100701-药物化学

蛋白降级剂的设计与生物学研究

2009-09--2014-05   华东师范大学   博士学位
2001-09--2005-06   上海师范大学   学士学位

   

2019-07~2020-12,美国佛罗里达大学, 科研助理教授
2018-06~2019-07,美国佛罗里达大学, 博士后
2014-12~2018-05,美国阿肯色大学医学部, 博士后
2014-08~2014-11,华东师范大学, 科研助理
2005-07~2009-09,中国科学院上海药物研究所, 研究助理

   

[1] 吕伟, 刘雅倩, 张翾, 方艳芬, 罗宇, 鲍彬, 章雄文. 一种应用于靶向给药系统的新的支链连接体. CN: CN104587487A, 2015-05-06.
[2] 沈竞康, 耿美玉, 章海燕, 陈越磊, 姜如炜, 杜晓光, 傅燕, 张翾, 胡定宇, 王昕, 孟韬. 一种寡糖类化合物在神经保护方面的应用. CN: CN103340881A, 2013-10-09.
[3] 罗宇, 黄颖, 张翾, 吕伟, 谢欣, 王志龙. 手性茚满衍生物及其制备方法和用途. CN: CN103193668A, 2013-07-10.
[4] 吕伟, 张翾, 罗宇, 陈奕, 李佳, 李静雅, 丁健. 含有异羟肟酸结构的表鬼臼毒化合物及制备方法和用途. CN: CN102603761A, 2012-07-25.

   

