-1277.
Haiying Sun, Jeanne A. Stuckey, Zaneta Nikolovska-Coleska, Dongguang Qin, Jennifer L. Meagher, Su Qiu, Jianfeng Lu, Chao-Yie Yang, Naoyuki G. Saito and Shaomeng Wang. Structure-Based Design, Synthesis, Evaluation, and Crystallographic Studies of Conformationally Constrained Smac Mimetics as Inhibitors of the X-linked Inhibitor of Apoptosis Protein (XIAP). J. Med. Chem.; (Article); 2008, 51 (22), 7169-7180.
Jianfeng Lu, Longchuan Bai, Haiying Sun, Zaneta Nikolovska-Coleska, Donna McEachern, Su Qiu, Rebecca S. Miller, Han Yi, Sanjeev Shangary, Yi Sun, Jennifer L. Meagher, Jeanne A. Stuckey and Shaomeng Wang. SM-164: a novel, bivalent Smac mimetic that induces apoptosis and tumor regression by concurrent removal of the blockade of cIAP-1/2 and XIAP.Cancer Research; 2008, 68 (22), 9384-9393.
Yuefeng Peng, Haiying Sun, Zaneta Nikolovska-Coleska, Chao-YieYang, Su Qiu, Jianfeng Lu, Qian Cai, Han Yi and Shaomeng Wang. Design, Synthesis and Evaluation of Potent and Orally Bioavailable Diazabicyclic Smac Mimetics. J. Med. Chem.; 2008, 51 (24), 8151-8162.
Haiying Sun, Zaneta Nikolovska-Coleska, Jianfeng Lu, Jennifer L. Meagher, Chao-Yie Yang, Su Qiu, Krzysztof Krajewski, Peter P. Roller, Jeanne Stuckey, and Shaomeng Wang. Design, Synthesis and Characterization of A Non-Peptide, Cell-Permeable, Bivalent Smac Mimetic that Targets both the BIR2 and BIR3 Domains in XIAP. J. Am. Chem. Soc.; (article) 2007, 15279-15294.
Haiying Sun, Zaneta Nikolovska-Coleska, Jianfeng Lu, Su Qiu, Chao-Yie Yang, Wei Gao, Jennifer Meagher, Jeanne Stuckey and Shaomeng Wang. Design, Synthesis, and Evaluation of a Potent, Cell-Permeable, Conformationally Constrained Second Mitochondria Derived Activator of Caspase (Smac) Mimetic, J. Med. Chem.;(Brief Article); 2006; 49(26); 7916-7920.
Haiying Sun, Zaneta Nikolobska-Coleska, Chao-Yie Yang, Liang Xu, York Tomita, Peter Roller and Shaomeng Wang, Design, Synthesis and Evaluation of Highly Potent Conformationally Constrained Smac Mimetics, Journal of the American Chemical Society (communication), 2004, 126 (51), 16686-16687.
Haiying Sun; Zaneta Nikolovska-Coleska; Chao-Yie Yang; Liang Xu; York Tomita; Peter P Roller; Shaomeng Wang Structure-Based Design, Synthesis, and Evaluation of Conformationally Constrained Mimetics of the Second Mitochondria-Derived Activator of Caspase That Target theX-Linked Inhibitor of Apoptosis Protein/Caspase-9 Interaction Site. J. Med.Chem. 2004, 47 (17), 4147-4150.
Alan P. Kozikowski; Haiying Sun; John Brognard; Phillip A. Dennis Novel PI Analogues Selectively Block Activation of the Pro-survival Serine/Threonine Kinase Akt. J. Am. Chem. Soc. (communication). 2003, 125 (5), 1144-1145.
Dawei Ma and Haiying Sun. A Simple and Stereospecific Route to 2,6-Disubstituted 4-Hydroxypiperidines. Synthesis of Dendrobate Alkaloid (+)-241D and Formal Synthesis of (-)-Indolizidine 167B. Organic Letters. 2000, 2 (16), 2503-2505.
