个人简介蔡晓青，2011年在美国亚利桑那州立大学获博士学位；2011至2015年在美国Scripps研究所从事博士后研究；2016年通过中山大学“****二期”人才引进回国工作，任职中山大学药学院，从事药物化学生物学和生物技术药物的相关研究。长期致力于蛋白质修饰和偶联技术的研究，针对蛋白质的胞内转运途径和降解等关键科学问题，聚焦抗体和抗体偶联药物(ADC)的研究。作为第一作者及通信作者在国际著名刊物J. Am. Chem. Soc., J. Med. Chem, Chem. Eur. J.等发表学术论文多篇。申请获得国家和国际专利多项。主持多项国家级、省级、校级基金项目以及横向课题项目。
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研究方向以抗体为代表的生物大分子药物由于其优秀的药理学性质、高特异性、高亲和性和低毒副作用，是目前国际上重大疾病的首选或唯一的治疗方法，也是当前转化医学和药物研发中发展最为迅猛的领域。本课题组研究主要聚焦化学和生物学的前沿交叉领域，通过对蛋白质进行化学或酶法修饰、重组融合等方法的改造和修饰，实现抗体药物的功能改造和升级，进而提高对癌症等重大疾病的有效治疗。主要研究内容如下：
构建溶酶体靶向型的抗体偶联药物(ADC)，从分子水平上干预和调控ADC的内吞和胞内转运途径，实现增强ADC的抗肿瘤活性、拓宽ADC的肿瘤适应症。
利用溶酶体的降解途径，发展靶向蛋白质降解技术，降解疾病相关的细胞膜蛋白，实现“不可成药”靶标的功能干预。
通过遗传密码扩增技术，利用含有特殊活性基团的非天然氨基酸对蛋白质进行定点修饰，发展基于非天然氨基酸的蛋白质修饰和标记技术，实现蛋白功能和活性的改造和升级。
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教育经历2006年8月－2011年7月：博士，美国亚利桑那州立大学?
2004年9月－2006年7月：硕士，浙江大学
2000年9月－2004年7月：学士，浙江大学
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工作经历2016年9月－至今：副教授，中山大学药学院
2011年8月－2015年6月：博士后，美国Scripps研究所
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科研项目国家自然科学基金：青年科学基金项目，主持（2018-2020）
国家自然科学基金：重大研究计划培育项目，参加（2019-2021）
广东省基础与应用基础研究基金：面上项目，主持（2020-2022）
中山大学“****二期”启动项目，主持
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招聘招生信息本课题组和所在研究团队长期招聘具有药学、化学、生物学或相近专业背景，对蛋白质修饰、抗体和生物大分子药物感兴趣的特聘副研究员、博士后和研究助理。
欢迎有志于大分子药物和交叉学科研究的考生报考本课题组研究生。
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论著专利Qian Zhao, Guoying Guo, Weiwei Zhu, Yifan Da, Hongjiao Xu, Shuohan Wu, Yaping Cheng, Yani Zhou,?Xiaoqing Cai*, Xianxing Jiang*, Suzuki cross-coupling reaction with genetically encoded fluorosulfates for fluorogenic protein labeling, Chemistry-A European Journal, 26, 15938-15943, 2020.
Ying Han, Yifan Da, Mingjia Yu, Yaping Cheng, Xin Wang, Jiale Xiong, Guoying Guo, Yan Li, Xianxing Jiang,?Xiaoqing Cai*, Protein labeling?approach to improve lysosomal targeting and efficacy of antibody-drug conjugates, Organic & Biomolecular Chemistry, 18, 3229-3223, 2020.（封面文章）
Zhenquan?Liu, Xing?Feng, Jingyao Xu, Xianxing?Jiang,?Xiaoqing?Cai*, Construction of allylic amino acid derivatives through a catalytic asymmetric allylic alkylation of azlactones with vinyl cyclopropanes, Tetrahedron Letters, 61, 151694, 2020.?
Hongjiao Xu, Lu Gan, Ying Han, Yifan?Da, Jiale Xiong, Sihua Hong, Qian Zhao, Nazi Song,?Xiaoqing Cai*, Xianxing Jiang, Site-psecific labeling of an anti-MUC1 antibody: probing the effects of conjugation and linker chemistry on the internalization process, RSC Advances, 9, 1909-1917, 2019.
Yani Zhou, Nannan Chen, Yaping Chen,?Xiaoqing Cai*, Efficient Construction of Drug-like Bispirocyclic Scaffolds Via Organocatalytic Cycloadditions of α-Imino γ-Lactones and Alkylidene Pyrazolones, Journal of Visualized Experiments, 144, e59155, 2019.
Nannan Chen, Liping Zhu, Lu Gan, Zhenquan Liu, Rui Wang,?Xiaoqing Cai*, Xianxing Jiang, Asymmetric synthesis of bispiro[r-butyrolactone-pyrrolidin-4,4'-pyrozolone] scaffolds containg two quarternary spirocenters via an organocatalytic 1,3-dipolar cycloaddition, European Journal of Organic Chemistry, 2939-2943, 2018.
