陆晓杰 - 中国科学院上海药物研究所 -

个人简介

陆晓杰，2005年毕业于南京大学化学系获得化学学士学位，随后到美国Brandeis University 在邓力老师的指导下从事有机小分子催化的不对称反应研究。在2007和2011年先后获得了有机化学的硕士和博士学位。2010年底加入美国葛兰素史克（GSK）任研究员,专门从事核酸编码化合物库的技术开发研究，并于2016年入选了葛兰素史克Associate Fellow。2017年入选国家高层次人才青年计划并加入中国科学院上海药物研究所任研究员及课题组长。教育经历 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，化学本科工作经历 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

研究领域

将核酸编码化合库筛选技术和其他药物开发技术（计算机辅助药物设计，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

近期论文

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Lulu Jiang, Sixiu Liu, Xinglong Jia, Qinting Gong, Xin Wen, Weiwei Lu, Jintong Yang, Xinyuan Wu, Xuan Wang, Yanrui Suo, Yilin Li, Motonari Uesugi, Zhi-bei Qu, Minjia Tan*, Xiaojie Lu* and Lu Zhou*，ABPP-CoDEL: Activity-Based Proteome Profiling-Guided Discovery of Tyrosine-Targeting Covalent Inhibitors from DNA-Encoded Libraries，J.Am.Chem.Soc. 2023, https://doi.org/10.1021/jacs.3c08852. PMID: 37857329 Wen X, Zhang M, Duan Z, Suo Y, Lu W, Jin R, Mu B, Li K, Zhang X, Meng L, Hong Y, Wang X, Hu H, Zhu J, Song W, Shen A, Lu X. Discovery, SAR Study of GST Inhibitors from a Novel Quinazolin-4(1H)-one Focused DNA-Encoded Library. J Med Chem. 2023，doi: 10.1021/acs.jmedchem.2c02129. PMID: 37552553. Mengnisa Seydimemet, Yixuan Yang, Yuhan Lv, Jiaxiang Liu, Ziqin Yan, Yujun Zhao*, Xuan Wang*, and Xiaojie Lu* Design, Construction, and Screening of Diversified Pyrimidine-Focused DNA-Encoded Libraries，ACS Medicinal Chemistry Letters， 2023，DOI: 10.1021/acsmedchemlett.3c00205. PMID: 37583819 Chang Shen, Peijia Xu, Changfa Zhang, Zhaoming Su, Bin Shan, Rui Li, Qibang Sui, Keke Zhang, Zhengyang Chen, Jingyi Zhou, Xiaojie Lu, Kaixian Chen, Mingyue Zheng, Sulin Zhang*, and Hui Hou*Structure–Activity Relationship Study of 1H-Pyrrole-3-carbonitrile Derivatives as STING Receptor Agonists, ACS Med. Chem. Lett. 2023, doi: 10.1021/acsmedchemlett.3c00208. PMID: 37583816 He S, Li L*, Jin R, Lu X. * Biological Function of Pin1 in Vivo and Its Inhibitors for Preclinical Study: Early Development, Current Strategies, and Future Directions. J Med Chem. 2023 Jul 12. doi: 10.1021/acs.jmedchem.3c00390. PMID: 37438908 Chen L, Fan Z, Chang J, Yang R, Hou H, Guo H, Zhang Y, Yang T, Zhou C, Sui Q, Chen Z, Zheng C, Hao X, Zhang K, Cui R, Zhang Z, Ma H, Ding Y, Zhang N, Lu X, Luo X, Jiang H, Zhang S, Zheng M. Sequence-based drug design as a concept in computational drug design. Nat Commun. 2023 Jul 14;14(1):4217. doi:10.1038/s41467-023-39856-w. PMID: 37452028; PMCID: PMC10349078. Bao Y, Xing M, Matthew N, Chen X, Wang X*, Lu X*. Macrocyclizing DNA-Linked Peptides via Three-Component Cyclization and Photoinduced Chemistry. Org Lett. 2023 Jun 29. doi: 10.1021/acs.orglett.3c01817. Epub ahead of print. PMID:37382883. Zhao Q, Bao Y, Niu D*, Wang X*, Lu X. * The Development of DNA-Compatible S-Glycosyl Transformations. Org Lett. 2023 Jun 26. doi:10.1021/acs.orglett.3c01799. Epub ahead of print. PMID: 37358352. Zhang Z, Wang G, Li R, Ni L, Zhang R, Cheng K, Ren Q, Kong X, Ni S, Tong X, Luo L, Wang D, Lu X, Zheng M, Li X. Tora3D: an autoregressive torsion angle prediction model for molecular 3D conformation generation. J Cheminform. 