陈小华
研究员
所属大学: 中国科学院上海药物研究所
所属学院: 未知
个人主页:
https://simm.cas.cn/sourcedb/zw/gb2020/yjzz/202008/t20200825_5676092.html
个人简介
教育经历 2003.9-2008.6, 有机化学博士,中科院成都有机化学研究所 1999.9-2003.6, 理学学士, 温州大学,化学与材料工程学院 工作经历 2015. 6- 至今 研究员、课题组长,中科院上海药物研究所 2012. 1- 2015. 6 博士后, 加州大学旧金山分校(UCSF)药学院/美国索克生物研究所 2009. 11- 2011. 12 洪堡学者/博士后,德国柏林洪堡大学,生物有机化学研究所 2008. 9- 2009. 10 副教授,中国科学技术大学,化学与材料科学学院
研究领域
药物化学及化学生物学,目前课题组主要进行蛋白质相互作用和蛋白质稳态调控研究,结合药物化学、有机化学、分子及细胞生物学、蛋白质工程、化学蛋白质组学等多学科交叉手段和多种新兴技术,开展蛋白质间相互作用和靶标确证研究、基于靶向蛋白降解技术的创新药物研发等。 1) 发展活细胞中蛋白质相互作用工具箱,开展蛋白质功能及靶标发现研究; 2) 发展生物大分子靶向降解的筛选新技术,针对“难成药”靶标发现小分子降解剂; 3) 开展蛋白质稳态调控及其作用机制研究,发现高效的分子胶降解剂及创新药物研究。
近期论文
An-Di Guo,+ Ke-Nian Yan,+ Hao Hu,+ Linhui Zhai, Teng-fei Hu, Haixia Su, Yijia Chi, Jinyin Zha, Yechun Xu, Dongxin Zhao, Xiaojie Lu, Yong-Jiang Xu, Jian Zhang, Minjia Tan,* Xiao-Hua Chen*. Spatiotemporal and global profiling of DNA-protein interactions enables discovery of low-affinity transcription factors. Nat. Chem., 2023, 15, 803-814; DOI: 10.1038/s41557-023-01196-z.(+ contributed equally) Yali Xu+, Wensi Zhao+, Hui-Jun Nie+, Jiamin Wang+, Jingjing Fu, Hao Hu, Zihao Liu, Shengna Tao, Mingya Zhang, Yubo Zhou, Jia Li*, Minjia Tan*, Xiao-Hua Chen*. Cross-Linking Profiling of Molecular Glue Degrader-Induced E3 Ligase Interactome to Expand Target Space. Angew. Chem. Int. Ed. 2025, 64, e202505053.(+ contributed equally) Hao Hu,+ Wei Hu,+ An-Di Guo,+ Linhui Zhai,+ Song Ma, Hui-Jun Nie, Bin-Shan Zhou, Tianxian Liu, Xinglong Jia, Xing Liu, Xuebiao Yao, Minjia Tan* Xiao-Hua Chen*. Spatiotemporal and direct capturing global substrates of lysine-modifying enzymes in living cells. Nat. Commun., 2024, 15, 1465. DOI :10.1038/s41467-024-45765-3 (+ contributed equally ). Ke-Nian Yan,+ Yong-Qiang Nie,+ Jia-Yu Wang,+ Guang-Liang Yin, Qia Liu, Hao Hu, Xiaoxia Sun* and Xiao-Hua Chen*. Accelerating PROTACs Discovery through a Direct-to-Biology Platform Enabled by Modular Photoclick Chemistry. Advanced Science, 2024, 11, 2400594. DOI: 10.1002/advs.202400594. (+, contributed equally ) An-Di Guo,+ Dan Wei,+ Hui-Jun Nie,+ Hao Hu, Chengyuan Peng, Shao-Tong Li, Ke-Nian Yan, Bin-Shan Zhou, Lei Feng, Chao Fang, Minjia Tan, Ruimin Huang, Xiao-Hua Chen*. Light-induced primary amines and o-nitrobenzyl alcohols cyclization as a versatile photoclick reaction for modular conjugation; Nat. Commun., 2020, 11, 5472; (+, contributed equally ). Wei Hu, Yi Yuan, Cai-Hu Wang, Hong-Tao Tian, An-Di Guo, Hui-Jun Nie, Hao Hu, Minjia Tan, Zhuo Tang,* Xiao-Hua Chen*. Genetically Encoded Residue-Selective Photo-Crosslinker to Capture Protein-Protein Interactions in Living Cells; Chem., 2019, 5, 2955-2968. Hui-Jun