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

   

100706-药理学
070321-化学生物学

化学生物学；分子生物学；细胞生物学

1997-09--2002-06   中科院上海有机化学研究所   博士
1993-09--1997-06   华中理工大学   学士

基于化学生物学的新药发现

   

（1） 中科院特聘研究员计划, 其他, 2016
（2） 科技部中青年科技创新领军人才计划, 其他, 2015
（3） 药明康德生命化学研究（学者）奖, 其他, 2014
（4） 上海市浦江人才计划, 市地级, 2009
（5） 中国科学院****, 院级, 2008
（6） 中科院院长优秀奖, , 院级, 2002

（ 1 ） 取代的喹啉-2-甲醛-苯腙类化合物及制备方法和用途, 发明, 2011, 第 3 作者, 专利号: 201110091665.4
（ 2 ） 2-( 取代苯氨基 ) 苯甲酸及其酯类化合物制备 FTO 抑制剂的用途, 发明, 2014, 第 1 作者, 专利号: 201410334466.5
（ 3 ） 大黄酸或大黄酸类化合物在制备治疗以FTO为靶点的疾病药物中的用途, 发明, 2012, 第 1 作者, 专利号: 201210197108.5
（ 4 ） 3,6-二取代[1,2,4]三咗[3,4-b][1,3,4]噻二唑化合物及其用途, 发明, 2014, 第 1 作者, 专利号: 201410081218.4
（ 5 ） 香兰胺/香兰醇衍生物及其制备方法和应用, 发明, 2015, 第 3 作者, 专利号: 201510120796.9
（ 6 ） 类三环二萜并吡唑衍生物及其制备方法和应用, 发明, 2014, 第 2 作者, 专利号: 201410153124.3
（ 7 ） 含金刚烷基的萘醌类衍生物、其制备方法及应用, 发明, 2015, 第 2 作者, 专利号: 201510199108.2
（ 8 ） 12-肟醚脱氢枞酸衍生物的用途, 发明, 2016, 第 4 作者, 专利号: 201610325861.6
（ 9 ） B环改造脱氢枞酸衍生物的用途, 发明, 2016, 第 4 作者, 专利号: 201610327314.1
（ 10 ） 2-亚胺-5-酮基-2,5-二氢-1-H-二吡啶并[3,4-c:1',2'-f]嘧啶类化合物合成及其用途, 发明, 2016, 第 1 作者, 专利号: 201610116185.1

   