X. Cai, K. Tsuchikama, K. D. Janda*, Modulating anti-cocaine vaccine potency through hapten fluorination,?Journal of the American Chemical Society, 135, 2971–2974, 2013.?
?X. Cai, T. Whitfield, M. S. Hixon, Y. Grant, G. F. Koob, K. D. Janda*, Probing active cocaine vaccination performance through catalytic and noncatalytic hapten design,?Journal of Medicinal Chemistry, 56, 3701–3709, 2013.
X. Cai, T. Whitfield, A. Y. Moreno, Y. Grant, M. S. Hixon, G. F. Koob, K. D. Janda*, Probing the effects of hapten stability on cocaine vaccine immunogenicity,?Molecular Pharmaceutics, 10, 4176–4184, 2013.
C. J. Wenthur,?X. Cai, B. A. Ellis, K. D. Janda*, Augmenting the efficacy of anti-cocaine catalytic antibodies through chimeric hapten design and combinatorial vaccination, Bioorganic & Medicinal Chemistry Letters, 15, 3666-3668, 2017.?
J. Zhu,?X. Cai, T. Harris, M. Gooyit, M. Wood, M. Lardy, K. D. Janda*, Disarming Pseudomonas aeruginosa virulence factor LasB by leveraging a Caenorhabditis elegans infection model.?Chemistry & Biology, 22, 483–491, 2015.
J. Lu,?X. Cai, S. M. Hecht*, Concise synthesis of bicyclic pyridinol antioxidants,?Organic Letters, 12, 5189–5191, 2010.
X. Cai, K. D. Janda*, A chemoenzymatic approach toward the preparation of site-specific antibody-drug conjugates,?Tetrahedron Letters, 56, 3172–3175, 2015.
X. Cai, O. M. Khdour, J. Jaruvangsanti, S. M. Hecht*, Simplified bicyclic pyridinol analogues protect mitochondrial function,?Bioorganic & Medicinal Chemistry, 20, 3584–3595, 2012.
X. Cai, P. Zaleski, A. Cagir, S. M. Hecht, Deglycobleomycin A6 analogues modified in the methylvalerate moiety,?Bioorganic & Medicinal Chemistry, 19, 3831–3844, 2011.
X. Cai, N. Wang, X. Lin, Chemo-enzymatic synthesis of optically active polymeric prodrug of Naproxen, Ketoprofen and Ibuprofen,?Polymer, 47, 6491–6495, 2006.
X. Cai, N. Wang, X. Lin*, The preparation of polymerizable, optically active-non-steroidal anti-inflammatory drugs derivatives by irreversible enzymatic methods, Journal of Molecular Catalysis. B,?Enzymatic, 40, 51–57, 2006.
X. Cai, Z. Chen, N. Wang, X. Lin*, A facile method for preparation of polymerizable Optically active Ketoprofen prodrug by irreversible lipase-catalyzed resolution,?World Journal of Microbiology & Biotechnology, 22, 723–727, 2006.
L. M. Eubanks, B. A. Ellis,?X. Cai, J. E. Schlosburg, K. D. Janda*, A human recombinant monoclonal antibody to cocaine: preparation, characterization and behavioral studies,?Bioorganic & Medicinal Chemistry Letters, 24, 4664–4666, 2014.
J. L. Fullagar, A. L. Garner, A. K. Struss, J. A. Day, D. P. Martin, J. Yu,?X. Cai, K. D. Janda*, S. M. Cohen*, Antagonism of a zinc metalloprotease using a unique metal-chelating scaffold: tropolones as inhibitors of P. aeruginosa elastase,?Chemical Communications, 49, 3197–3199, 2013.
J. C. Chapuis, O. M. Khdour,?X. Cai, J. Lu, S. M. Hecht*, Synthesis and characterization of Δlac-acetogenins that potently inhibit mitochondrial complex I,?Bioorganic & Medicinal Chemistry, 17, 2204–2209, 2009.
J. Quan, N. Wang,?X. Cai, Q. Wu, X. Lin*, Controllable selective enzymatic synthesis of N-acyl and O-acylpropranolol vinyl esters and preparation of polymeric prodrug of propranolol,?Journal of Molecular Catalysis. B, Enzymatic,?44, 1–7, 2007.
Q. Wu*, Q. Chen,?X. Cai, J. Wang, J. Zhang, Preparation and conductivity of solid high-proton conductor silica gel containing 80 wt.% decatungstodivanadogermanic acid,?Materials Letters, 61, 663–665, 2007.
Q. Wu*,?X. Cai, W. Feng, W. Pang, Thermal stability of ternary transition metal heteropoly complexes,?Thermochimica Acta, 428, 15–18, 2005.?
S. M. Hecht*,?X. Cai, O. Khdour, J. I. A. Guajardo, 1H-Pyrroolo [2,3-B] Pyridine Derivatives and Their Use as Radical Quenchers, U.S. Patent on file: PCT/US2013/025590, 2013.