个人简介：

周晖皓，博士，教授，博士生导师。1999-2003年就读于中国科学技术大学生命科学学院生物科学专业，获学士学位；2003-2009年于中国科学技术大学生命科学学院，师从牛立文教授、滕脉坤教授学习生物化学与结构生物学，获理学博士学位；2009-2015年于美国Scripps研究所从事博士后研究，在Paul Schimmel教授、Xiang-Lei Yang教授指导下开展氨酰转运核糖核酸合成酶（AARS）相关的结构功能、发病机制及药物发现研究；2015年初入职中山大学药学院药物分子设计研究中心，受聘为教授、博士生导师。研究成果先后在Nature、Science、Nat Commun、J Biol Chem、J Mol Biol、ACS Chem Biol、Eur J Med Chem等国际学术期刊发表了50多篇高水平研究论文，申请国内外发明专利多项。
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研究方向：
? 药物靶标结构生物学
? 基于片段的药物发现
? 药物化学生物学
蛋白质是生命活动的载体，也是药物作用的主要靶标。深入理解蛋白质的生物学功能、阐明蛋白质功能失调与疾病发生之间的关系、开展理性的药物分子设计等等，都依赖于蛋白质的高分辨率三维结构。特别是，药物靶蛋白与药物分子复合物的三维结构对于在原子分辨率水平上理解药物分子的作用机制，对于开展结构指导的药物分子设计与优化研究，都发挥着核心作用。我们的研究方向就是利用X射线晶体学等结构生物学技术手段，解析关键生命活动过程中的药物靶蛋白的三维结构，以靶标为中心开展发病机制、结构药理、药物设计和药物化学等药学研究。基于片段的药物发现（FBDD）是近年来快速发展的药物发现新方法。我们的研究方向还包括针对药物靶蛋白发展片段筛选新技术，解析片段与靶蛋白的共晶结构，从而鉴定新颖的化学基元和发现靶蛋白的新可药口袋，并在此基础上设计新骨架、新机制的药物先导物。
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教育经历：

2003.09 - 2009.06: 理学博士，中国科学技术大学生命科学学院
2001.09 - 2003.06: 工学双学士，中国科学技术大学计算机系
1999.09 - 2003.06: 理学学士，中国科学技术大学生命科学学院
1993.09 - 1999.06: 湖南桃源第一中学
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工作经历：

2015.01 - 至今??? 中山大学药学院教授
2009.09 - 2015.01? 美国Scripps研究所博士后
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教学情况：
主讲和参与教学的课程：
本科生课程：《结构生物学与药学研究》
《生物化学与分子生物学实验》
研究生课程：《结构生物学》
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学术兼职：

2021 - 至今? ??广东省药理学会第二届药物筛选与评价专业委员会常务委员
2020 - 至今? ??中国药学会第九届老年药学专业委员会委员
2018 - 至今? ??广东省药学会第十届药物化学专业委员会委员
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科研项目：

国家自然科学基金面上项目，**，负责人
广东省自然科学基金面上项目，2019A，负责人
国家重点研发计划政府间国际科技创新合作重点专项，2017YFE**，参与人
广东省自然科学基金自由申请项目，2017A，负责人
广东省“珠江人才计划”引进创新创业团队，2016ZT06Y337，团队核心成员，子课题负责人
中央高校基本科研业务费医科重大项目培育项目，36，负责人
中山大学“****二期”青年杰出人才项目，36，负责人
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学术论文：

(^# first author; * corresponding author)
Bingyi Chen, Siting Luo, Songxuan Zhang, Yingchen Ju, Qiong Gu, Jun Xu, Xiang-Lei Yang, Huihao Zhou*, Inhibitory mechanism of reveromycin A at the tRNA binding site of a class I synthetase, Nature Communications, 2021, 12, 1616.
Zhiteng Luo, Siting Luo, Yingchen Ju, Peng Ding, Jun Xu, Qiong Gu, Huihao Zhou*, Structural insights into the ligand recognition and catalysis of the key aminobutanoyltransferase CntL in staphylopine biosynthesis, The FASEB Journal, 2021, 35, e21575.