[1] LinLin Zhou, CaiGuang Yang. Structural insights into the evolutionary simplification of human ClpP activators. STRUCTURE[J]. 2023, 31(2): 125-127, http://dx.doi.org/10.1016/j.str.2023.01.002.
[2] 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, [3] Heping Zhu, Xiaomin Song, Yihui Pan, Ming Li, Liang Chen, Pan Xiao, Rong Du, Ze Dong, CaiGuang Yang. Design, synthesis, and biological evaluation of novel spirocyclic compounds as potential anti-glioblastoma agents. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY[J]. 2023, 258: http://dx.doi.org/10.1016/j.ejmech.2023.115595.
[4] 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, 44(3): 22-35, http://lib.cqvip.com/Qikan/Article/Detail?id=7109134608.
[5] Ranran Zhang, Pengyu Wang, Bingyan Wei, Liang Chen, Xiaomin Song, Yihui Pan, Jiahui Li, Jianhua Gan, Tao Zhang, CaiGuang Yang. Assessment of the structure-activity relationship and antileukemic activity of diacylpyramide compounds as human ClpP agonists. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY[J]. 2023, 258: http://dx.doi.org/10.1016/j.ejmech.2023.115577.
[6] 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, 13(1): 1-16, https://doaj.org/article/3ad823d96ae14bc0b6151b4bf9628fa0.
[7] 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, 67(2): 198-212, http://lib.cqvip.com/Qikan/Article/Detail?id=7106564950.
[8] 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, [9] 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, 52(4): 580-592, http://lib.cqvip.com/Qikan/Article/Detail?id=7107186119.
[10] 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, 29(9): 1396-+, http://dx.doi.org/10.1016/j.chembiol.2022.07.002.
[11] 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, 39(3): 671-676, http://dx.doi.org/10.1002/cjoc.202000502.
[12] 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, 12(1): https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7854732/.
[13] 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, 69(27): 7545-7553, http://dx.doi.org/10.1021/acs.jafc.1c01470.
[14] 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, 66(11): 1101-1118, http://dx.doi.org/10.1016/j.scib.2021.01.002.
[15] 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, 33(6): 1221-+, http://dx.doi.org/10.1016/j.cmet.2021.04.001.
[16] 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, 39(2): 274-280, http://dx.doi.org/10.1002/cjoc.202000462.
[17] 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, 274-280, [18] 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, 63(9): 4849-4866, https://www.webofscience.com/wos/woscc/full-record/WOS:000535279800029.
[19] 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, 38(10): 1111-1115, http://lib.cqvip.com/Qikan/Article/Detail?id=7103440057.
[20] 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, 63(15): 8442-8457, https://www.webofscience.com/wos/woscc/full-record/WOS:000562941200034.
[21] Lai, GanQiang, Zhou, LinLin, Yang, CaiGuang. RNA Methylation m(6)A: A New Code and Drug Target?. CHINESE JOURNAL OF CHEMISTRY[J]. 2020, 38(4): 420-421, http://lib.cqvip.com/Qikan/Article/Detail?id=7101969872.
[22] 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, 103: http://dx.doi.org/10.1016/j.bioorg.2020.104176.
[23] Zhou, LinLin, Yang, CaiGuang. Targeting Epitranscriptomic Proteins for Therapeutic Intervention. BIOCHEMISTRY. 2020, 59(2): 125-127, https://www.webofscience.com/wos/woscc/full-record/WOS:000509420600001.
[24] 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, 226: http://dx.doi.org/10.1016/j.jprot.2020.103900.
