基于核酸编码化合库筛选平台的药物发现技术开发

将核酸编码化合库筛选技术和其他药物开发技术（人工智能药物设计、化学蛋白组学和天然产物药物开发等）相结合，设计并合成针对特定靶点的核酸编码集中库来加快小分子、环肽和核酸药物的开发。 

1. 针对特定靶点的核酸编码集中库的设计、合成和筛选 

2. 核酸编码环肽库，糖库和共价化合物库的设计、合成和筛选技术开发

3. 核酸药物的靶向递送技术开发

4. 核酸编码化合物库在蛋白降解药物（分子胶和Protac）开发中的应用

   

100701-药物化学

小分子药物筛选， DNA Encoded Library

   

2007.9-2011.5 Brandeis University, 有机化学博士 　　

2005.9-2007.8 Brandeis University, 有机化学硕士　　

2001.9-2005.6南京大学，化学本科

博士

2017.7-至今 上海药物研究所，课题组长，研究员 　　

2016.5-2017.6葛兰素史克, 美国波士顿， Associate Fellow　　

2010.11-2016.5葛兰素史克, 美国波士顿, 研究员

国家引才计划青年人才计划

[1] 郑明月, 陆晓杰, 刘小红, 蒋华良, 李召军. 一种基于DNA编码化合物数据库的系统及其分析方法. CN: CN110021366A, 2019-07-16.

[2] 王璇, 索延瑞, 张雨晴, 刘小红, 郑明月, 蒋华良, 陆晓杰. DNA编码化合物文库起始片段及其制备和应用. CN: CN115506036A, 2022-12-23.

[3] 温馨, 张敏敏, 段志强, 沈爱军, 耿美玉, 陆晓杰. 一种GST蛋白抑制剂、其制备方法、药用组合物及其用途. CN: CN116693515A, 2023-09-05.

[4] 凌星, 闫克念, 段志强, 岳金凤, 郑明月, 陈小华, 陆晓杰. 一种CBP/P300抑制剂、其制备方法、药用组合物及其用途. CN: CN116446054A, 2023-07-18.

