周璐
药物化学, 教授, 博士生导师

姓      名

 周璐

性      别

 男

职      称

 教授

学      历

 博士

电      话

 021-51980125 

传      真

 021-51980125

电子邮件

 zhoulu@fudan.edu.cn 

个人主页

 http://spfdu.fudan.edu.cn 

通讯地址

 上海市浦东新区张衡路826号实验南楼315室

 

教育经历

(1) 2001.9–2006.7, 北京大学化学与分子工程学院, 博士

(2) 1997.9–2001.7, 北京大学化学与分子工程学院,学士

工作经历

(1)2019.12- 至今复旦大学药学院, 教授

(2)2013.12-2019.11 复旦大学药学院, 副教授

(3)2010.9-2012.7 芝加哥大学化学系, 访问学者

(4)2008.7-2013.11 复旦大学药学院, 讲师

(5)2006.7-2008.7北京大学化学与分子工程学院, 博士后

承担科研项目情况

1、国家自然科学基金面上项目,21877014, 小分子介导的位点选择性PGAM1赖氨酸乙酰化研究,2019/01-2022/12。

2、国家自然科学基金面上项目,21472026,作用于磷酸甘油酸变位酶1变构位点的抑制剂设计、合成及生物活性测定,2015/01-2018/12。

3、上海市青年科技启明星计划,15QA1400300,抗肿瘤新靶标PGAM1的药物研究,2015/04-2018/03。

4、上海市科委面上项目,13ZR1403900,磷酸甘油酸变位酶抑制剂研究,2013/07-2016/6。

5、国家自然科学基金青年项目,20902013,磷脂酶及鞘磷脂合成酶双功能抑制剂研究,2010/01-2012/12。

研究方向

主要从事药物化学生物学研究,研究方向为“全新靶点的小分子药物设计合成”。主要围绕抗肿瘤新靶点的药物分子设计合成与机制研究,致力于发现具有良好开发前景的新型候选药物。现主要研究课题有:磷酸甘油酸变位酶1(PGAM1)抑制剂设计合成,针对肿瘤HIF-1α的小分子新靶标确认和机制研究等。

科研成果

主持国家自然科学基金项目多项,入选上海市“青年科技启明星”计划、复旦大学首届“卓学”计划。在国内外学术刊物发表科研论文和教学论文共70余篇,其中通讯作者和第一作者SCI论文20余篇,IF>20的论文3篇(Cancer Cell 2012, Nature Chemistry 2014, Cell Metabolism 2019),申请国家发明专利6项,其中已授权4项,并申请和获得美国、日本等国家和地区的专利授权。

代表性论著

1Zhang XD, Jiang, LlL, Huang K, Fang CT, Li J, Yang JT, Li HT, Ruan XX, Wang PH, Mo MG, Wu P, Xu YH, Peng C, Uesugi M, Ye DY*, Yu FX*, Zhou L*. Site-Selective Phosphoglycerate Mutase 1 Acetylation by a Small Molecule.  ACS Chem. Biol. 2020, 15(3): 632-639.

2Wen CL, Huang K, Jiang LL, Lu XX, Dai YT, Shi MM, Tang XM, Wang QB, Zhang XD, Wang PH, Li HT, Ruan XX, Wang LW, Wang XJ, Wang Q, Lu W, Xiang XQ, Sun X, Xu YH, Lai LH, Zhan Q, Li HW, Peng CH, Chen J, Huang JY, Ye DY, Chen SJ, Chen Z*, Li M*, Fang Y*, Shen BY*, Zhou L*. An allosteric PGAM1 inhibitor effectively suppresses pancreatic ductal adenocarcinoma. Proc Natl Acad Sci U S A. 2019 ;116(46):23264-23273.

3Huang K, Liang Q, Zhou Y, Jiang LL, Gu WM, Luo MY, Tang YB, Wang Y, Lu W, Huang M, Zhang SZ, Zhuang GL, Dai Q, Shen QC, Zhang J, Lei HM, Zhu L, Ye DY, Chen HZ*, Zhou L*, Shen Y*. A Novel Allosteric Inhibitor of Phosphoglycerate Mutase 1 Suppresses Growth and Metastasis of Non-Small-Cell Lung Cancer. Cell Metab. 2019. 30(6):1107-1119.

4Huang K, Jiang L, Li H, Ye D*, Zhou L*. Development of Anthraquinone Analogues as Phosphoglycerate Mutase 1 Inhibitors. Molecules. 2019; 24(5). pii: E845.