[25] 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, 198: http://dx.doi.org/10.1016/j.ejmech.2020.112352.
[26] 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, 114(3): 423-442, http://dx.doi.org/10.1111/mmi.14519.
[27] 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, 13(656): http://dx.doi.org/10.1126/scisignal.aaz1529.
[28] 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, 35(4): 677-+, http://dx.doi.org/10.1016/j.ccell.2019.03.006.
[29] 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, 168: 385-385, https://www.webofscience.com/wos/woscc/full-record/WOS:000463120300029.
[30] 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, 168: 385-385, http://dx.doi.org/10.1016/j.ejmech.2019.02.059.
[31] 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, 67(25): 6962-6969, [32] 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, 162: 203-211, http://dx.doi.org/10.1016/j.ejmech.2018.11.016.
[33] 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, 5(6): 841-850, [34] 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, 5(7): https://www.webofscience.com/wos/woscc/full-record/WOS:000478770400107.
[35] Zhou, LinLin, Yang, CaiGuang. Chemical Intervention on Staphylococcus aureus Virulence. CHINESE JOURNAL OF CHEMISTRY[J]. 2019, 37(2): 183-193, http://lib.cqvip.com/Qikan/Article/Detail?id=7001637155.
[36] Hou, Xiaochen, Wang, Meining, Wen, Yi, Ni, Tengfeng, Guan, Xiangna, Lan, Lefu, Zhang, Naixia, Zhang, Ao, Yang, CaiGuang. Quinone skeleton as a new class of irreversible inhibitors against Staphylococcus aureus sortase A. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS[J]. 2018, 28(10): 1864-1869, http://dx.doi.org/10.1016/j.bmcl.2018.04.005.
[37] 王蓬宇, 杨财广. RNA甲基化修饰与病理效应. 生命科学[J]. 2018, 30(4): 431-, http://lib.cqvip.com/Qikan/Article/Detail?id=675263910.
[38] Zhang, WenMing, Yao, Yang, Yang, Teng, Wang, XueYing, Zhu, ZhenYun, Xu, WenTao, Lin, HaiXia, Gao, ZhaoBing, Zhou, Hu, Yang, CaiGuang, Cui, YongMei. The synthesis and antistaphylococcal activity of N-sulfonaminoethyloxime derivatives of dehydroabietic acid. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS[J]. 2018, 28(10): 1943-1948, http://dx.doi.org/10.1016/j.bmcl.2018.03.062.
[39] Ye, Fei, Li, Jiahui, Yang, CaiGuang. The development of small-molecule modulators for ClpP protease activity. MOLECULAR BIOSYSTEMSnull. 2017, 13(1): 23-31, https://www.webofscience.com/wos/woscc/full-record/WOS:000391697500002.
[40] Wang, Jing, Yang, Teng, Chen, Huang, Xu, YunNan, Yu, LiFang, Liu, Ting, Tang, Jie, Yi, Zhengfang, Yang, CaiGuang, Xue, Wei, Yang, Fan. The synthesis and antistaphylococcal activity of 9, 13-disubstituted berberine derivatives. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY[J]. 2017, 127: 424-433, http://dx.doi.org/10.1016/j.ejmech.2017.01.012.
[41] Zheng, Tong, Yang, CaiGuang. Targeting SPOP with small molecules provides a novel strategy for kidney cancer therapy. SCIENCE CHINA-LIFE SCIENCES[J]. 2017, 60(1): 91-93, https://www.webofscience.com/wos/woscc/full-record/WOS:000394044500014.
[42] Zhang, WenMing, Yang, Teng, Pan, XueYing, Liu, XinLan, Lin, HaiXia, Gao, ZhaoBing, Yang, CaiGuang, Cui, YongMei. The synthesis and antistaphylococcal activity of dehydroabietic acid derivatives: modifications at C12 and C7. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY[J]. 2017, 127: 917-927, http://www.corc.org.cn/handle/1471x/2194286.