Litao Sun^#, Na Wei^#, Bernhard Kuhle, David Blocquel, Scott Novick, Zaneta Matuszek, Huihao Zhou, Weiwei He, Jingjing Zhang, Thomas Weber, Rita Horvath, Philippe Latour, Tao Pan, Paul Schimmel*, Patrick Griffin, Xiang-Lei Yang*, CMT2N-causing aminoacylation domain mutants enable Nrp1 interaction with AlaRS, Proceedings of the National Academy of Sciences of the United States of America, 2021, 118, e.
Mengyang Xu^#, Chao Zhao^#, Biying Zhu, Liangyue Wang, Huihao Zhou, Daoguang Yan*, Qiong Gu*, Jun Xu*, Discovering high potent Hsp90 inhibitors as anti- nasopharyngeal carcinoma agent through fragment assembling approach, Journal of Medicinal Chemistry, 2021, 64, 2010-2023.
Songxuan Zhang, Yuting Zhang, Yuying Fang, Hao Chen, Mengjiao Hao, Qingyun Tan, Chen Hu, Huihao Zhou, Jun Xu, Qiong Gu*, Synthesis and evaluation of andrographolide derivatives as potent anti-osteoporosis agents in vitro and in vivo, European Journal of Medicinal Chemistry, 2021, 213, 113185.
Zhejun Sun^#, Yuting Zhang^#, Huihao Zhou, Jun Xu*, Qiong Gu*, Diverse diterpenoids and sesquiterpenoids from Siegesbeckia pubescens and their activity against RANKL-induced osteoclastogenesis, Bioorganic Chemistry, 2021, 107, 104537.
Jieyu Tang^#, Yingchen Ju^#, Jingwei Zhou, Junsong Guo, Qiong Gu, Jun Xu, Huihao Zhou*, Structural and biochemical characterization of SbnC as a representative of type B siderophore synthetases, ACS Chemical Biology, 2020, 15, 2731-2740.
Junsong Guo, Bingyi Chen, Ying Yu, Bao Cheng, Yingchen Ju, Jieyu Tang, Qiong Gu, Jun Xu, Huihao Zhou*, Structure-guided optimization and mechanistic study on a class of quinazolinone-threonine hybrids as antibacterial ThrRS inhibitors, European Journal of Medicinal Chemistry, 2020, 207, 112848.
Ziyang Chen^#, Hao Chen^#, Zizhen Zhang, Peng Ding, Xin Yan, Yanwen Li, Songxuan Zhang, Qiong Gu, Huihao Zhou*, Jun Xu*, Discovery of novel liver X receptor inverse agonists as lipogenesis inhibitors, European Journal of Medicinal Chemistry, 2020, 206, 112793.
Hao Chen^#, Ziyang Chen^#, Zizhen Zhang^#, Yali Li, Shushu Zhang, Fuqiang Jiang, Junkang Wei, Peng Ding, Huihao Zhou*, Qiong Gu*, Jun Xu*, Discovery of new LXRβ agonists as glioblastoma inhibitors, European Journal of Medicinal Chemistry, 2020, 194, 112240.
Junsong Guo^#, Bingyi Chen^#, Ying Yu, Bao Cheng, Yanfang Cheng, Yingchen Ju, Qiong Gu, Jun Xu, Huihao Zhou*, Discovery of novel tRNA-amino acid dual-site inhibitors against threonyl-tRNA synthetase by fragment-based target hopping, European Journal of Medicinal Chemistry, 2020, 187, 111941.?
Hongjiao Xu^#, Qian Zhao^#, Nazi Song^#, Zhibin Yan, Runfeng Lin, Shuohan Wu, Lili Jiang, Sihua Hong, Junqiu Xie, Huihao Zhou, Rui Wang, Xianxing Jiang*, AdipoR1/AdipoR2 dual agonist recovers nonalcoholic steatohepatitis and related fibrosis via endoplasmic reticulum-mitochondria axis. Nature Communications, 2020, 11, 5807.