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[10] Wu, Wenting, Sun, Zhen, Wang, Xuan, Lu, Xiaojie, Dai, Dongcheng. Construction of Thiazole-Fused Dihydropyrans via Formal 4+2 Cycloaddition Reaction on DNA. ORGANIC LETTERS[J]. 2020, 22(8): 3239-3244, https://www.webofscience.com/wos/woscc/full-record/WOS:000526894000075.
[11] Li, Ke, Liu, Xiaohong, Liu, Sixiu, An, Yulong, Shen, Yanfang, Sun, Qingxia, Shi, Xiaodong, Su, Wenji, Cui, Weiren, Duan, Zhiqiang, Kuai, Letian, Yang, Hongfang, Satz, Alexander L, Chen, Kaixian, Jiang, Hualiang, Zheng, Mingyue, Peng, Xuanjia, Lu, Xiaojie. Solution-Phase DNA-Compatible Pictet-Spengler Reaction Aided by Machine Learning Building Block Filtering. ISCIENCE[J]. 2020, 23(6): http://dx.doi.org/10.1016/j.isci.2020.101142.
[12] Wen, Xin, Duan, Zhiqiang, Liu, Jiaxiang, Lu, Weiwei, Lu, Xiaojie. On-DNA Cross-Dehydrogenative Coupling Reaction toward the Synthesis of Focused DNA-Encoded Tetrahydroisoquinoline Libraries. ORGANIC LETTERS[J]. 2020, 22(15): 5721-5725, http://dx.doi.org/10.1021/acs.orglett.0c01565.
[13] Qu, Yi, Liu, Sixiu, Wen, Huanan, Xu, Yanfen, An, Yulong, Li, Ke, Ni, Mengyuan, Shen, Yanfang, Shi, Xiaodong, Su, Wenji, Cui, Weiren, Kuai, Letian, Satz, Alexander L, Yang, Hongfang, Lu, Xiaojie, Peng, Xuanjia. Palladium-mediated Suzuki-Miyaura Cross-Coupling Reaction of Potassium Boc-protected aminomethyltrifluoroborate with DNA-Conjugated aryl bromides for DNA-Encoded chemical library synthesis. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS[J]. 2020, 533(2): 209-214, http://dx.doi.org/10.1016/j.bbrc.2020.04.027.
[14] Wang, Xuan, Sun, Hui, Liu, Jiaxiang, Zhong, Wenge, Zhang, Mingqiang, Zhou, Hu, Dai, Dongcheng, Lu, Xiaojie. Palladium-Promoted DNA-Compatible Heck Reaction. ORGANIC LETTERS[J]. 2019, 21(3): 719-723, https://www.webofscience.com/wos/woscc/full-record/WOS:000457947900030.
[15] Wang, Xuan, Sun, Hui, Liu, Jiaxiang, Dai, Dongcheng, Zhang, Mingqiang, Zhou, Hu, Zhong, Wenge, Lu, Xiaojie. Ruthenium-Promoted C-H Activation Reactions between DNA-Conjugated Acrylamide and Aromatic Acids. ORGANIC LETTERS[J]. 2018, 20(16): 4764-4768, http://dx.doi.org/10.1021/acs.orglett.8b01837.
[16] Li, Hailong, Sun, Zhen, Wu, Wenting, Wang, Xuan, Zhang, Mingqiang, Lu, Xiaojie, Zhong, Wenge, Dai, Dongcheng. Inverse-Electron-Demand Diels-Alder Reactions for the Synthesis of Pyridazines on DNA. ORGANICLETTERS[J]. 2018, 20(22): 7186-7191, https://www.webofscience.com/wos/woscc/full-record/WOS:000451101500046.
[17] Lu, Xiaojie, Fan, Lijun, Phelps, Christopher B, Davie, Christopher P, Donahue, Christine P. Ruthenium Promoted On-DNA Ring-Closing Metathesis and Cross-Metathesis. BIOCONJUGATE CHEMISTRY[J]. 2017, 28(6): 1625-1629, https://www.webofscience.com/wos/woscc/full-record/WOS:000404090500004.
[18] Lu, Xiaojie, Roberts, Sarah E, Franklin, George J, Davie, Christopher P. On-DNA Pd and Cu promoted C-N cross-coupling reactions. MEDCHEMCOMM[J]. 2017, 8(8): 1614-1617, https://www.webofscience.com/wos/woscc/full-record/WOS:000407769400004.
[19] Thomas, Baptiste, Lu, Xiaojie, Birmingham, William R, Huang, Kun, Both, Peter, Martinez, Juana Elizabeth Reyes, Young, Robert J, Davie, Christopher P, Flitsch, Sabine L. Application of Biocatalysis to on-DNA Carbohydrate Library Synthesis. CHEMBIOCHEM[J]. 2017, 18(9): 858-863, https://www.webofscience.com/wos/woscc/full-record/WOS:000400572500007.
[20] 陆晓杰. Hydrogen Bonding-Mediated Cooperative Organocataoysis by Modified Cinchona Alkaloids. Wiley-VCH Gmbh & Co. 2015, [21] Hu, Lin, Lu, Xiaojie, Deng, Li. Catalytic Enantioselective Peroxidation of alpha,beta-Unsaturated Aldehydes for the Asymmetric Synthesis of Biologically Important Chiral Endoperoxides. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY[J]. 2015, 137(26): 8400-8403, https://www.webofscience.com/wos/woscc/full-record/WOS:000357964400022.
[22] Lu, Xiaojie, Deng, Li. Catalytic Asymmetric Peroxidation of alpha,beta-Unsaturated Nitroalkenes by a Bifunctional Organic Catalyst. ORGANIC LETTERS[J]. 2014, 16(9): 2358-2361, https://www.webofscience.com/wos/woscc/full-record/WOS:000335491000016.
[23] 刘. Catalytic Enantioselective Peroxidation of a,b-Unsaturated Ketones. 2008, [24] 陆晓杰. Asymmetric aza-Michael reactions of a,b-unsaturated ketones with bifunctional organic catalysts. Angew. Chem. Int. Ed. 2008, [25] 陆晓杰. Enantioselective Diels-Alder reaction of simple a,b-unsaturated ketones with a Cinchona Alkaloid catalyst. JAMCHEMSOC. 2008,