[43] Liu, Guijie, Liu, Xing, Xu, Hongjiao, Liu, Xichun, Zhou, Hu, Huang, Zhen, Gan, Jianhua, Chen, Hao, Lan, Lefu, Yang, CaiGuang. Structural Insights into the Redox-Sensing Mechanism of MarR-Type Regulator AbfR. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY[J]. 2017, 139(4): 1598-1608, http://dx.doi.org/10.1021/jacs.6b11438.
[44] 郑桐, 杨财广. 小分子破坏E3接头蛋白SPOP-底物相互作用与肾癌治疗. 2016, 136-, https://kns.cnki.net/KCMS/detail/detail.aspx?dbcode=CPFD&dbname=CPFDLAST2017&filename=ZGHY201607037119&v=MjM4NTNyaWZaZVp2SGludFU3N01JMW9TUHlyRGQ3RzRIOWZNcUk5R1krb09CUk5LdWhkaG5qOThUbmpxcXhkRWVNT1VL.
[45] Chen, Weizhong, Wang, Dan, Zhou, Wenquan, Sang, Hong, Liu, Xichun, Ge, Zhiyun, Zhang, Jin, Lan, Lefu, Yang, CaiGuang, Chen, Hao. Novobiocin binding to NalD induces the expression of the MexAB-OprM pump in Pseudomonas aeruginosa. MOLECULAR MICROBIOLOGY[J]. 2016, 100(5): 749-758, http://dx.doi.org/10.1111/mmi.13346.
[46] Li, Qi, Huang, Yue, Liu, Xichun, Gan, Jianhua, Chen, Hao, Yang, CaiGuang. Rhein Inhibits AlkB Repair Enzymes and Sensitizes Cells to Methylated DNA Damage. JOURNAL OF BIOLOGICAL CHEMISTRY[J]. 2016, 291(21): 11083-11093, http://dx.doi.org/10.1074/jbc.M115.711895.
[47] Ni, Tengfeng, Ye, Fei, Liu, Xing, Zhang, Jie, Liu, Hongchuan, Li, Jiahui, Zhang, Yingyi, Sun, Yinqiang, Wang, Meining, Luo, Cheng, Jiang, Hualiang, Lan, Lefu, Gan, Jianhua, Zhang, Ao, Zhou, Hu, Yang, CaiGuang. Characterization of Gain-of-Function Mutant Provides New Insights into ClpP Structure. ACS CHEMICAL BIOLOGY[J]. 2016, 11(7): 1964-1972, http://www.corc.org.cn/handle/1471x/2374513.
[48] Liu, MingLiang, Pan, XueYing, Yang, Teng, Zhang, Wen Ming, Wang, TianQi, Wang, HeYun, Lin, HaiXia, Yang, CaiGuang, Cui, YongMei. The synthesis and antistaphylococcal activity of dehydroabietic acid derivatives: Modifications at C-12. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS[J]. 2016, 26(22): 5492-5496, http://www.corc.org.cn/handle/1471x/2230821.
[49] Chen, Feifei, Di, Hongxia, Wang, Youxin, Cao, Qiao, Xu, Bin, Zhang, Xue, Yang, Nana, Liu, Guijie, Yang, CaiGuang, Xu, Yong, Jiang, Hualiang, Lian, Fulin, Zhang, Naixia, Li, Jian, Lan, Lefu. Small-molecule targeting of a diapophytoene desaturase inhibits S. aureus virulence. NATURE CHEMICAL BIOLOGY[J]. 2016, 12(3): 174-179, https://www.webofscience.com/wos/woscc/full-record/WOS:000371377000010.
[50] 蒋华良. Small-molecule targeting of E3 ligase adaptor SPOP in kidney cancer. CANCER CELL[J]. 2016, 30(3): 474-484, http://www.corc.org.cn/handle/1471x/2376307.
[51] Yu, LiGang, Ni, TengFeng, Gao, Wei, He, Yuan, Wang, YingYing, Cui, HaiWei, Yang, CaiGuang, Qiu, WenWei. The synthesis and antibacterial activity of pyrazole-fused tricyclic diterpene derivatives. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY[J]. 2015, 90: 10-20, http://dx.doi.org/10.1016/j.ejmech.2014.11.015.
[52] Yang, Nana, Ding, Shuting, Chen, Feifei, Zhang, Xue, Xia, Yongjie, Di, Hongxia, Cao, Qiao, Deng, Xin, Wu, Min, Wong, Catherine C L, Tian, XiaoXu, Yang, CaiGuang, Zhao, Jing, Lan, Lefu. The Crc protein participates in down-regulation of the Lon gene to promote rhamnolipid production and rhl quorum sensing in Pseudomonas aeruginosa. MOLECULAR MICROBIOLOGY[J]. 2015, 96(3): 526-547, https://www.webofscience.com/wos/woscc/full-record/WOS:000353895800007.
[53] Huang, Yue, Yan, Jingli, Li, Qi, Li, Jiafei, Gong, Shouzhe, Zhou, Hu, Gan, Jianhua, Jiang, Hualiang, Jia, GuiFang, Luo, Cheng, Yang, CaiGuang. Meclofenamic acid selectively inhibits FTO demethylation of m(6)A over ALKBH5. NUCLEIC ACIDS RESEARCH[J]. 2015, 43(1): 373-384, https://www.webofscience.com/wos/woscc/full-record/WOS:000350207100037.
