Shanghai Institute of Material Medical Chinese Academy of Sciences

Biography

Shilin Xu 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 small-molecule drugs, particularly targeting epigenetic and immune-related therapeutic targets for the treatment of cancer and autoimmune diseases.

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 Degree, Nanchang University

Research Directions

1. Development of small-molecule drugs targeting epigenetic and immunity-related proteins

2. Design and discovery of bioactive lead compounds using innovative drug design strategies (e.g. covalent inhibition, induced proximity-based degrader)

Grants & Research Projects

Achievements

1. Developed the first covalent inhibitors and protein degraders targeting methylation-regulating enzymes such as METTL3, MLL, and NSD, achieving efficient modulation and demonstrating outstanding antitumor efficacy.

2. Designed highly selective inhibitors against phosphorylation-regulating kinases, including ZAP-70, HPK1, and TTK, enabling precise regulation and exhibiting significant therapeutic potential in disease treatment.

3. Discovered potent inhibitors targeting tumor immunotherapy-related enzymes such as QPCTL and ENPP1, which markedly enhanced antitumor immune responses.

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Social Titles

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Awards & Honors

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Publications

Selected Publications

1.Qian Zhang; Yingqi He; Danni Rao; Rui He; Lei Yu; Yaoliang Sun; Yuanhui Lai; Zihan Shi; Lijie Peng; Zhang Zhang; Shilin Xu, Discovery of an Efficacious RET PROTAC Degrader with Enhanced Antiproliferative Activity against Resistant Cancer Cells Harboring RET Solvent-Front Mutations. J. Med. Chem. 2025, 68 (1), 753-775.

2.Lei Yu; Yaoliang Sun; Longyan Xie; Xiao Tan; Ping Wang; Shilin Xu, Targeting QPCTL: An emerging therapeutic opportunity. J. Med. Chem. 2025, 68 (2), 929-943.

3.Jingqing Liu; Chaoming Huang; Shengrong Li; Lijie Peng; Yaoliang Sun; Jianzhang Yang; Shan Li; Shilin Xu; Xiaoyun Lu; Ke Ding; Zhengqiu Li, Proteome-Wide Ligand and Target Discovery by Using Covalent Probes and Natural Products. J. Med. Chem. 2025, 68 (19), 20228-20242. (Corresponding author)

4.Yaoliang Sun; Manman Chen; Yuyan Han; Weiqiang Li; Xiaoyu Ma; Zihan Shi; Yang Zhou; Lan Xu; Lei Yu; Yuxiang Wang; Jinghua Yu; Xingxing Diao; Linghua Meng; Shilin Xu, Discovery of Pyrido[2,3-d]pyrimidin-7-one Derivatives as Highly Potent and Efficacious Ectonucleotide Pyrophosphatase/Phosphodiesterase 1 (ENPP1) Inhibitors for Cancer Treatment. J. Med. Chem. 2024, 67 (5), 3986-4006.

5.Wenhao Du; Yuting Huang; Xiaoai Chen; Yue Deng; Yaoliang Sun; Hong Yang; Qiongyu Shi; Feifei Wu; Guobin Liu; He Huang; Jian Ding; Xun Huang; Shilin Xu, Discovery of a PROTAC degrader for METTL3-METTL14 complex. Cell Chem. Biol. 2024, 31 (1), 177-183 e17.

6.Lei Yu; Pengcheng Zhao; Yaoliang Sun; Zening Zheng; Wenhao Du; Lishan Zhang; Yaxu Li; Longyan Xie; Shilin Xu; Ping Wang, Development of a potent benzonitrile-based inhibitor of glutaminyl-peptide cyclotransferase-like protein (QPCTL) with antitumor efficacy. Signal Transduct. Target. Ther. 2023, 8 (1), 454. (Corresponding author)

7.Danni Rao; Tao Yang; Huixu Feng; Qi An; Shaofeng Zhang; Jinghua Yu; Xuelian Ren; Xingxing Diao; He Huang; Wei Tang; Shilin Xu, Discovery and Structural Optimization of Covalent ZAP-70 Kinase Inhibitors against Psoriasis. J. Med. Chem. 2023, 66 (17), 12018-12032.

8.Na Li; Hong Yang; Ke Liu; Liwei Zhou; Yuting Huang; Danyan Cao; Yanlian Li; Yaoliang Sun; Aisong Yu; Zhiyan Du; Feng Yu; Ying Zhang; Bingyang Wang; Meiyu Geng; Jian Li; Bing Xiong; Shilin Xu; Xun Huang; Tongchao Liu, Structure-Based Discovery of a Series of NSD2-PWWP1 Inhibitors. J. Med. Chem. 2022, 65 (13), 9459-9477. (Corresponding author)

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

10.Shilin Xu; Angelo Aguilar; Tianfeng Xu; Ke Zheng; Liyue Huang; Jeanne Stuckey; Krishnapriya Chinnaswamy; Denzil Bernard; Ester Fernández‐Salas; Liu Liu; Mi Wang; Donna McEachern; Sally Przybranowski; Caroline Foster; Shaomeng Wang, Design of the First‐in‐class, Highly Potent Irreversible Inhibitor Targeting the Menin‐MLL Protein–protein Interaction. Angew. Chem. Int. Ed. 2018, 57 (6), 1601-1605.

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