[1] Li Hu, Chanjuan Dong, Zhe Wang, Shengyuan He, Yiwen Yang, Meiting Zi, Huiqin Li, Yanghuan Zhang, Chuanjie Chen, Runzi Zheng, Shuting Jia, Jing Liu, Xuan Zhang, Yonghan He. A rationally designed fluorescence probe achieves highly specific and long-term detection of senescence in vitro and in vivo. Aging Cell[J]. 2023, https://onlinelibrary.wiley.com/doi/10.1111/acel.13896.
[2] Chuanjie Chen, Yiwen Yang, Zhe Wang, Huiwen Li, Chanjuan Dong, Xuan Zhang. Recent Advances in Pro-PROTAC Development to Address On-Target Off-Tumor Toxicity. JOURNAL OF MEDICINAL CHEMISTRY[J]. 2023, https://pubs.acs.org/doi/10.1021/acs.jmedchem.3c00302.
[3] Ryan Kolb, Umasankar De, Sajid Khan, Yuewan Luo, MyungChul Kim, Haijun Yu, Chaoyan Wu, Jiao Mo, Xin Zhang, Peiyi Zhang, Xuan Zhang, Nicholas Borcherding, Daniel Koppel, YangXin Fu, Song Guo Zheng, Dorina Avram, Guangrong Zheng, Daohong Zhou, Weizhou Zhang. Proteolysis-targeting chimera against BCL-XL destroys tumor-infiltrating regulatory T cells. Nature Communications[J]. 2021, 12: 1281-, http://oa.las.ac.cn/oainone/service/browseall/read1?ptype=JA&workid=JA202106295396309ZK.
[4] Matthew Burke, Pratik Pal, Peiyi Zhang, Xuan Zhang, Guangrong Zheng. Concise Synthesis of ( S )-δ-CEHC,a Metabolite of Vitamin E. ACS OMEGA[J]. 2021, 6(6): 4355-4361, https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7893788/.
[5] He, Yonghan, Li, Wen, Lv, Dongwen, Zhang, Xin, Zhang, Xuan, Ortiz, Yuma T, Budamagunta, Vivekananda, Campisi, Judith, Zheng, Guangrong, Zhou, Daohong. Inhibition of USP7 activity selectively eliminates senescent cells in part via restoration of p53 activity. AGING CELL[J]. 2020, 19(3): http://dx.doi.org/10.1111/acel.13117.
[6] Xiao, Yufeng, Zhang, Xuan. Recent advances in small molecular modulators targeting histone deacetylase 6. Future Drug Discov.[J]. 2020, 2(4): [7] Liu, Xingui, Zhang, Xuan, Lv, Dongwen, Yuan, Yaxia, Zheng, Guangrong, Zhou, Daohong. Assays and technologies for developing proteolysis targeting chimera degraders. FUTURE MEDICINAL CHEMISTRYnull. 2020, 12(12): 1155-1179, https://www.webofscience.com/wos/woscc/full-record/WOS:000613274900006.
[8] Yonghan He, Xuan Zhang, Jianhui Chang, HaNeui Kim, Peiyi Zhang, Yingying Wang, Sajid Khan, Xingui Liu, Xin Zhang, Dongwen Lv, Lin Song, Wen Li, Dinesh Thummuri, Yaxia Yuan, Janet S Wiegand, Yuma T Ortiz, Vivekananda Budamagunta, Jennifer H Elisseeff, Judith Campisi, Maria Almeida, Guangrong Zheng, Daohong Zhou. Using proteolysis-targeting chimera technology to reduce navitoclax platelet toxicity and improve its senolytic activity. NATURE COMMUNICATIONS[J]. 2020, 11(1): http://dx.doi.org/10.1038/s41467-020-15838-0.
[9] Xingui Liu, Zhengya Gao, Qiang Fu, Lin Song, Peiyi Zhang, Xuan Zhang, Howard Hendrickson, Peter A Crooks, Daohong Zhou, Guangrong Zheng. Deuteration of the farnesyl terminal methyl groups of δ-tocotrienol and its effects on the metabolic stability and ability of inducing G-CSF production. BIOORGANIC & MEDICINAL CHEMISTRY. 2020, 28(11): http://dx.doi.org/10.1016/j.bmc.2020.115498.
[10] Peiyi Zhang, Xuan Zhang, Xingui Liu, Sajid Khan, Daohong Zhou, Guangrong Zheng. PROTACs are effective in addressing the platelet toxicity associated with BCL-XL inhibitors. EXPLORATION OF TARGETED ANTI-TUMOR THERAPY[J]. 2020, 1(4): 259-272, https://doaj.org/article/1f987b9edd34458ba9d003a436382594.
[11] Khan, Sajid, He, Yonghan, Zhang, Xuan, Yuan, Yaxia, Pu, Shaoyan, Kong, Qingpeng, Zheng, Guangrong, Zhou, Daohong. PROteolysis TArgeting Chimeras (PROTACs) as emerging anticancer therapeutics. ONCOGENE[J]. 2020, 39(26): 4909-4924, https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7319888/.