[54] Wang, Tianlu, Hong, Tingting, Huang, Yue, Su, Haomiao, Wu, Fan, Chen, Yi, Wei, Lai, Huang, Wei, Hua, Xiaoluan, Xia, Yu, Xu, Jinglei, Gan, Jianhua, Yuan, Bifeng, Feng, Yuqi, Zhang, Xiaolian, Yang, CaiGuang, Zhou, Xiang. Fluorescein Derivatives as Bifunctional Molecules for the Simultaneous Inhibiting and Labeling of FTO Protein. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY[J]. 2015, 137(43): 13736-13739, https://www.webofscience.com/wos/woscc/full-record/WOS:000364355900004.
[55] Chen, Xinhuan, Xu, Zhijian, Zhang, Lingna, Liu, Hongchuan, Liu, Xia, Lou, Meng, Zhu, Lijun, Huang, Bingding, Yang, CaiGuang, Zhu, Weiliang, Shao, Jimin. The Conserved Lys-95 Charged Residue Cluster Is Critical for the Homodimerization and Enzyme Activity of Human Ribonucleotide Reductase Small Subunit M2. JOURNAL OF BIOLOGICAL CHEMISTRY[J]. 2014, 289(2): 909-920, http://dx.doi.org/10.1074/jbc.M113.524546.
[56] 杨财广. A metabolic sensor governing bacterial virulence in Staphylococcus aureus. Proc. Natl. Acad. Sci.. 2014, [57] Cao, Qiao, Wang, Yue, Chen, Feifei, Xia, Yongjie, Lou, Jingyu, Zhang, Xue, Yang, Nana, Sun, Xiaoxu, Zhang, Qin, Zhuo, Chao, Huang, Xi, Deng, Xin, Yang, CaiGuang, Ye, Yan, Zhao, Jing, Wu, Min, Lan, Lefu. A Novel Signal Transduction Pathway that Modulates rhl Quorum Sensing and Bacterial Virulence in Pseudomonas aeruginosa. PLOS PATHOGENS[J]. 2014, 10(8): https://doaj.org/article/fc0b9beaa247452d9a583209922b5a30.
[58] Zhang, Jie, Liu, Hongchuan, Zhu, Kongkai, Gong, Shouzhe, Dramsi, Shaynoor, Wang, YaTing, Li, Jiafei, Chen, Feifei, Zhang, Ruihan, Zhou, Lu, Lan, Lefu, Jiang, Hualiang, Schneewind, Olaf, Luo, Cheng, Yang, CaiGuang. Antiinfective therapy with a small molecule inhibitor of Staphylococcus aureus sortase. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA[J]. 2014, 111(37): 13517-13522, http://dx.doi.org/10.1073/pnas.1408601111.
[59] Ding, Yue, Liu, Xing, Chen, Feifei, Di, Hongxia, Xu, Bin, Zhou, Lu, Deng, Xin, Wu, Min, Yang, CaiGuang, Lan, Lefu. Metabolic sensor governing bacterial virulence in Staphylococcus aureus. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA[J]. 2014, 111(46): E4981-E4990, https://www.webofscience.com/wos/woscc/full-record/WOS:000345153300013.
[60] Chen Baoen, Gan Jianhua, Yang Caiguang. The complex structures of ALKBH2 mutants cross-linked to dsDNA reveal the conformational swing of β-hairpin. SCIENCE CHINA. CHEMISTRY[J]. 2014, 57(2): 307-,  http://dx.doi.org/10.1007/s11426-013-5029-z.
[61] Chen BaoEn, Gan JianHua, Yang CaiGuang. The complex structures of ALKBH2 mutants cross-linked to dsDNA reveal the conformational swing of beta-hairpin. SCIENCE CHINA-CHEMISTRY[J]. 2014, 57(2): 307-313, https://www.webofscience.com/wos/woscc/full-record/WOS:000330681700013.
[62] 杨财广. 蛋白质/DNA相互作用的分子识别机制. 2013, 74-, https://kns.cnki.net/KCMS/detail/detail.aspx?dbcode=CPFD&dbname=CPFD0914&filename=ZGHY201309001040&v=MzE3OTZIaW50VTd6SklGNFdQeXJEZDdHNEg5TE1wbzlGWmVzTERCTkt1aGRobmo5OFRuanFxeGRFZU1PVUtyaWZaZVp2.
[63] 杨财广. ClpP水解酶的作用机制与调控. 2013, 70-, https://kns.cnki.net/KCMS/detail/detail.aspx?dbcode=IPFD&dbname=IPFDLAST2015&filename=ZGHY201310023069&v=MTEzMDZPVUtyaWZaZVp2SGludFU3L01KMXdVUHlyRGQ3RzRIOUxOcjQ5SForc0pCUk5LdWhkaG5qOThUbmpxcXhkRWVN.
[64] Liu, Xing, Sun, Xiaoxu, Wu, Youcong, Xie, Cen, Zhang, Wenru, Wang, Dan, Chen, Xiaoyan, Qu, Di, Gan, Jianhua, Chen, Hao, Jiang, Hualiang, Lan, Lefu, Yang, CaiGuang. Oxidation-sensing Regulator AbfR Regulates Oxidative Stress Responses, Bacterial Aggregation, and Biofilm Formation in Staphylococcus epidermidis. JOURNAL OF BIOLOGICAL CHEMISTRY[J]. 2013, 288(6): 3739-3752, http://dx.doi.org/10.1074/jbc.M112.426205.
