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个人简介

教育背景 1997.09-2002.07 中科院上海有机化学研究所,有机化学博士; 1993.09-1997.07 华中理工大学化学系,学士. 工作经历 2008.05-至今 中国科学院上海药物研究所,课题组长、中心主任; 2020.01-至今 国科大杭州高等研究院,课题组长、研究员; 2002.12-2008.04 芝加哥大学化学系,博士后

研究领域

基于化学生物学的新药发现研究。 作为不同于遗传学技术研究蛋白质功能的选择性小分子工具,化学探针(chemical probe)是药物发现化学生物学研究的核心内容。针对重要的“可药靶”(undruggable,尚无药物可及)蛋白质,发展并正确利用化学探针,可以从生化、细胞、动物等多层面描述小分子调节这些蛋白质功能的表型和作用机制,促进“可药靶”蛋白质的靶标成药性的发现与确证研究。 具体研究内容例如: 1、RNA甲基化修饰关键酶的化学探针研究 2、泛素化修饰信号通路中蛋白质相互作用的小分子调节及其抗肿瘤研究 3、新类型抗生素以及运用“非抗生素效应”控制致病菌感染的研究

近期论文

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LinLin Zhou, CaiGuang Yang. Structural insights into the evolutionary simplification of human ClpP activators. STRUCTURE[J]. 2023, 第 2 作者 通讯作者 31(2): 125-127, http://dx.doi.org/10.1016/j.str.2023.01.002. Pan Xiao, Zongliang Duan, Zeyu Liu, Liang Chen, Deyan Zhang, Lu Liu, Chen Zhou, Jianhua Gan, Ze Dong, Cai-Guang Yang. Rational Design of RNA Demethylase FTO Inhibitors with Enhanced Antileukemia Drug-Like Properties. JOURNAL OF MEDICINAL CHEMISTRY[J]. 2023, 第 10 作者 通讯作者 Zhu, Heping, Song, Xiaomin, Pan, Yihui, Li, Ming, Chen, Liang, Xiao, Pan, Du, Rong, Dong, Ze, Yang, CaiGuang. Design, synthesis, and biological evaluation of novel spirocyclic compounds as potential anti-glioblastoma agents. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY[J]. 2023, 第 9 作者 通讯作者 258: http://dx.doi.org/10.1016/j.ejmech.2023.115595. 郇歆宇, 赖淦强, 黄悦, 杨财广. 化学干预N^(6)-甲基腺嘌呤修饰的研究进展. 高等学校化学学报[J]. 2023, 第 4 作者 通讯作者 44(3): 22-35, http://lib.cqvip.com/Qikan/Article/Detail?id=7109134608. Zhang, Ranran, Wang, Pengyu, Wei, Bingyan, Chen, Liang, Song, Xiaomin, Pan, Yihui, Li, Jiahui, Gan, Jianhua, Zhang, Tao, Yang, CaiGuang. Assessment of the structure-activity relationship and antileukemic activity of diacylpyramide compounds as human ClpP agonists. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY[J]. 2023, 第 10 作者 通讯作者 258: http://dx.doi.org/10.1016/j.ejmech.2023.115577. Bingyan Wei, Tao Zhang, Pengyu Wang, Yihui Pan, Jiahui Li, Weizhong Chen, Min Zhang, Quanjiang Ji, Wenjuan Wu, Lefu Lan, Jianhua Gan, CaiGuang Yang. Anti-infective therapy using species-specific activators of Staphylococcus aureus ClpP. NATURE COMMUNICATIONS[J]. 2022, 第 12 作者 通讯作者 13(1): 1-16, https://doaj.org/article/3ad823d96ae14bc0b6151b4bf9628fa0. 余梁, 曹荞, 陈未中, 杨娜娜, 杨财广, 季泉江, 吴敏, Taeok, Bae, 蓝乐夫. 一个新的感应铜离子的双组分信号转导系统. 科学通报:英文版[J]. 2022, 第 5 作者67(2): 198-212, http://lib.cqvip.com/Qikan/Article/Detail?id=7106564950. Liu, Zeyu, Duan, Zongliang, Zhang, Deyan, Xiao, Pan, Zhang, Tao, Xu, Hongjiao, Wang, ChuanHui, Rao, GuoWu, Gan, Jianhua, Huang, Yue, Yang, CaiGuang, Dong, Ze. Structure-Activity Relationships and Antileukemia Effects of the Tricyclic Benzoic Acid FTO Inhibitors. JOURNAL OF MEDICINAL CHEMISTRY[J]. 2022, 第 11 作者 通讯作者 邢曦雯, 杨财广, 杨俊林, 张艳. 化学生物学2017~2021年回顾及未来发展规划. 中国科学:化学[J]. 2022, 第 2 作者52(4): 580-592, http://lib.cqvip.com/Qikan/Article/Detail?id=7107186119. Wang, Pengyu, Zhang, Tao, Wang, Xinjing, Xiao, Hongying, Li, Huiti, Shou, LinLin, Yang, Teng, Wei, Bingyan, Zhu, Zeyun, Zhou, Lu, Yang, Song, Lu, Xiongxiong, Zhang, Yonghui, Huang, Yue, Gan, Jianhua, Yang, CaiGuang. Aberrant human ClpP activation disturbs mitochondrial proteome homeostasis to suppress pancreatic ductal adenocarcinoma. CELL CHEMICAL BIOLOGY[J]. 