Nie+, Hao Hu+, Xinming Qi+, Yin-Jue Zhou, Lu Liu, Xiao-Hua Chen*. General Platform for Efficient and Modular Assembly of GalNAc–siRNA Conjugates via Primary Amines and o-Nitrobenzyl Alcohol Cyclization Photoclick Chemistry Enabling Rapid Access to Therapeutic Oligonucleotides. JACS Au 2025, 5, 3, 1402–1412. (+, contributed equally ). Wen-Jing Wang+, Lixin Gao+, Simei Wang+, Wensi Huang+, Xin-Yu Meng, Hao Hu, Ziqiang Chen, Jingya Sun, Yali Yuan, Yubo Zhou, Xingxing Diao*, Ruimin Huang*, Jia Li*, Xiao-Hua Chen*. Discovery of Orally Bioavailable and Potent CDK9 Inhibitors for Targeting Transcription Regulation in Triple-Negative Breast Cancer. J. Med. Chem., 2024, 67, 10035–10056. (+, contributed equally ). Dan Wei,+ Hanlin Wang,+ Qinghe Zeng,+ Wenjing Wang, Bingbing Hao, Xule Feng, Peipei Wang, Ning Song, Weijuan Kan, Guifang Huang, Xiaoyu Zhou, Minjia Tan, Yubo Zhou, Ruimin Huang,* Jia Li,* Xiao-Hua Chen*. Discovery of Potent and Selective CDK9 Degraders for Targeting Transcription Regulation in Triple-Negative Breast Cancer; J. Med. Chem., 2021, 64, 14822-14847 ( +, contributed equally ) Yan Xu, Dingqiang Fu, Yi Yuan, Yan Peng, Juan Dong, Feng Du, Xin Huang, Guangxun Li, Xiaohua Chen,* Qiwei Wang,* and Zhuo Tang*; A heterobifunctional molecule recruits cereblon to an RNA scaffold and activates its PROTAC function,Cell Reports Physical Science, 2022, 3, 101064. Hui-Jun Nie+, Ying-Jie Fu+, Shang Long, Jia-Yu Wang, Wensi Zhao, Linhui Zhai, Yin-Long Yang, Minjia Tan, Hao Hu*, Xiao-Hua Chen*. Chemoproteomics reveals proteome-wide covalent and non-covalent targets of withaferin A. Acta Pharmacologica Sinica, 2025, DOI: 10.1038/s41401-024-01468-5 ( +, contributed equally ) Zhi-Feng, Zou,+ Lei, Yang,+ Hui-Jun, Nie,+ Jing, Gao,* Shu-Min, Lei, Yi, Lai, Fan, Zhang, Ernst, Wagner, Hai-Jun, Yu,* Xiao-Hua, Chen,* Zhi-Ai, Xu*. Tumor-targeted PROTAC prodrug nanoplatform enables precise protein degradation and combination cancer therapy. Acta Pharmacologica Sinica, 2024, DOI: 10.1038/s41401-024-01266-z. (+, contributed equally ) Hui-Jun Nie+, Ben-Fu Li+, Jingya Sun+, Yali Yuan+, Zhi-Gao Zhang, Hao Hu, Wen-Jing Wang, Ziqiang Chen, Simei Wang, Wensi Huang, Xingxing Diao, Jinghua Yu*, Ruimin Huang*, Xiao-Hua Chen*. Discovery of a Potent, selective and orally bioavailable CDK9 degrader for targeting transcription regulation in Triple-Negative breast cancer. Bioorganic Chemistry, 2024, 153, 107876. (+, contributed equally). Yanrui Suo, Kaige Li, Xing Ling, Kenian Yan, Weiwei Lu, Jinfeng Yue, Xiao-Hua Chen*, Zhiqiang Duan*, Xiaojie Lu*. Discovery Small-Molecule p300 Inhibitors Derived