[65] Ye, Fei, Zhang, Jie, Liu, Hongchuan, Hilgenfeld, Rolf, Zhang, Ruihan, Kong, Xiangqian, Li, Lianchun, Lu, Junyan, Zhang, Xinlei, Li, Donghai, Jiang, Hualiang, Yang, CaiGuang, Luo, Cheng. Helix Unfolding/Refolding Characterizes the Functional Dynamics of Staphylococcus aureus Clp Protease. JOURNALOFBIOLOGICALCHEMISTRY[J]. 2013, 288(24): 17643-17653, http://dx.doi.org/10.1074/jbc.M113.452714.
[66] 陈报恩, 叶飞, 李琦, 杨财广. 核酸去甲基化酶小分子抑制剂研究. 2013, 164-, https://kns.cnki.net/KCMS/detail/detail.aspx?dbcode=CPFD&dbname=CPFD0914&filename=ZGHY201309001128&v=MTA1MTFGWmVvTkJCTkt1aGRobmo5OFRuanFxeGRFZU1PVUtyaWZaZVp2SGludFU3ekpJMXNTUHlyRGQ3RzRIOUxNcG85.
[67] Li, Xiangyang, Song, Baoan, Chen, Xi, Wang, Zhenchao, Zeng, Mengjiao, Yu, Dandan, Hu, Deyu, Chen, Zhuo, Jin, Linhong, Yang, Song, Yang, Caiguang, Chen, Baoen. Crystal Structure of a Four-Layer Aggregate of Engineered TMV CP Implies the Importance of Terminal Residues for Oligomer Assembly. PLOS ONE[J]. 2013, 8(11): http://dx.doi.org/10.1371/journal.pone.0077717.
[68] 陈报恩, 杨财广. 人源ALKB氧化酶识别甲基化碱基的机理研究. 2012, 56-, https://kns.cnki.net/KCMS/detail/detail.aspx?dbcode=CPFD&dbname=CPFD0914&filename=ZGJY201208002052&v=MDk1MzB6TUtWd2NQeXJCZDdHNEg5UE1wNDlGWnVzS0RoTkt1aGRobmo5OFRuanFxeGRFZU1PVUtyaWZaZVp2SGludFU3.
[69] Deng, Jing, Li, Ning, Liu, Hongchuan, Zuo, Zhili, Liew, Oi Wah, Xu, Weijun, Chen, Gang, Tong, Xiankun, Tang, Wei, Zhu, Jin, Zuo, Jianping, Jiang, Hualiang, Yang, CaiGuang, Li, Jian, Zhu, Weiliang. Discovery of Novel Small Molecule Inhibitors of Dengue Viral NS2B-NS3 Protease Using Virtual Screening and Scaffold Hopping. JOURNAL OF MEDICINAL CHEMISTRY[J]. 2012, 55(14): 6278-6293, https://www.webofscience.com/wos/woscc/full-record/WOS:000306764600003.
[70] Chen, Baoen, Ye, Fei, Yu, Lu, Jia, Guifang, Huang, Xiaotian, Zhang, Xueju, Peng, Shuying, Chen, Kai, Wang, Meining, Gong, Shouze, Zhang, Ruihan, Yin, Jinya, Li, Haiyan, Yang, Yiming, Liu, Hong, Zhang, Jiwen, Zhang, Haiyan, Zhang, Ao, Jiang, Hualiang, Luo, Cheng, Yang, CaiGuang. Development of Cell-Active N-6-Methyladenosine RNA Demethylase FTO Inhibitor. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY[J]. 2012, 134(43): 17963-17971, https://www.webofscience.com/wos/woscc/full-record/WOS:000310483500025.
[71] Yi, Chengqi, Chen, Baoen, Qi, Bo, Zhang, Wen, Jia, Guifang, Zhang, Liang, Li, Charles J, Dinner, Aaron R, Yang, CaiGuang, He, Chuan. Duplex interrogation by a direct DNA repair protein in search of base damage. NATURE STRUCTURAL & MOLECULAR BIOLOGY[J]. 2012, 19(7): 671-+, https://www.webofscience.com/wos/woscc/full-record/WOS:000306107100005.
[72] Zhang, Jie, Ye, Fei, Lan, Lefu, Jiang, Hualiang, Luo, Cheng, Yang, CaiGuang. Structural Switching of Staphylococcus aureus Clp Protease A KEY TO UNDERSTANDING PROTEASE DYNAMICS. JOURNAL OF BIOLOGICAL CHEMISTRY[J]. 2011, 286(43): 37590-37601, http://dx.doi.org/10.1074/jbc.M111.277848.
[73] Song, ChunXiao, Sun, Yao, Dai, Qing, Lu, XingYu, Yu, Miao, Yang, CaiGuang, He, Chuan. Detection of 5-Hydroxymethylcytosine in DNA by Transferring a Keto-Glucose by Using T4 Phage beta-Glucosyltransferase. CHEMBIOCHEM[J]. 2011, 12(11): 1682-1685, https://www.webofscience.com/wos/woscc/full-record/WOS:000293842300007.
[74] Chen, Hao, Yi, Chengqi, Zhang, Jin, Zhang, Wenru, Ge, Zhiyun, Yang, CaiGuang, He, Chuan. Structural insight into the oxidation-sensing mechanism of the antibiotic resistance of regulator MexR. EMBO REPORTS[J]. 2010, 11(9): 685-690, http://ir.simm.ac.cn/handle/153631/1975.