[12] Liu, Xingui, Poddar, Saikat, Song, Lin, Hendrickson, Howard, Zhang, Xuan, Yuan, Yaxia, Zhou, Daohong, Zheng, Guangrong. Synthesis and Liver Microsomal Metabolic Stability Studies of a Fluorine-Substituted delta-Tocotrienol Derivative. CHEMMEDCHEM[J]. 2020, 15(6): 506-516, https://www.webofscience.com/wos/woscc/full-record/WOS:000512437700001.
[13] He, Yonghan, Koch, Raphael, Budamagunta, Vivekananda, Zhang, Peiyi, Zhang, Xuan, Khan, Sajid, Thummuri, Dinesh, Ortiz, Yuma T, Zhang, Xin, Lv, Dongwen, Wiegand, Janet S, Li, Wen, Palmer, Adam C, Zheng, Guangrong, Weinstock, David M, Zhou, Daohong. DT2216-a Bcl-xL-specific degrader is highly active against Bcl-xL-dependent T cell lymphomas. JOURNAL OF HEMATOLOGY & ONCOLOGY[J]. 2020, 13(1): http://dx.doi.org/10.1186/s13045-020-00928-9.
[14] He, Yonghan, Khan, Sajid, Huo, Zhiguang, Lv, Dongwen, Zhang, Xuan, Liu, Xingui, Yuan, Yaxia, Hromas, Robert, Xu, Mingjiang, Zheng, Guangrong, Zhou, Daohong. Proteolysis targeting chimeras (PROTACs) are emerging therapeutics for hematologic malignancies. JOURNAL OF HEMATOLOGY & ONCOLOGYnull. 2020, 13(1): https://doaj.org/article/d50c64223d3741a28884e3b3aee78b69.
[15] Xiao, Yufeng, Wang, Jia, Zhao, Lisa Y, Chen, Xinyi, Zheng, Guangrong, Zhang, Xuan, Liao, Daiqing. Discovery of histone deacetylase 3 (HDAC3)-specific PROTACs. CHEMICAL COMMUNICATIONS[J]. 2020, 56(68): 9866-9869, http://dx.doi.org/10.1039/d0cc03243c.
[16] Zhang, Xuan, Thummuri, Dinesh, Liu, Xingui, Hu, Wanyi, Zhang, Peiyi, Khan, Sajid, Yuan, Yaxia, Zhou, Daohong, Zheng, Guangrong. Discovery of PROTAC BCL-X-L degraders as potent anticancer agents with low on-target platelet toxicity. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY[J]. 2020, 192: 112186-112186, https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7433031/.
[17] Zhang, Xuan, He, Yonghan, Zhang, Peiyi, Budamagunta, Vivekananda, Lv, Dongwen, Thummuri, Dinesh, Yang, Yang, Pei, Jing, Yuan, Yaxia, Zhou, Daohong, Zheng, Guangrong. Discovery of IAP-recruiting BCL-X-L PROTACs as potent degraders across multiple cancer cell lines. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY[J]. 2020, 199: http://dx.doi.org/10.1016/j.ejmech.2020.112397.
[18] Zhang, Xuan, Liu, Xingui, Zhou, Daohong, Zheng, Guangrong. Targeting anti-apoptotic BCL-2 family proteins for cancer treatment. FUTURE MEDICINAL CHEMISTRYnull. 2020, 12(7): 563-565, https://www.webofscience.com/wos/woscc/full-record/WOS:000522963600001.
[19] Xuan Zhang, Dinesh Thummuri, Yonghan He, Xingui Liu, Peiyi Zhang, Daohong Zhou, Guangrong Zheng. Utilizing PROTAC technology to address the on-target platelet toxicity associated with inhibition of BCL-XL. Chem. Commun. Chem. Commun.[J]. 2019, 55: 14765-14768, [20] Khan, Sajid, Zhang, Xuan, Lv, Dongwen, Zhang, Qi, He, Yonghan, Zhang, Peiyi, Liu, Xingui, Thummuri, Dinesh, Yuan, Yaxia, Wiegand, Janet S, Pei, Jing, Zhang, Weizhou, Sharma, Abhisheak, McCurdy, Christopher R, Kuruvilla, Vinitha M, Baran, Natalia, Ferrando, Adolfo A, Kim, Yongmi, Rogojina, Anna, Houghton, Peter J, Huang, Guangcun, Hromas, Robert, Konopleva, Marina, Zheng, Guangrong, Zhou, Daohong. A selective BCL-X-L PROTAC degrader achieves safe and potent antitumor activity. NATURE MEDICINE[J]. 2019, 25(12): 1938-+, https://www.webofscience.com/wos/woscc/full-record/WOS:000500824900037.