2022, 第 16 作者 通讯作者 29(9): 1396-+, http://dx.doi.org/10.1016/j.chembiol.2022.07.002. Yu, ChenXi, Wei, BingYan, Kong, XueQing, Yang, CaiGuang, Nan, FaJun. Synthesis and Structure-Activity Relationships of Ring-Opened Bengamide Analogues against Methicillin-Resistant Staphylococcus aureus(dagger). CHINESE JOURNAL OF CHEMISTRY[J]. 2021, 第 4 作者 通讯作者 39(3): 671-676, http://dx.doi.org/10.1002/cjoc.202000502. Bernasocchi, Tiziano, El Tekle, Geniver, Bolis, Marco, Mutti, Azzurra, Vallerga, Arianna, Brandt, Laura P, Spriano, Filippo, Svinkina, Tanya, Zoma, Marita, Ceserani, Valentina, Rinaldi, Anna, Janouskova, Hana, Bossi, Daniela, Cavalli, Manuela, Mosole, Simone, Geiger, Roger, Dong, Ze, Yang, CaiGuang, Albino, Domenico, Rinaldi, Andrea, Schraml, Peter, Linder, Simon, Carbone, Giuseppina M, Alimonti, Andrea, Bertoni, Francesco, Moch, Holger, Carr, Steven A, Zwart, Wilbert, Kruithofde Julio, Marianna, Rubin, Mark A, Udeshi, Namrata D, Theurillat, JeanPhilippe P. Dual functions of SPOP and ERG dictate androgen therapy responses in prostate cancer. NATURE COMMUNICATIONS[J]. 2021, 第 18 作者12(1): https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7854732/. Yang, Teng, Zhang, Tao, Zhou, Xiang, Wang, Pengyu, Gan, Jianhua, Song, Baoan, Yang, Song, Yang, CaiGuang. Dysregulation of ClpP by Small-Molecule Activators Used Against Xanthomonas oryzae pv. oryzae Infections. JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY[J]. 2021, 第 8 作者 通讯作者 69(27): 7545-7553, http://dx.doi.org/10.1021/acs.jafc.1c01470. Wang, Yaya, Cao, Qiao, Cao, Qin, Gan, Jianhua, Sun, Ning, Yang, CaiGuang, Bae, Taeok, Wu, Min, Lan, Lefu. Histamine activates HinK to promote the virulence of Pseudomonas aeruginosa. SCIENCE BULLETIN[J]. 2021, 第 6 作者66(11): 1101-1118, http://dx.doi.org/10.1016/j.scib.2021.01.002. Liu, Yi, Liang, Guanghao, Xu, Hongjiao, Dong, Wenxin, Dong, Ze, Qiu, Zhiwei, Zhang, Zihao, Li, Fangle, Huang, Yue, Li, Yilin, Wu, Jun, Yin, Shenyi, Zhang, Yawei, Guo, Peijin, Liu, Jun, Xi, Jianzhong Jeff, Jiang, Peng, Han, Dali, Yang, CaiGuang, Xu, Meng Michelle. Tumors exploit FTO-mediated regulation of glycolytic metabolism to evade immune surveillance. CELL METABOLISM[J]. 2021, 第 19 作者 通讯作者 33(6): 1221-+, http://dx.doi.org/10.1016/j.cmet.2021.04.001. Wang, Zhen, Zhang, Hao, Chen, Baoen, Ouyang, Sisheng, Zheng, Tong, Zhou, Ran, Dong, Ze, Huang, Yue, Zhang, Tao, Jiang, Hualiang, Gan, Jianhua, Luo, Cheng, Yang, CaiGuang. A Peptide Binder of E3 Ligase Adaptor SPOP Disrupts Oncogenic SPOP-Protein Interactions in Kidney Cancer Cells. CHINESE JOURNAL OF CHEMISTRY[J]. 2021, 第 13 作者 通讯作者 39(2): 274-280, http://dx.doi.org/10.1002/cjoc.202000462. Wang, Zhen, Zhang, Hao, Chen, Baoen, Ouyang, Sisheng, Zheng, Tong, Zhou, Ran, Dong, Ze, Huang, Yue, Zhang, Tao, Jiang, Hualiang, Gan, Jianhua, Luo, Cheng, Yang, CaiGuang. A Peptide Binder of E3 Ligase Adaptor SPOP Disrupts Oncogenic SPOP-Protein Interactions in Kidney Cancer Cells. CHINESE JOURNAL OF CHEMISTRY[J]. 