[75] Chen, Baoen, Liu, Hongchuan, Sun, Xiaoxu, Yang, CaiGuang. Mechanistic insight into the recognition of single-stranded and double-stranded DNA substrates by ABH2 and ABH3. MOLECULAR BIOSYSTEMS[J]. 2010, 6(11): 2143-2149, https://www.webofscience.com/wos/woscc/full-record/WOS:000282765000007.
[76] Yi, Chengqi, Jia, Guifang, Hou, Guanhua, Dai, Qing, Zhang, Wen, Zheng, Guanqun, Jian, Xing, Yang, CaiGuang, Cui, Qiang, He, Chuan. Iron-catalysed oxidation intermediates captured in a DNA repair dioxygenase. NATURE[J]. 2010, 468(7321): 330-U223, http://dx.doi.org/10.1038/nature09497.
[77] Yu, Kunqian, Luo, Cheng, Qin, Guangrong, Xu, Zhijian, Li, Ning, Liu, Hong, Shen, Xu, Ma, Jianpeng, Wang, Qinghua, Yang, Caiguang, Zhu, Weiliang, Jiang, Hualiang. Why are oseltamivir and zanamivir effective against the newly emerged influenza A virus (A/H1N1)?. CELL RESEARCH. 2009, 19(10): 1221-1224, https://www.webofscience.com/wos/woscc/full-record/WOS:000270527600010.
[78] Kunqian Yu, Cheng Luo, Guangrong Qin, Zhijian Xu, Ning Li, Hong Liu, Xu Shen, Jianpeng Ma, Qinghua Wang, Caiguang Yang, Weiliang Zhu, Hualiang Jiang. Why are oseltamivir and zanamivir effective against the newly emerged influenza A virus (A/HIN1)?. 细胞研究：英文版[J]. 2009, 1221-1224, http://lib.cqvip.com/Qikan/Article/Detail?id=31761703.
[79] Yang, CaiGuang, Garcia, Kristel, He, Chuan. Damage Detection and Base Flipping in Direct DNA Alkylation Repair. CHEMBIOCHEMnull. 2009, 10(3): 417-423, https://www.webofscience.com/wos/woscc/full-record/WOS:000263803100002.
[80] Yang, CaiGuang, Sullivan, Christopher, He, Chuan. Structural study of ABH proteins by utilizing chemical crosslinking strategy. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETYnull. 2007, 233: http://apps.webofknowledge.com/CitedFullRecord.do?product=UA&colName=WOS&SID=5CCFccWmJJRAuMzNPjj&search_mode=CitedFullRecord&isickref=WOS:000207722808349.
[81] Yi, Chengqi, Yang, CaiGuang, Duguid, Erica M, Jian, Xing, He, Chuan. Mechanistic studies on Escherichia coli AlkB protein through a disulfide crosslinking strategy. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETYnull. 2007, 233: http://apps.webofknowledge.com/CitedFullRecord.do?product=UA&colName=WOS&SID=5CCFccWmJJRAuMzNPjj&search_mode=CitedFullRecord&isickref=WOS:000207722808527.
[82] Li, Zigang, Zhang, Junliang, Brouwer, Chad, Yang, CaiGuang, Reich, Nicholas W, He, Chuan. Bronsted acid catalyzed addition of phenols, carboxylic acids, and tosylamides to simple olefins. ORGANIC LETTERS[J]. 2006, 8(19): 4175-4178, https://www.webofscience.com/wos/woscc/full-record/WOS:000240339700001.
[83] Reich, Nicholas W, Yang, CaiGuang, Shi, Zhangjie, He, Chuan. Gold(I)-catalyzed synthesis of dihydrobenzofurans from aryl allyl ethers. SYNLETT[J]. 2006, 1278-1280, https://www.webofscience.com/wos/woscc/full-record/WOS:000237719500034.
[84] 杨财广, 刘钢, 姜标. Preparing functional bis(indole)pyrazine by stepwise cross-coupling reactions: An efficient method to construct the skeleton of dragmacidin D. J. ORG. CHEM.[J]. 2002, 67(26): 9392-9396, http://ir.sioc.ac.cn/handle/331003/20179.
[85] 姜标, 杨财广, 王骏. Enantioselective synthesis for the (-)-Antipode of the pyazinone marine alkaloid, hamacanthin A. J. ORG. CHEM.[J]. 2001, 66(14): 4865-4869, http://ir.sioc.ac.cn/handle/331003/20117.
[86] 姜标, 王全伏, 杨财广, 胥敏. α-(Trifluoromehyl)ethenyl boronic acid as a useful trifluoromethyl containing building block. Preparation and palladium-catalysed coupling with aryl halides. TETRAHEDRONLETT[J]. 2001, 42(24): 4083-4085, http://ir.sioc.ac.cn/handle/331003/20127.