[21] Zhang, Xuan, Zhang, Lun, Liu, Yaqian, Bao, Bin, Zang, Yi, Li, Jia, Lu, Wei. A near-infrared fluorescent probe for rapid detection of hydrogen peroxide in living cells. TETRAHEDRON[J]. 2015, 71(29): 4842-4845, http://dx.doi.org/10.1016/j.tet.2015.05.025.
[22] Zhang, Xuan, Kong, Yannan, Zhang, Jie, Su, Mingbo, Zhou, Yubo, Zang, Yi, Li, Jia, Chen, Yi, Fang, Yanfen, Zhang, Xiongwen, Lu, Wei. Design, synthesis and biological evaluation of colchicine derivatives as novel tubulin and histone deacetylase dual inhibitors. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY[J]. 2015, 95: 127-135, http://dx.doi.org/10.1016/j.ejmech.2015.03.035.
[23] Tang, Kaiyong, Huang, Jinwen, Pan, Junfang, Zhang, Xuan, Lu, Wei. Design, synthesis and biological evaluation of C(6)-indole celastrol derivatives as potential antitumor agents. RSC ADVANCES[J]. 2015, 5(25): 19620-19623, https://www.webofscience.com/wos/woscc/full-record/WOS:000350043600082.
[24] Bao, Bin, Liu, Meng, Liu, Yaqian, Zhang, Xuan, Zang, Yi, Li, Jia, Lu, Wei. NIR absorbing DICPO derivatives applied to wide range of pH and detection of glutathione in tumor. TETRAHEDRON[J]. 2015, 71(41): 7865-7868, http://dx.doi.org/10.1016/j.tet.2015.08.020.
[25] Zhang, Xuan, Wang, Zhilong, Huang, Qingqing, Luo, Yu, Xie, Xin, Lu, Wei. Design, synthesis, and biological evaluation of a new class of MT2-selective agonists. RSC ADVANCES[J]. 2014, 4(49): 25871-25874, https://www.webofscience.com/wos/woscc/full-record/WOS:000338434500050.
[26] Zhang, Xuan, Zhang, Jie, Su, Mingbo, Zhou, Yubo, Chen, Yi, Li, Jia, Lu, Wei. Design, synthesis and biological evaluation of 4 '-demethyl-4-deoxypodophyllotoxin derivatives as novel tubulin and histone deacetylase dual inhibitors. RSC ADVANCES[J]. 2014, 4(76): 40444-40448, https://www.webofscience.com/wos/woscc/full-record/WOS:000341936400046.
[27] Zhang, Xuan, Su, Mingbo, Chen, Yi, Li, Jia, Lu, Wei. The Design and Synthesis of a New Class of RTK/HDAC Dual-Targeted Inhibitors. MOLECULES[J]. 2013, 18(6): 6491-6503, https://doaj.org/article/1931d88e67a04fde989bca8c31affee4.
[28] Zhang, Xuan, Bao, Bin, Yu, Xiuhua, Tong, Linjiang, Luo, Yu, Huang, Qingqing, Su, Mingbo, Sheng, Li, Li, Jia, Zhu, Hong, Yang, Bo, Zhang, Xiongwen, Chen, Yi, Lu, Wei. The discovery and optimization of novel dual inhibitors of topoisomerase ii and histone deacetylase. BIOORGANIC & MEDICINAL CHEMISTRY[J]. 2013, 21(22): 6981-6995, http://dx.doi.org/10.1016/j.bmc.2013.09.023.
[29] Jiang, Ruwei, Du, Xiaoguang, Zhang, Xuan, Wang, Xin, Hu, Dingyu, Meng, Tao, Chen, Yuelei, Geng, Meiyu, Shen, Jingkang. Synthesis and bioassay of beta-(1,4)-D-mannans as potential agents against Alzheimer's disease. ACTA PHARMACOLOGICA SINICA[J]. 2013, 34(12): 1585-1591, https://www.webofscience.com/wos/woscc/full-record/WOS:000328268600013.
[30] Zhang, Xuan, Zhang, Jie, Tong, Linjiang, Luo, Yu, Su, Mingbo, Zang, Yi, Li, Jia, Lu, Wei, Chen, Yi. The discovery of colchicine-SAHA hybrids as a new class of antitumor agents. BIOORGANIC & MEDICINAL CHEMISTRY[J]. 2013, 21(11): 3240-3244, http://dx.doi.org/10.1016/j.bmc.2013.03.049.
[31] Zhang, Xuan, Yuan, Wei, Luo, Yu, Huang, QingQing, Lu, Wei. STEREOSELECTIVE SYNTHESIS OF MELATONIN RECEPTOR AGONIST RAMELTEON VIA ASYMMETRIC MICHAEL ADDITION. HETEROCYCLES[J]. 2012, 85(1): 73-84, https://www.webofscience.com/wos/woscc/full-record/WOS:000302848800006.

   

（1）Discovery of BCL-XL degraders as potent and platelet-sparing anticancer agents   2019-08-26
（2）Induced Degradation of Bcl-xL: A PROTAC Approach to Target the Achilles’ Heel of Senescent Cells   2017-09-26