Qi Huang^#, Zhemin Zhang^#, Huinan Li^#, Yu Guo, Xiangwen Liao, Hongyan Li, Huihao Zhou, Wei Xia*, Identification of a novel inhibitor of catabolite control protein A from Staphylococcus aureus, ACS Infectious Diseases, 2020, 6, 347-354.
Mengyang Xu^#, Biying Zhu^#, Xiuye Cao^#, Shannai Li, Dan Li, Huihao Zhou, Vesa M. Olkkonen, Wenbin Zhong*, Jun Xu*, Daoguang Yan*, OSBP-related protein 5L maintains intracellular IP3/Ca²⁺ signaling and proliferation in T Cells by facilitating PIP2 hydrolysis, The Journal of Immunology, 2020, 204, 1134-1145.
Shengheng Yuan^#, Pei Hua^#, Chao Zhao, Huihao Zhou, Jiake Xu, Jun Xu*, Qiong Gu*, Jatrophane diterpenoids from Euphorbia esula as inhibitors of RANKL-induced osteoclastogenesis, Journal of Natural Products, 2020, 83, 1005-1017.
Shengheng Yuan^#, Yuting Zhang^#, Pei Hua, Huihao Zhou, Jun Xu, Qiong Gu*, Discovery of Ingenane and Jatrophane Diterpenoids from Euphorbia esula as Inhibitors of RANKL-Induced Osteoclastogenesis, Fitoterapia, 2020, 146, 104718.?
Jieyu Tang^#, Yingchen Ju^#, Qiong Gu, Jun Xu, Huihao Zhou*, Structural insights into substrate recognition and activity regulation of the key decarboxylase SbnH in staphyloferrin B biosynthesis, Journal of Molecular Biology, 2019, 431, 4868-4881.
Siting Luo^#, Yingchen Ju^#, Jingwei Zhou, Qiong Gu, Jun Xu, Huihao Zhou*, Crystal structure of CntK, the cofactor-independent histidine racemase in staphylopine-mediated metal acquisition of Staphylococcus aureus, International Journal of Biological Macromolecules, 2019, 135, 725-733.
Zizhen Zhang^#, Hao Chen^#, Ziyang Chen, Peng Ding, Yingchen Ju, Qiong Gu, Jun Xu, Huihao Zhou*, Identify Liver X receptor β modulator building blocks by developing a fluorescence polarization-based assay, European Journal of Medicinal Chemistry, 2019, 178, 458-467.
Chang Wen, Xin Yan, Qiong Gu, Jiewen Du, Di Wu, Yutong Lu, Huihao Zhou*, Jun Xu*, Systematic Studies on the Protocol and Criteria for Selecting a Covalent Docking Tool, Molecules, 2019, 24, 2183.
Peng Ding^#, Ziyang Chen^#, Hao Chen, Zizhen Zhang, Zhihong Liu, Xin Yan, Huihao Zhou, Qiong Gu, Chanjuan Li*, Jun Xu*, Structurally selective mechanism of liver X receptor ligand: in silico and in vitro studies, Journal of Chemical Information and Modeling, 2019, 59, 7, 3277-3299.
Chanjuan Li^#, Hao Chen^#, Xinying Chen, Yanwen Li, Pei Hua, Junkang Wei, Ching Song, Qiong Gu,? Huihao Zhou, Jingxia Zhang*, Jun Xu*, Discovery of tissue selective liver X receptor agonists for the treatment of atherosclerosis without causing hepatic lipogenesis, European Journal of Medicinal Chemistry, 2019, 182, 111647.
Yuying Fang, Huihao Zhou, Qiong Gu*, Jun Xu*, Synthesis and evaluation of tetrahydroisoquinoline- benzimidazole hybrids as multifunctional agents for the treatment of Alzheimer's disease, European Journal of Medicinal Chemistry, 2019, 167, 133-145.
Xiuming Li^#, Xin Yan^#, Qiong Gu, Huihao Zhou, Di Wu, Jun Xu*, DeepChemStable: Chemical Stability Prediction with an Attention-Based Graph Convolution Network, Journal of Chemical Information and Modeling, 2019, 59, 1044-1049.