（ 1 ） 化学生物学学科前沿与展望, 科学出版社, 2013-08, 第 5 作者
（ 2 ） 中国学科发展战略·化学生物学, 科学出版社, 2015-03, 第 5 作者

   

（ 1 ） RNA去甲基化酶的作用机制和抑制剂研究, 主持, 国家级, 2014-01--2017-12
（ 2 ） RNA表观遗传对DNA损伤修复调控机制, 参与, 国家级, 2015-01--2019-12
（ 3 ） 基于新机制发现抗感染新类型活性化合物的研究, 主持, 市地级, 2016-01--2017-12
（ 4 ） 信号转导过程中蛋白质机器的活细胞标记与在体调控, 参与, 国家级, 2016-07--2021-06
（ 5 ） FBLD技术平台在抗菌新药研究中的应用, 主持, 国家级, 2016-07--2019-06
（ 6 ） mRNA去甲基化酶FTO的化学探针研究, 主持, 市地级, 2016-09--2017-12
（ 7 ） m1A去甲基化酶ALKBH3的小分子调控研究, 主持, 国家级, 2017-01--2020-12

（1）化学探针—化学生物学促进新药发现之桥   第十一届全国天然有机化学学术会议   2016-09-25
（2）Development of inhibitors for mRNA demethylase   2016-08-29
（3）化学探针—化学生物学促进新药发现之桥   中国化学会第30 届学术年会   2016-07-01
（4）Development of inhibitors for mRNA demethylase   第十届世界华人药物化学国际研讨会   2016-01-18
（5）Development of inhibitors of mRNA demethylase   2015-11-09
（6）Development of inhibitors for mRNA demethylase   2015-10-25
（7）Small-molecule targeting of E3 ligase adaptor SPOP in kidney cancer   第九届全国化学生物学学术会议   2015-08-30
（8）Antibacterial drug discovery: from Antibiotic to Antivirulence   2015-08-26
（9）Development of inhibitors for m6A RNA demethylase   2015年皇后镇分子生物学（上海）会议-药物发现与前沿技术   2015-03-20

已指导学生

刘洪川  02  52427  

陈报恩  01  19499  

刘幸  01  19499  

张婕  01  19499  

倪腾凤  02  67127  

现指导学生

刘桂杰  01  19499  

李琦  01  19499  

黄悦  01  19499  

侯孝晨  02  67129  

郑桐  01  19499  

徐洪蛟   02  67129  

李家慧  01  19499