5Huang K, Jiang L, Liang R, Li H, Ruan X, Shan C, Ye D*, Zhou L*. Synthesis and biological evaluation of anthraquinone derivatives as allosteric phosphoglycerate mutase 1 inhibitors for cancer treatment. Eur. J. Med. Chem. 2019;168:45-57.

6Li Y, Huang T, Lou B, Ye D, Qi X, Li X, Hu S, Ding T, Chen Y, Cao Y, Mo M, Dong J, Wei M, Chu Y, Li H, Jiang XC*, Cheng N*, Zhou L*. Discovery, synthesis and anti-atherosclerotic activities of a novel selective sphingomyelin synthase 2 inhibitor. Eur. J. Med. Chem. 2019; 163:864-882.

7Yang X, Shen J, Jiang L, Li W, Yu M, Pan G, Yan Y, Zhang C, Jia W, Xiao L, Yu H, Chen H, Zheng Y, Yu L, Xie Q*, Zhou L*, Shao L*. Discovery, cocrystallization and biological evaluation of novel piperidine derivatives as high affinity Ls-AChBP ligands possessing α7 nAChR activities. Eur J Med Chem. 2018;160:37-48.

8Mo M, Yang J, Jiang XC, Cao Y, Fei J, Chen Y, Qi X, Chu Y, Zhou L*, Ye D*. Discovery of 4-Benzyloxybenzo[ d]isoxazole-3-amine Derivatives as Highly Selective and Orally Efficacious Human Sphingomyelin Synthase 2 Inhibitors that Reduce Chronic Inflammation in db/ db Mice. J. Med. Chem. 2018; 61(18):8241-8254.

9Wang P, Jiang L, Cao Y, Ye D*, Zhou L*. The Design and Synthesis of N-Xanthone Benzenesulfonamides as Novel Phosphoglycerate Mutase 1 (PGAM1) Inhibitors. Molecules. 2018; 23(6). pii: E1396.

10Wang P, Jiang L, Cao Y, Zhang X, Chen B, Zhang S, Huang K, Ye D*, Zhou L*. Xanthone derivatives as phosphoglycerate mutase 1 inhibitors: Design, synthesis, and biological evaluation. Bioorg. Med. Chem. 2018; 26(8):1961-1970.

11Liu SE, Hu JC, Zhang H, Xu P, Wan W, Zheng MY, Yu KQ, Ding H, Jiang HL, Zhou L*, Luo C*. Conformation and dynamics of the C-terminal region in human phosphoglycerate mutase 1. Acta Pharmacol Sin. 2017 Jul 27.

12Song J, Peng P, Chang J, Liu MM, Yu JM, Zhou L*, Sun X*. Selective non-zinc binding MMP-2 inhibitors: Novel benzamide Ilomastat analogs with anti-tumor metastasis. Bioorg Med Chem Lett. 2016; 26(9):2174-8.

13 Zhou L#, Bosscher M#, Zhang C#, Oz?ubuk?u S, Zhang L, Zhang W, Li CJ, Liu J, Jensen MP, Lai L, He C. A protein engineered to bind uranyl selectively and with femtomolar affinity. Nat Chem. 2014;6(3):236-41.

14Hitosugi T#, Zhou L#, Fan J, Elf S, Zhang L, Xie J, Wang Y, Gu TL, Ale?kovi? M, LeRoy G, Kang Y, Kang HB, Seo JH, Shan C, Jin P, Gong W, Lonial S, Arellano ML, Khoury HJ, Chen GZ, Shin DM, Khuri FR, Boggon TJ, Kang S, He C, Chen J. Tyr26 phosphorylation of PGAM1 provides a metabolic advantage to tumours by stabilizing the active conformation. Nat Commun. 2013;4:1790. (#contribute equally)

15Hitosugi T#, Zhou L#, Elf S, Fan J, Kang HB, Seo JH, Shan C, Dai Q, Zhang L, Xie J, Gu TL, Jin P, Ale?kovi? M, LeRoy G, Kang Y, Sudderth JA, DeBerardinis RJ, Luan CH, Chen GZ, Muller S, Shin DM, Owonikoko TK, Lonial S, Arellano ML, Khoury HJ, Khuri FR, Lee BH, Ye K, Boggon TJ, Kang S, He C, Chen J. Phosphoglycerate mutase 1 coordinates glycolysis and biosynthesis to promote tumor growth. Cancer Cell. 2012;22(5):585-600. (#contribute equally)


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