Xiuming Li^#, Xin Yan^#*, Yuedong Yang, Qiong Gu, Huihao Zhou, Yunfei Du, Yutong Lu, Jielou Liao, Jun Xu*, LSA: a local-weighted structural alignment tool for pharmaceutical virtual screening, RSC Advances, 2019, 9, 3912-3917.
Wenjuan Xia^#, Pan Luo^#, Pei Hua, Peng Ding, Chanjuan Li, Jun Xu, Huihao Zhou, Qiong Gu*, Discovery of a new pterocarpan-type anti-neuroinflammatory compound from Sophora tonkinensisis through suppression of the TLR4/NF-κB/MAPK signaling pathway with PU.1 as a Potential Target, ACS Chemical Neuroscience, 2019, 10, 295-303.
Xiaojie Huang, Junsong Guo, Qi Liu, Qiong Gu, Jun Xu, Huihao Zhou*, Identification of an auxiliary druggable pocket in DNA gyrase ATPase domain using fragment probes, MedChemComm, 2018, 9, 1619-1629.
Pan Luo, Zhi-Yong Yin, Zhe-Jun Sun, Hao Chen, Chan-Juan Li, Hui-Hao Zhou, Qiong Gu*, Jun Xu, Cembrane-type diterpenoids from Macaranga pustulata, Fitoterapia, 2018, 129, 162-166. ?
Yuying Fang^#, Wenjuan Xia^#, Bao Cheng, Pei Hua, Huihao Zhou, Qiong Gu*, Jun Xu*, Design, synthesis, and biological evaluation of compounds with a new scaffold as anti-neuroinflammatory agents for the treatment of Alzheimer's disease, European Journal of Medicinal Chemistry, 2018, 149, 129-138.
Zhihong Liu^#, Jiewen Du^#, Xin Yan, Jiali Zhong, Lu Cui, Jinyuan Lin, Lizhu Zeng, Peng Ding, Pin Chen, Xinxin Zhou, Huihao Zhou, Qiong Gu*, Jun Xu*, TCMAnalyzer: a Chemo- and Bioinformatics Web Service for Analyzing Traditional Chinese Medicine, Journal of Chemical Information and Modeling, 2018, 58, 550-555.
Chanjuan Li^#, Bao Cheng^#, Sai Fang, Huihao Zhou, Qiong Gu*, Jun Xu*, Design, syntheses and lipid accumulation inhibitory activities of novel resveratrol mimics, European Journal of Medicinal Chemistry, 2018, 143, 114-122.
Xiaoling Xu*, Huihao Zhou, Quansheng Zhou, Fei Hong, My-Nuong Vo, Wanqiang Niu, Zhiguo Wang, Xiaolin Xiong, Kanaha Nakamura, Keisuke Wakasugi, Paul Schimmel, Xiang-Lei Yang*, An alternative conformation of human TrpRS suggests a role of zinc in activating non-enzymatic function, RNA Biology, 2018, 15, 649-658.
Peng Ding^#, Xin Yan^#, Zhihong Liu, Jiewen Du, Yunfei Du, Yutong Lu, Di Wu, Yuehua Xu, Huihao Zhou, Qiong Gu, Jun Xu*, PTS: a pharmaceutical target seeker, Database, 2017, 2017, bax095.
Youngzee Song, Huihao Zhou, My-Nuong Vo, Yi Shi, Mir Hussain Nawaz, Oscar Vargas-Rodriguez,? Jolene K. Diedrich, John R. Yates III, Shuji Kishi, Karin Musier-Forsyth, Paul Schimmel*, Double mimicry evades tRNA synthetase editing by toxic vegetable-sourced non-proteinogenic amino acid, Nature Communications, 2017, 8, 2281.
Yingchen Ju, Zhihong Liu, Zizhen Zhang, Lijun Duan, Qi Liu, Qiong Gu, Cheng Zhang, Jun Xu*, Huihao Zhou*, Membrane binding of the insertion sequence of Proteus vulgaris L-amino acid deaminase stabilizes protein structure and increases catalytic activity, Scientific Reports, 2017, 7, 13719.
