Shanghai Institute of Material Medical Chinese Academy of Sciences

Biography

XU Shilin is a principal investigator at Shanghai Institute of Materia Medica, Chinese Academy of Sciences. After Dr. Xu received his PhD in medicinal chemistry at Guangzhou Institute of Biomedicine and Health, Chinese Academy of Sciences in 2014, he joined the laboratory of Professor Shaomeng Wang as a postdoc at University of Michigan, Ann Arbor. Upon completing his postdoc training in 2019, Dr. Xu began his independent professional career as a medicinal chemist at Shanghai Institute of Materia Medica. His laboratory’s research focuses on the design, synthesis and development of new drug molecules with an emphasis on drug resistance of tumor. Dr. Xu developed the first-in-class covalent inhibitors against the Menin-MLL protein-protein interaction, which has been licensed to a famous pharmaceutical company for further development.

Experience

Sep 2019 to Present, Principal Investigator, Shanghai Institute of Materia Medica, Chinese Academy of Science,

Nov 2014 to Sep 2019, Postdoc Research Fellow, University of Michigan, Ann Arbor,

Education

2009 to 2014, PhD in Medicinal Chemistry, Guangzhou Institute of Biomedicine and Health, Chinese Academy of Sciences

2005 to 2009, Bachelor’s Degress, Nanchang University

Research Directions

1.Development of small molecule drug overcoming the drug resistance of tumor

2.Discovery of chemical molecules targeting cancer immunology and metabolism.

Grants & Research Projects

Achievements

1.Dr. Xu designed and synthesized the first-in-class covalent inhibitors targeting the Menin-MLL interaction that can significantly suppress the growth of leukemia cell bearing MLL fusion in vitro and in vivo.

2.Dr. Xu discovered the most selective EGFR(T790M) inhibitor which can overcome the drug resistance of NSCLC harboring EGFR(T790M) mutant.

3.Dr. Xu developed a series of modulators of estrogen-related receport (ERR) which confirmed the function of ERR in triple-negative breast cancer.

Representative Patent

1.Shaomeng Wang, Shilin Xu, Angelo Aguilar, Liyue Huang, Jeanne Stuckey, PIPERIDINE COMPOUNDS AS COVALENT MENIN INHIBITORS (PCT/US 2019/024729)

2.Shaomeng Wang, Shilin Xu, Angelo Aguilar, Liyue Huang, Tianfeng Xu, CYCLOPENTYL CARBAMATES AS MENIN INHIBITORS (US patent application No.: 62/740,561)

3.Shaomeng Wang, Shilin Xu, Angelo Aguilar, Liyue Huang, SMALL MOLECULE MENIN INHIBITORS (US patent application No.:62/740,567)

4.Shaomeng Wang, Angelo Aguilar, Shilin Xu, Liyue Huang, Jeanne Stuckey, Tianfeng Xu, PIPERIDINES AS COVALENT MENIN INHIBITORS (PCT/US2018/025417)

5.Shaomeng Wang, Angelo Aguilar, Ke Zheng, Shilin Xu, Tianfeng Xu, Denzil Bernard, PIPERIDINES AS MENIN INHIBITORS (PCT/US2017/030577)

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Social Titles

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Awards & Honors

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Pubilcations

Full Publication List

Selected Publications

1. Xu, Shilin#; Aguilar, Angelo#; Huang, Liyue#; Xu, Tianfeng; Zheng, Ke; McEachern, Donna; Przybranowski, Sally; Foster, Caroline; Zawacki, Kaitlin; Liu, Zhaomin; Chinnaswamy, Krishnapriya; Stuckey, Jeanne; Wang, Shaomeng*, Discovery of M-808 as a Highly Potent, Covalent, Small-Molecule Inhibitor of the Menin–MLL Interaction with Strong In Vivo Antitumor Activity. Journal of Medicinal Chemistry 2020, 63 (9), 4997-5010. (# Co-first author)

2. Chang, Yu; Xu, Shilin; Ding, Ke*, Tyrosine Kinase 2 (TYK2) Allosteric Inhibitors To Treat Autoimmune Diseases. Journal of Medicinal Chemistry 2019, 62 (20), 8951-8952.