2023 Jun 7;15(1):57. doi: 10.1186/s13321-023-00726-8. PMID: 37287071; PMCID: PMC10245430. Guo AD, Yan KN, Hu H, Zhai L, Hu TF, Su H, Chi Y, Zha J, Xu Y, Zhao D, Lu X, Xu YJ, Zhang J, Tan M, Chen XH. Spatiotemporal and global profiling of DNA-protein interactions enables discovery of low-affinity transcription factors. Nat Chem. 2023 Jun;15(6):803-814. doi: 10.1038/s41557-023-01196-z. Epub 2023 Apr27. PMID: 37106095. Ling X, Liu S, Yang Y, Dong Q, Marcaurelle LA, Huang W, Ding Y*, Wang X*, Lu X*. Modular Click Assembly DNA-Encoded Glycoconjugate Libraries with on-DNA Functional Group Transformations. Bioconjug Chem. 2023 Mar 24. doi:10.1021/acs.bioconjchem.3c00068. Epub ahead of print. PMID: 36961996. Wen X, Wu X, Jin R, Lu X*. Privileged heterocycles for DNA-encoded library design and hit-to-lead optimization. Eur J Med Chem. 2023 Feb 15;248:115079.doi: 10.1016/j.ejmech.2022.115079. Epub 2023 Jan 14. PMID: 36669370. Suo Y, Xu M, Sun M, Lu W, Wang X*, Lu X*. Ruthenium-Mediated [2 + 2 + 2] Cyclization: A Route to Forge Indane and Isoindoline Core and Its Application in DNA-Encoded Library Technology. Org Lett. 2022 Dec 16;24(49):9092-9096. doi:10.1021/acs.orglett.2c03759. Epub 2022 Dec 7. PMID: 36475704. Zhang Y, Xia S, Shi WX, Lin B, Su XC, Lu W, Wu X, Wang X, Lu X, Yan M, Zhang XJ. Radical C-H Sulfonation of Arenes: Its Applications on Bioactive and DNA-Encoded Molecules. Org Lett. 2022 Nov 4;24(43):7961-7966. doi:10.1021/acs.orglett.2c03077. Epub 2022 Oct 24. PMID: 36278920. Li L, Su M, Lu W, Song H, Liu J, Wen X, Suo Y, Qi J, Luo X, Zhou YB, Liao XH*, Li J*, Lu X*. Triazine-Based Covalent DNA-Encoded Libraries for Discovery of Covalent Inhibitors of Target Proteins. ACS Med Chem Lett. 2022 Aug15;13(10):1574-1581. doi: 10.1021/acsmedchemlett.2c00127. PMID: 36262386; PMCID:PMC9575176. Wu X, Chen Y, Lu W, Jin R, Lu X*. Quantitative Validation and Application of the Photo-Cross-Linking Selection for Double-Stranded DNA-Encoded Libraries. Bioconjug Chem. 2022 Oct 19;33(10):1818-1824. doi:10.1021/acs.bioconjchem.2c00421. Epub 2022 Oct 5. PMID: 36197318. Wang X, Lu X. Ruthenium-Promoted On-DNA C-H Activation Reaction. Methods Mol Biol. 2022; 2541:63-66. doi: 10.1007/978-1-0716-2545-3_10. PMID: 36083545. Wang X, Lu X. Palladium-Promoted On-DNA Heck Reactions. Methods Mol Biol. 2022; 2541:55-61. doi: 10.1007/978-1-0716-2545-3_9. PMID: 36083544. Lu X, Wang X. On-DNA Pd and Cu-Promoted C-N Cross-Coupling Reactions. Methods Mol Biol. 2022; 2541:49-54. doi: 10.1007/978-1-0716-2545-3_8. PMID:36083543. Liu W, Bai X, Song L, Wang X*, Lu X*. Constructing Head-to-Tail Cyclic Peptide DNA-Encoded Libraries Using Two-Directional Synthesis Strategy. Bioconjug Chem. 2022 Apr 20;33(4):560-565. doi: 10.1021/acs.bioconjchem.2c00078. Epub 2022 Mar 11. PMID: 35274526. Qi J, Liu S, Seydimemet M, Wang X*, Lu X*. A General Set of DNA-Compatible Reactions for Preparing DNA-Tagged Multisubstituted Pyrroles. Bioconjug Chem.2021 Nov 17;32(11):2290-2294. doi: 10.1021/acs.bioconjchem.1c00427. Epub 2021 Oct 26. PMID: 34699185. Lin B, Lu W, Chen ZY, Zhang Y, Duan YZ, Lu X, Yan M, Zhang XJ. Enhancing the Potential of Miniature-Scale DNA-Compatible Radical Reactions via an Electron Donor-Acceptor Complex and a Reversible Adsorption to Solid Support Strategy. Org Lett. 2021 Oct 1;23(19):7381-7385. doi: 10.1021/acs.orglett.1c02562. Epub 2021 Sep 21. PMID: 34546064. Yang P, Wang X, Li B, Yang Y, Yue J, Suo Y, Tong H, He G, Lu X*, Chen G*. Streamlined construction of peptide macrocycles via