Jiewen Du^#, Xin Yan^#, Zhihong Liu, Lu Cui, Peng Ding, Xiaoqing Tan, Xiuming Li, Huihao Zhou, Qiong Gu*, Jun Xu*, cBinderDB: a covalent binding agent database, Bioinformatics, 2017, 33, 1258-1260.
Yingchen Ju, Shuilong Tong, Yongxiang Gao, Wei Zhao, Qi Liu, Qiong Gu, Jun Xu, Liwen Niu*, Maikun Teng*, Huihao Zhou*, Crystal structure of a membrane-bound L-amino acid deaminase from Proteus vulgaris, Journal of Structural Biology, 2016, 195, 306-315.
Litao Sun, Ana Cristina Gomes, Weiwei He, Huihao Zhou, Xiaoyun Wang, David W. Pan, Paul Schimmel, Tao Pan*, Xiang-Lei Yang*, Evolutionary gain of alanine mischarging to non-cognate tRNAs with a G4:U69 base pair, Journal of the American Chemical Society, 2016, 138, 12948-12955.
Zhihong Liu, Peng Ding, Xin Yan, Minghao Zheng, Huihao Zhou, Yuehua Xu, Yunfei Du, Qiong Gu, Jun Xu*, ASDB: a resource for probing protein functions with small molecules, Bioinformatics, 2016, 32, 1752-1754.
Gongrui Guo, Yongxiang Gao, Zhongliang Zhu, Debiao Zhao, Zhihong Liu, Huihao Zhou*, Liwen Niu*, Maikun Teng*, Structural and biochemical insights into the DNA-binding mode of MjSpt4p:Spt5 complex at the exit tunnel of RNAPII, Journal of Structural Biology, 2015, 192, 418-425.
Weiwei He^#, Ge Bai^#, Huihao Zhou, Na Wei, Nicholas M. White, Janelle Lauer, Huaqing Liu, Yi Shi, Calin Dan Dumitru, Karen Lettieri, Veronica Shubayev, Albena Jordanova, Velina Guergueltcheva, Patrick R. Griffin, Robert W. Burgess, Samuel L. Pfaff*, Xiang-Lei Yang*, CMT2D neuropathy is linked to the neomorphic binding activity of glycyl-tRNA synthetase, Nature, 2015, 526, 710-714.
Long Li, Xiu Le, Ling Wang, Qiong Gu, Huihao Zhou, Jun Xu*, Discovering new DNA gyrase inhibitors using machine learning approaches, RSC Advances, 2015, 5, 105600-105608.
Jonathan D. Herman^#, Lauren R. Pepper^#, Joseph F. Cortese, Guillermina Estiu, Kevin Galinsky, Vanessa Zuzarte-Luis, Emily R. Derbyshire, Ulf Ribacke, Amanda K. Lukens, Sofia A. Santos, Vishal Patel, Clary B. Clish, William J. Sullivan Jr., Huihao Zhou, Selina E. Bopp, Paul Schimmel, Susan Lindquist, Jon Clardy, Maria M. Mota, Tracy L. Keller, Malcolm Whitman, Olaf Wiest, Dyann F. Wirth*, Ralph Mazitschek*, The cytoplasmic prolyl-tRNA synthetase of the malaria parasite is a dual-stage target of febrifugine and its analogs, Science Translational Medicine, 2015, 7, 288ra77.
Qianzhi Ding, Chanjuan Li, Ling Wang, Yali Li, Huihao Zhou, Qiong Gu*, Jun Xu*, Identifying farnesoid X receptor agonists by na?ve Bayesian and recursive partitioning approaches, MedChemComm, 2015, 6, 1393-1403.
Ryuta Ishimura^#, Gabor Nagy^#, Ivan Dotu, Huihao Zhou, Xiang-Lei Yang, Paul Schimmel, Satoru Senju, Yasuharu Nishimura, Jeffrey H. Chuang, Susan L. Ackerman*, Ribosome stalling induced by mutation of a CNS-specific tRNA causes neurodegeneration, Science, 2014, 345, 455-459.
Huihao Zhou, Litao Sun, Xiang-Lei Yang, Paul Schimmel*, ATP-directed capture of bioactive herbal-based medicine on human tRNA synthetase, Nature, 2013, 494, 121-124.