from a Newly Developed Indazolone-Focused DNA-Encoded Library. Bioconjugate Chem. 2024, 35, 1251–1257. Hongtao Tian, jiale yang, An-Di Guo, Yu Ran, Yun-Zhi Yang, Bing Yang,Ruimin Huang, Haiming Liu*, Xiao-Hua Chen*. Genetically Encoded Benzoyllysines Serve as Versatile Probe for Interrogating Histone Benzoylations and Interactions in Living Cells; ACS Chem. Biol., 2021,16, 2560-2569. An-Di Guo, Ke-Huan Wu, Xiao-Hua Chen*. Light-induced efficient and residue-selective bioconjugation of native proteins via indazolone formation; RSC Advances, 2021, 11, 2235. Hui-Jun Nie, An-Di Guo, Hai-Xia Lin, Xiao-Hua Chen*. Rapid and halide compatible synthesis of 2-Nsubstituted indazolone derivatives via photochemical cyclization in aqueous media, RSC Adv., 2019, 9, 13249-13253. Nan Li,* Honglian Feng, Qian Gong, Chunxiao Wu, Hao Zhou, Zhiyan Huang, Jun Yang, Xiao-Hua Chen,* Na Zhao.* BINOL-based chiral aggregation-induced emission luminogens and t.heir application in detecting copper(II) ions in aqueous media. J. Mater. Chem.C, 2015, 3, 11458-11463. Xiao-Hua Chen, Zheng Xiang, Ying S. Hu, Vanessa K. Lacey, Hu Cang, and Lei Wang*. Genetically Encoding an Electrophilic Amino Acid for Protein Stapling and Covalent Binding to Native Receptors. ACS Chem. Biol., 2014, 9, 1956-1961. Xiao-Hua Chen, Alexander Roloff, Oliver Seitz*. Consecutive Signal Amplification for DNA Detection Based on De Novo Fluorophore Synthesis and Host-Guest Chemistry. Angew. Chem. Int. Ed., 2012, 51, 4479-4483. Xiao-Hua Chen, Jie Yu and Liu-Zhu Gong*. The Role of Double Hydrogen Bonds in Asymmetric Direct Aldol Reactions Catalyzed by Amino Amide Derivatives. Chem. Commun., 2010, 46, 6437-6448. Xiao-Hua Chen, Qiang Wei, Shi-Wei Luo, Han Xiao, and Liu-Zhu Gong*. Organocatalytic Synthesis of Spiro[pyrrolidin-3,3′-oxindoles] with High Enantiopurity and Structural Diversity. J. Am. Chem. Soc.; 2009, 131, 13819-13825 Xiao-Hua Chen, Wen-Quan Zhang, and Liu-Zhu Gong*. Asymmetric Organocatalytic Three-Component 1,3-Dipolar Cycloaddition: Control of Stereochemistry via a Chiral Bronsted Acid Activated Dipole. J. Am. Chem. Soc.; 2008, 130, 5652-5653. Xiao-Hua Chen, Xiao-Ying Xu, Hua Liu, Lin-Feng Cun, and Liu-Zhu Gong*. Highly Enantioselective Organocatalytic Biginelli Reaction. J. Am. Chem. Soc.; 2006, 128, 14802-14803. Xiao-Hua Chen, Shi-Wei Luo, Zhuo Tang, Lin-Feng Cun, Ai-Qiao Mi, Yao-Zhong Jiang, and Liu-Zhu Gong*. Organocatalyzed Highly Enantioselective Direct Aldol Reactions of Aldehydes with Hydroxyacetone and Fluoroacetone in Aqueous Media. The Use of Water to Control the Regioselectivity. Chem. Eur. J.; 2007. 13. 689-701.