palladium-catalyzed intramolecular S-arylation in solution and on DNA. Chem Sci. 2021 Mar 11;12(16):5804-5810. doi: 10.1039/d1sc00789k. PMID: 34168804; PMCID: PMC8179660. Wang X, Liu J, Yan Z, Liu X, Liu S, Suo Y, Lu W, Yue J, Chen K, Jiang H, Zhao Y*, Zheng M*, Dai D*, Lu X*. Diversified strategy for the synthesis of DNA-encoded oxindole libraries. Chem Sci. 2021 Jan 4;12(8):2841-2847. doi:10.1039/d0sc06696f. PMID: 34164048; PMCID: PMC8179416. Shan J, Ling X, Liu J, Wang X*, Lu X*. DNA-encoded CH functionality via photoredox-mediated hydrogen atom transformation catalysis. Bioorg Med Chem. 2021 Jul 15;42:116234. doi: 10.1016/j.bmc.2021.116234. Epub 2021 May 28. PMID: 34098191. Ling X, Lu W, Miao L, Marcaurelle LA, Wang X*, Ding Y*, Lu X*. Divergent On-DNA Transformations from DNA-Linked Piperidones. J Org Chem. 2022 Feb 18;87(4):1971-1976. doi: 10.1021/acs.joc.1c00670. Epub 2021 May 7. PMID:33960188. Liu C, Zhou F, Yan Z, Shen L, Zhang X, He F, Wang H, Lu X, Yu K, Zhao Y, Zhu D. Discovery of a novel, potent and selective small-molecule inhibitor of PD-1/PD-L1 interaction with robust in vivo anti-tumour efficacy. Br J Pharmacol. 2021 Jul;178(13):2651-2670. doi: 10.1111/bph.15457. Epub 2021 May 4. PMID:33768523. Liu S, Qi J, Lu W, Wang X*, Lu X*. Synthetic Studies toward DNA-Encoded Heterocycles Based on the On-DNA Formation of , -Unsaturated Ketones. Org Lett.2021 Feb 5;23(3):908-913. doi: 10.1021/acs.orglett.0c04118. Epub 2021 Jan 14. Erratum in: Org Lett. 2022 Jul 1;24(25):4716. PMID: 33444029. Wen X, Duan Z, Liu J, Lu W, Lu X*. On-DNA Cross-Dehydrogenative Coupling Reaction toward the Synthesis of Focused DNA-Encoded Tetrahydroisoquinoline Libraries. Org Lett. 2020 Aug 7; 22(15):5721-5725. doi: 10.1021/acs.orglett.0c01565. Epub 2020 Jul 9. PMID: 32644810. Li K, Liu X, Liu S, An Y, Shen Y, Sun Q, Shi X, Su W, Cui W, Duan Z, Kuai L, Yang H, Satz AL, Chen K, Jiang H, Zheng M*, Peng X*, Lu X*. Solution-Phase DNA-Compatible Pictet-Spengler Reaction Aided by Machine Learning Building Block Filtering. iScience. 2020 Jun 26;23(6):101142. doi: 10.1016/j.isci.2020.101142. Epub 2020 May 7. PMID: 32446221; PMCID: PMC7243192. Qu Y, Liu S, Wen H, Xu Y, An Y, Li K, Ni M, Shen Y, Shi X, Su W, Cui W, Kuai L, Satz AL, Yang H, Lu X*, Peng X*. Palladium-mediated Suzuki-Miyaura Cross-Coupling Reaction of Potassium Boc-protected aminomethyltrifluoroborate with DNA-Conjugated aryl bromides for DNA-Encoded chemical library synthesis. Biochem Biophys Res Commun. 2020 Dec 3;533(2):209-214. doi: 10.1016/j.bbrc.2020.04.027. Epub 2020 May 4. PMID: 32376009. Wu W, Sun Z, Wang X, Lu X, Dai D. Construction of Thiazole-Fused Dihydropyrans via Formal [4 + 2] Cycloaddition Reaction on DNA. Org Lett. 2020 Apr 17;22(8):3239-3244. doi: 10.1021/acs.orglett.0c01016. Epub 2020 Apr 3. PMID: 32243186. Wang DY, Wen X, Xiong CD, Zhao JN, Ding CY, Meng Q, Zhou H, Wang C, Uchiyama M, Lu XJ*, Zhang A*. Non-transition Metal-Mediated Diverse Aryl-Heteroatom Bond Formation of Arylammonium Salts. iScience. 2019 May 31;15:307-315. doi: 10.1016/j.isci.2019.04.038. Epub 2019 May 3. PMID: 31102996; PMCID: PMC6525302. Wang X, Sun H, Liu J, Zhong W, Zhang M, Zhou H, Dai D*, Lu X*. Palladium-Promoted DNA-Compatible Heck Reaction. Org Lett. 2019 Feb 1;21(3):719-723. doi:10.1021/acs.orglett.8b03926. Epub 2019 Jan 24. PMID: 30676761.