2020, 第 13 作者 通讯作者 274-280, Dong, Ze, Wang, Zhen, Guo, ZhongQiang, Gong, Shouzhe, Zhang, Tao, Liu, Jiang, Luo, Cheng, Jiang, Hualiang, Yang, CaiGuang. Structure-Activity Relationship of SPOP Inhibitors against Kidney Cancer. JOURNAL OF MEDICINAL CHEMISTRY[J]. 2020, 第 9 作者 通讯作者 63(9): 4849-4866, https://www.webofscience.com/wos/woscc/full-record/WOS:000535279800029. Kong, XueQing, Wei, BingYan, Yu, ChenXi, Guan, XiangNa, Ma, WeiPing, Liu, Gang, Yang, CaiGuang, Nan, FaJun. Design, Synthesis and Biological Evaluation of Bengamide Analogues as ClpP Activators. CHINESE JOURNAL OF CHEMISTRY[J]. 2020, 第 7 作者38(10): 1111-1115, http://lib.cqvip.com/Qikan/Article/Detail?id=7103440057. Yang, Teng, Zhang, Tao, Guan, XiangNa, Dong, Ze, Lan, Lefu, Yang, Song, Yang, CaiGuang. Tideglusib and Its Analogues As Inhibitors of Staphylococcus aureus SrtA. JOURNALOFMEDICINALCHEMISTRY[J]. 2020, 第 7 作者 通讯作者 63(15): 8442-8457, https://www.webofscience.com/wos/woscc/full-record/WOS:000562941200034. Lai, GanQiang, Zhou, LinLin, Yang, CaiGuang. RNA Methylation m(6)A: A New Code and Drug Target?. CHINESE JOURNAL OF CHEMISTRY[J]. 2020, 第 3 作者 通讯作者 38(4): 420-421, http://lib.cqvip.com/Qikan/Article/Detail?id=7101969872. Song, Runzhe, Wang, Yue, Wang, Minghui, Gao, Ruixuan, Yang, Teng, Yang, Song, Yang, CaiGuang, Jin, Yongsheng, Zou, Siyuan, Cai, Jianfeng, Fan, Renhua, He, Qiuqin. Design and synthesis of novel desfluoroquinolone-aminopyrimidine hybrids as potent anti-MRSA agents with low hERG activity. BIOORGANIC CHEMISTRY[J]. 2020, 第 7 作者103: http://dx.doi.org/10.1016/j.bioorg.2020.104176. Zhou, LinLin, Yang, CaiGuang. Targeting Epitranscriptomic Proteins for Therapeutic Intervention. BIOCHEMISTRY. 2020, 第 2 作者 通讯作者 59(2): 125-127, https://www.webofscience.com/wos/woscc/full-record/WOS:000509420600001. Gu, Lei, Liu, Xing, Wang, YuQiu, Zhou, Yanting, Zhu, Hongwen, Huang, Jin, Lan, Lefu, Zheng, Jing, Yang, Caiguang, Zhou, Hu. Revelation of AbfR in regulation of mismatch repair and energy metabolism in S. epidermidis by integrated proteomic and metabolomic analysis. JOURNAL OF PROTEOMICS[J]. 2020, 第 9 作者 通讯作者 226: http://dx.doi.org/10.1016/j.jprot.2020.103900. Wang, ZhiCheng, Wei, Bingyan, Pei, FangNing, Yang, Teng, Tang, Jie, Yang, Song, Yu, LiFang, Yang, CaiGuang, Yang, Fan. Capsaicin derivatives with nitrothiophene substituents: Design, synthesis and antibacterial activity against multidrug-resistant S. aureus. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY[J]. 2020, 第 8 作者 通讯作者 198: http://dx.doi.org/10.1016/j.ejmech.2020.112352. Yang, Nana, Cao, Qiao, Hu, Shuyang, Xu, Chenchen, Fan, Ke, Chen, Feifei, Yang, CaiGuang, Liang, Haihua, Wu, Min, Bae, Taeok, Lan, Lefu. Alteration of protein homeostasis mediates the interaction of Pseudomonas aeruginosa with Staphylococcus aureus. MOLECULAR MICROBIOLOGY[J]. 2020, 第 7 作者114(3): 423-442, http://dx.doi.org/10.1111/mmi.14519. Cao, Qiao, Yang, Nana, Wang, Yanhui, Xu, Chenchen, Zhang, Xue, Fan, Ke, Chen, Feifei, Liang, Haihua, Zhang, Yingchao, Deng, Xin, Feng, Youjun, Yang, CaiGuang, Wu, Min, Bae, Taeok, Lan, Lefu. Mutation-induced remodeling of the BfmRS two-component system in Pseudomonas aeruginosa clinical isolates. SCIENCE SIGNALING[J]. 