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中国科学院上海药物研究所导师教师师资介绍简介-徐石林

本站小编 Free考研考试/2021-02-10

xm:徐石林
xb:男
zc:研究员
xl:博士
dh:-2115
cz:
dzyj:slxu@simm.ac.cn
grzy:
zjlb:研究员
zw:课题组长
txdz:上海市浦东新区张江高科技园区海科路501号 201203
grjj:徐石林,中国科学院上海药物研究所研究员,课题组长。2014年于中国科学院广州生物医药与健康研究院获得博士学位,随后进入美国密歇根大学安娜堡分校进行博士后研究,2019年9月加入上海药物研究所,担任课题组长。主要从事新药分子设计、合成与开发工作,围绕克服肿瘤耐药这一重大临床需求,取得了一系列重要成果,相关工作在Angew. Chem. Int. Ed.; J. Med. Chem等国际学术期刊发表文章10 篇,同时申请了多项中国和国际发明专利,部分专利已获授权。作为Menin抑制剂项目的主要贡献者,设计了该靶点的世界首个共价抑制剂,推动了该项目成功转让给国际著名制药公司,使合作团队获得了高额转让费。


yjfx:1.克服肿瘤耐药的小分子药物开发,
2.靶向肿瘤免疫和肿瘤代谢的新药小分子开发及抗肿瘤机制研究
dblz: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.

代表专利:

1. 丁克,徐石林,徐田锋,张连文,丁芳,涂正超,陆小云,丁健,耿美玉,嘧啶并杂环类化合物及其药用组合物和应用(中国授权专利号:0X)

2. 丁克,徐石林,庄晓曦,潘小芬,张章,段磊,陆小云,用作雌激素相关受体调节剂的化合物及其应用(中国授权专利号:20**)

3. 丁克,徐石林,常少华,张连文,涂正超,许永,陆小云,嘧啶并二氮杂卓类化合物及其药用组合物和应用(中国授权专利号:7X)

4. 丁克,常少华,徐石林,张连文,涂正超,丁健,耿美玉,陈奕,嘧啶并嘧啶酮类化合物及其药用组合物和应用(中国授权专利号:99)

5. 丁克,徐田锋,常少华,张连文,罗金凤,徐石林,肖宜平,涂正超,嘧啶并三环或嘧啶并四环类化合物及其药用组合物和应用(中国,授权专利号:93)

6. Shaomeng Wang, Shilin Xu, Angelo Aguilar, Liyue Huang, Jeanne Stuckey, PIPERIDINE COMPOUNDS AS COVALENT MENIN INHIBITORS (PCT专利申请号:PCT/US 2019/024729)

7. Shaomeng Wang, Shilin Xu, Angelo Aguilar, Liyue Huang, Tianfeng Xu, CYCLOPENTYL CARBAMATES AS MENIN INHIBITORS (美国专利申请号:62/740,561)

8. Shaomeng Wang, Shilin Xu, Angelo Aguilar, Liyue Huang, SMALL MOLECULE MENIN INHIBITORS (美国专利申请号:62/740,567)

9. Shaomeng Wang, Angelo Aguilar, Shilin Xu, Liyue Huang, Jeanne Stuckey, Tianfeng Xu, PIPERIDINES AS COVALENT MENIN INHIBITORS (PCT专利申请号:PCT/US2018/025417)

10. Shaomeng Wang, Angelo Aguilar, Ke Zheng, Shilin Xu, Tianfeng Xu, Denzil Bernard, PIPERIDINES AS MENIN INHIBITORS (PCT专利申请号:PCT/US2017/030577)


jyjl:南昌大学,理学学士
中国科学院广州生物医药与健康研究院,药物化学,理学博士
gzjl:美国密歇根大学,博士后中国科学院上海药物研究所,研究员,课题组长
ktxm:中国科协“青年人才托举工程”(2019-2021QNRC001)(人才基金)上海市“科技创新行动计划”自然科学基金面上项目(20ZR**)
ryhj:第五届中国科协“青年人才托举工程”广东省科学技术奖励二等奖广州市科学技术奖励一等奖中国科学院院长优秀奖博士研究生国家奖学金第四届中国青年创业大赛金奖
xpwj:http://sourcedb.simm.cas.cn/zw/gb2020/yjzz/202008/P.jpg
kycg:围绕克服肿瘤耐药这一重大临床需求,取得了一系列重要成果:1. 设计合成了世界首个Menin-MLL蛋白-蛋白相互作用的共价抑制剂,成功克服了携带 MLL 突变白血病细胞的耐药;2. 设计合成了具有最强选择性的EGFRT790M激酶抑制剂,可用于克服携带EGFRT790M突变的非小细胞肺癌耐药问题;3. 设计合成了一系列雌激素相关受体(ERR)的选择性调节剂,成功验证了孤儿核受体ERR可作为克服三阴性乳腺癌耐药的新靶点。
shrz:
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