Dawei Ma and Haiying Sun. General Route to 2,4,5-Trisubstituted Piperidines from Enantiopure -Amino Esters. Total Synthesis of Pseudodistomin B Triacetate and Pseudodistomin F. Journal of Organic Chemistry. 2000, 65 (19), 6009-6016.
Awarded Patents
Shaomeng Wang and Haiying Sun. Bivalent diazo bicyclic Smac mimetics and the use thereof. U.S Pat. Appl. Pub. (2011), 90pp. WO/2011/05006; PCT/US2010/053384.
Shaomeng Wang, Haiying Sun, Dongguang Qin, Zaneta Nikolovska-Coleska, Jianfeng Lu, Su Qiu, Yuefeng Peng and Qian Cai. Preparation of bivalent conformationally constrained Smac peptide mimetics as inhibitors of IAP proteins and inducers of apoptosis. U.S Pat. Appl. Publ. (2009), 137pp, Cont.-in-part of U.S. Ser. No. 800,220.
Shaomeng Wang, Yuefeng Peng, Haiying Sun, Qian Cai, Zaneta Nikolovska-Coleska, Jianfeng Lu, Su Qiu. Preparation of diazo bicyclic conformationally constrained Smac peptide mimetics as inhibitors of IAP proteins and inducers of apoptosis. PCT Int. Appl. (2008), 197pp. CODEN; PIXXD2 WO 2008128171 A2 20081023 Can 149;471831 An 2008:1282410 CAPLUS
Shaomeng Wang, Haiying Sun, Dongguang Qin, Zaneta Nikolovska-Coleska, Jianfeng Lu, Su Qiu, Yuefeng Peng and Qian Cai. Preparation of bivalent conformationally constrained Smac peptide mimetics as inhibitors of IAP proteins and inducers of apoptosis. PCT Int. Appl. (2007), 137pp. CODEN: PIXXD2 WO 2007130626 A2 20071115 CAN 147:542134 AN 2007:1302836.
Shaomeng Wang, Haiying Sun, Zaneta Nikolovska-Coleska, Chao-Yie Yang, Liang Xu, Naoyuki Saito and Jianyong Chen. Preparation of conformationally-constrained Smac peptidomimetics for use in inducing apoptosis. PCT Int. Appl. (2006), 127 pp. CODEN: PIXXD2 WO 2006010118 A2 20060126 AN 2006:79326 CAPLUS
Shaomeng Wang, Haiying Sun, Zaneta Nikolovska-Coleska, Chao-Yie Yang, Liang Xu. Conformationally constrained Smac mimetics and use in inducing apoptosis. PCT Int. Appl. (2005), 125 pp. CODEN: PIXXD2 WO 2005069894 A2 20050804 CAN 143:166630 AN 2005:696610 CAPLUS
Shaomeng Wang, Haiying Sun, Zaneta Nikolovska-Coleska, Chao-Yie Yang, Liang XuSmac peptidomimetics and use in inducing apoptosis. PCT Int. Appl. (2005), 110 pp. CODEN: PIXXD2 WO 2005069888 A2 20050804 CAN 143:166629 AN 2005:696606 CAPLUS
Shaomeng Wang, Haiying Sun, Zaneta Nikolovska-Coleska, Chao-Yie Yang, Liang Xu, Dajun Yang, Zengjian Hu and Guoping Wang. Embelin and other small molecule antagonists of XIAP family proteins, and therapeutic use thereof. PCT Int. Appl. (2005), 130 pp. CODEN: PIXXD2 WO 2005092326 A1 20051006 CAN 143:360077 AN 2005:1075624 CAPLUS
Alan P. Kozikowski; Phillip A. Dennis; Haiying Sun; John Brognard. Preparation of cyclitols as serine/threonine kinase Akt inhibitors. PCT Int. Appl. (2004), 41 pp. WO 2004022569 A1 20040318