3. Xu, Shilin#; Aguilar, Angelo#; Xu, Tianfeng#; Zheng, Ke#; Huang, Liyue; Stuckey, Jeanne; Chinnaswamy, Krishnapriya; Bernard, Denzil; Fernández‐Salas, Ester; Liu, Liu; Wang, Mi; McEachern, Donna; Przybranowski, Sally; Foster, Caroline; Wang, Shaomeng*, Design of the first‐in‐class, highly potent irreversible inhibitor targeting the menin‐MLL protein–protein interaction. Angewandte Chemie International Edition 2018, 57 (6), 1601-1605. (# Co-first author)

4. Aguilar, Angelo#; Zheng, Ke#; Xu, Tianfeng#; Xu, Shilin#; Huang, Liyue#; Fernandez-Salas, Ester; Liu, Liu; Bernard, Denzil; Harvey, Kaitlin P.; Foster, Caroline; McEachern, Donna; Stuckey, Jeanne; Chinnaswamy, Krishnapriya; Delproposto, James; Kampf, Jeff W.; Wang, Shaomeng*, Structure-Based Discovery of M-89 as a Highly Potent Inhibitor of the Menin-Mixed Lineage Leukemia (Menin-MLL) Protein–Protein Interaction. Journal of medicinal chemistry 2019, 62 (13), 6015-6034. (# Co-first author)

5. Xu, Shilin#; Mao, Liufeng#; Ding, Ping#; Zhuang, Xiaoxi; Zhou, Yang; Yu, Lei; Liu, Yingxue; Nie, Tao; Xu, Tingting; Xu, Yong; Liu, Jinsong; Smaill, Jeff; Ren, Xiaomei*; Wu, Donghai*; Ding, Ke*, 1-Benzyl-4-phenyl-1H-1,2,3-triazoles improve the transcriptional functions of estrogen-related receptor γ and promote the browning of white adipose. Bioorganic & Medicinal Chemistry 2015, 23 (13), 3751-3760. (# Co-first author)

6. Xu, Shilin; Xu, Tianfeng; Zhang, Lianwen; Zhang, Zhang; Luo, Jinfeng; Liu, Yingxue; Lu, Xiaoyun; Tu, Zhengchao; Ren, Xiaomei; Ding, Ke*, Design, Synthesis, and Biological Evaluation of 2-Oxo-3,4-dihydropyrimido[4,5-d]pyrimidinyl Derivatives as New Irreversible Epidermal Growth Factor Receptor Inhibitors with Improved Pharmacokinetic Properties. Journal of medicinal chemistry 2013, 56 (21), 8803-8813.

7. Xu, Shilin; Zhuang, Xiaoxi; Pan, Xiaofen; Zhang, Zhang; Duan, Lei; Liu, Yingxue; Zhang, Lianwen; Ren, Xiaomei*; Ding, Ke*, 1-Phenyl-4-benzoyl-1H-1,2,3-triazoles as Orally Bioavailable Transcriptional Function Suppressors of Estrogen-Related Receptor α. Journal of medicinal chemistry 2013, 56 (11), 4631-4640.

8. Xu, Shilin; Zhang, Lianwen; Chang, Shaohua; Luo, Jinfeng; Lu, Xiaoyun; Tu, Zhengchao; Liu, Yingxue; zhang, Zhang; Xu, Yong; Ren, Xiaomei; Ding, Ke*, Design, synthesis and biological evaluation of new molecules inhibiting epidermal growth factor receptor threonine790→ methionine790 mutant. MedChemComm 2012, 3 (9), 1155-1159.

9. Xu, Tianfeng#; Zhang, Lianwen#; Xu, Shilin; Yang, Chao-Yie; Luo, Jinfeng; Ding, Fang; Lu, Xiaoyun; Liu, Yingxue; Tu, Zhengchao; Li, Shiliang; Pei, Duanqing; Cai, Qian; Li, Honglin; Ren, Xiaomei; Wang, Shaomeng; Ding, Ke*, Pyrimido[4,5-d]pyrimidin-4(1H)-one Derivatives as Selective Inhibitors of EGFR Threonine790 to Methionine790 (T790M) Mutants. Angewandte Chemie International Edition 2013, 52 (32), 8387-8390.

10. Chang, Shaohua#; Zhang, Lianwen#; Xu, Shilin; Luo, Jinfeng; Lu, Xiaoyun; Zhang, Zhang; Xu, Tianfeng; Liu, Yingxue; Tu, Zhengchao; Xu, Yong; Ren, Xiaomei; Geng, Meiyu; Ding, Jian; Pei, Duanqing; Ding, Ke*, Design, Synthesis, and Biological Evaluation of Novel Conformationally Constrained Inhibitors Targeting Epidermal Growth Factor Receptor Threonine790 → Methionine790 Mutant. Journal of medicinal chemistry 2012, 55 (6), 2711-2723.

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