Huihao Zhou^#, Zhao Zha^#, Yang Liu^#, Hongtao Zhang, Juanjuan Zhu, Siyi Hu, Guodong Shen, Liansheng Cheng, Liwen Niu, Mark I. Greene, Maikun Teng*, Jing Liu*, Structural insight into the down-regulation of overexpressed p185(her2/neu) protein of transformed cells by the antibody chA21. Journal of Biological Chemistry, 2011, 286, 31676-31683.
Huihao Zhou, Qi Liu, Yongxiang Gao, Maikun Teng*, Liwen Niu*, Crystal structure of NusG N-terminal (NGN) domain from Methanocaldococcus jannaschii and its interaction with rpoE”, Proteins: Structure, Function, and Bioinformatics, 2009, 76, 784-793.
Huihao Zhou, Qi Liu, Weili Yang, Yongxiang Gao, Maikun Teng*, Liwen Niu*, Monomeric tRNA (m(7)G46) methyltransferase from Escherichia coli presents a novel structure at the function-essential insertion, Proteins: Structure, Function, and Bioinformatics, 2009, 76, 512-515.
Yang Liu, Huihao Zhou, Juanjuan Zhu, Yongxiang Gao, Liwen Niu, Jing Liu*, Maikun Teng*, Crystallization and preliminary crystallographic studies of the single-chain variable fragment of antibody chA21 in complex with an N-terminal fragment of ErbB2, Acta Crystallographica Section F: Structural Biology and Crystallization Communications, 2009, 65, 692-694.
Shuilong Tong, Huihao Zhou, Yongxiang Gao, Zhiqiang Zhu, Xiao Zhang, Maikun Teng*, Liwen Niu*, Crystal structure of human osteoclast stimulating factor, Proteins: Structure, Function, and Bioinformatics, 2009, 75, 245-251.
Yingji Cui, Heng Li, Xu Li, Yang Li, Huihao Zhou, Liwen Niu*, Maikun Teng*, Crystallization and preliminary crystallographic analysis of the second RRM of Pub1 from Saccharomyces cerevisiae, Acta Crystallographica Section F: Structural Biology and Crystallization Communications, 2009, 65, 108-110.?
Qi Liu, Yang Gao, Weili Yang, Huihao Zhou, Yongxiang Gao, Xiao Zhang, Maikun Teng*, and Liwen Niu*, Crystallization and preliminary crystallographic analysis of tRNA (m(7)G46) methyltransferase from Escherichia coli, Acta Crystallographica Section F: Structural Biology and Crystallization Communications, 2008, 64, 743-745.
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发明专利：



周晖皓，郭俊松，陈冰怡，顾琼，徐峻，“一种喹唑啉酮类化合物及其制备方法和应用”，中国发明专利号：ZL9.7，2021-04-03。
周晖皓，张子振，陈浩，顾琼，徐峻，“一种化合物及其制备方法和作为荧光偏振探针在LXRβ 配体筛选中的应用”，中国发明专利号：ZL8.0，2020-09-25。
周晖皓，程宝，顾琼，徐峻，“一种去氧常山酮类化合物及其制备方法和应用”，中国发明专利申请号：5.1，2018-08-24。
顾琼，徐峻，房玉影，夏文娟，周晖皓，程宝，“一种抗神经炎症的二苯乙烯类似物及其制备方法和应用”，中国发明专利申请号：4.4，2018-02-09。
周晖皓，黄晓杰，郭俊松，顾琼，徐峻，“一种DNA促旋酶的药物结合口袋及其应用”，中国发明专利申请号：6.7，2018-03-09。
Xiang-Lei Yang, Na Wei, Huihao Zhou, Paul Schimmel. Binding activity of aminoacyl-tRNA synthetase in Charcot-Marie-Tooth (CMT) neuropathy and CMT-related neurological disease. International Publication Number: WO, 2017-04-20.?
刘兢，程联胜，刘洋，周晖皓，滕脉坤，朱娟娟，魏海明，肖卫华，“一种抗原-抗体复合物晶体及其制备方法与抗原表位”，中国发明专利号：ZL2.8，2011-04-20。