2020, 第 12 作者13(656): http://dx.doi.org/10.1126/scisignal.aaz1529. Su, Liqiang, Li, Jiahui, Zhou, Zhen, Huang, Dongxia, Zhang, Yuanjin, Pei, Haixiang, Guo, Weikai, Wu, Haigang, Wang, Xin, Liu, Mingyao, Yang, CaiGuang, Chen, Yihua. Design, synthesis and evaluation of hybrid of tetrahydrocarbazole with 2,4-diaminopyrimidine scaffold as antibacterial agents. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY[J]. 2019, 第 11 作者 通讯作者 162: 203-211, http://dx.doi.org/10.1016/j.ejmech.2018.11.016. Zhang, Zhang, Chen, LiQian, Zhao, YuLi, Yang, CaiGuang, Roundtree, Ian A, Zhang, Zijie, Ren, Jian, Xie, Wei, He, Chuan, Luo, GuanZheng. Single-base mapping of m(6)A by an antibody-independent method. SCIENCE ADVANCES[J]. 2019, 第 4 作者5(7): https://www.webofscience.com/wos/woscc/full-record/WOS:000478770400107. Zhou, LinLin, Yang, CaiGuang. Chemical Intervention on Staphylococcus aureus Virulence. CHINESE JOURNAL OF CHEMISTRY[J]. 2019, 第 2 作者 通讯作者 37(2): 183-193, http://lib.cqvip.com/Qikan/Article/Detail?id=7001637155. Huang, Yue, Su, Rui, Sheng, Yue, Dong, Lei, Dong, Ze, Xu, Hongjiao, Ni, Tengfeng, Zhang, Zijie Scott, Zhang, Tao, Li, Chenying, Han, Li, Zhu, Zhenyun, Lian, Fulin, Wei, Jiangbo, Deng, Qiangqiang, Wang, Yungui, Wunderlich, Mark, Gao, Zhiwei, Pan, Guoyu, Zhong, Dafang, Zhou, Hu, Zhang, Naixia, Gan, Jianhua, Jiang, Hualiang, Mulloy, James C, Qian, Zhijian, Chen, Jianjun, Yang, CaiGuang. Small-Molecule Targeting of Oncogenic FTO Demethylase in Acute Myeloid Leukemia. CANCER CELL[J]. 2019, 第 28 作者 通讯作者 35(4): 677-+, http://dx.doi.org/10.1016/j.ccell.2019.03.006. Su, Liqiang, Li, Jiahui, Zhou, Zhen, Huang, Dongxia, Zhang, Yuanjin, Pei, Haixiang, Guo, Weikai, Wu, Haigang, Wang, Xin, Liu, Mingyao, Yang, CaiGuang, Chen, Yihua. Design, synthesis and evaluation of hybrid of tetrahydrocarbazole with 2,4-diaminopyrimidine scaffold as antibacterial agents (vol 162, pg 203, 2019). EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. 2019, 第 11 作者 通讯作者 168: 385-385, https://www.webofscience.com/wos/woscc/full-record/WOS:000463120300029. Liqiang Su, Jiahui Li, Zhen Zhou, Dongxia Huang, Yuanjin Zhang, Haixiang Pei, Weikai Guo, Haigang Wu, Xin Wang, Mingyao Liu, CaiGuang Yang, Yihua Chen. Corrigendum to "Design, synthesis and evaluation of hybrid of tetrahydrocarbazole with 2,4-diaminopyrimidine scaffold as antibacterial agents" Eur. J. Med. Chem. 162 (162) (2019) 203–211. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. 2019, 第 11 作者168: 385-385, http://dx.doi.org/10.1016/j.ejmech.2019.02.059. Chen, Biao, Long, Qingsu, Zhao, Yongliang, Wu, Yuanyuan, Ge, Shasha, Wang, Peiyi, Yang, CaiGuang, Chi, Yonggui, Song, Baoan, Yang, Song. Sulfone-Based Probes Unraveled Dihydrolipoamide S-Succinyltransferase as an Unprecedented Target in Phytopathogens. JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY[J]. 2019, 第 7 作者67(25): 6962-6969, Yang, Teng, Liu, Tingting, Gan, Jianhua, Yu, Kunqian, Chen, Kaixian, Xue, Wei, Lan, Lefu, Yang, Song, Yang, CaiGuang. Structural Insight into the Mechanism of Staphylococcus aureus Stp1 Phosphatase. ACS INFECTIOUS DISEASES[J]. 2019, 第 9 作者 通讯作者 5(6): 841-850,

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