2006.09 – 2011.07 中国科杏悦上海有机化学研究所🧔🏿♂️，有机化学👱🏿♂️🤍， 博士
2002.09 – 2006.07 安徽大学➙，应用化学， 学士
2022.10 – 至今 杏悦 青年研究员，博士生导师
2021.01 – 2022.08 西奈山伊坎医杏悦 讲师
2017.01 – 2020.12 西奈山伊坎医杏悦 博士后
2013.07 – 2014.07 普渡大学 博士后
2011.08 – 2013.07 夏威夷大学 博士后
1. 国家重点研发计划“前沿生物技术”重点专项🧈🪣，2023YFC3404103 (2023.11-2028,11, 100万，参与)
2. 国家自然科学基金青年项目，22307021（2024.01-2026. 12，30万🍧，主持）
3. 国家海外高层次人才引进青年项目（2023.01-2025. 12，200万，主持）
4. 杏悦娱乐引进人才科研基金（2022.10-2025.10, 300万👎🏽，主持）
1.基于蛋白质降解技术（PROTAC）发展创新型肿瘤和其它重大疾病靶蛋白降解剂
2.新型E3泛素连接酶配体的开发与应用
3.具有高生物活性和选择性的GPCR小分子激动剂🤱、抑制剂以及变构调节剂的合成与化学生物学研究
通过多学科包括有机合成化学🛞、药物化学🧍🏻♂️、化学生物学、蛋白质组学、结构生物学以及基因组学等交叉合作🧑🏿🚀，利用蛋白裂解靶向嵌合体（PROTAC)技术🧗🏻♀️，针对易发生“耐药突变”的蛋白激酶、以及易于其它致癌蛋白结合且小分子药物难以靶向的表观遗传学等肿瘤靶标，发展多类高选择性和高活性的创新型PROTAC小分子降解剂，并利用降解剂作为化学工具，揭示这些靶标在调控细胞功能信号通路中的新机制，以及与其它致癌蛋白相互作用诱导肿瘤发生和发展的非传统致癌功能👩🏼🏫。迄今，在国际学术刊物发表科研论文共30余篇🫡，其中以第一作者和通讯作者（含共同）在Sci. Transl. Med.👵🏿，Cancer Discov., Nat. Cell Biol.🧔🏻♂️，J. Am. Chem. Soc., J. Med. Chem.🛌🏼，Oncogene等核心SCI期刊发表学科高影响力研究论文20余篇，其中多篇被国际专业科学杂志和网站热点推送。获授权国际专利3项🧘🏻♀️，其中一项专利已转化💷。
(#Co-first author & *Co-corresponding author)
2023
1. Yu, X.#; Li, D. #; Kottur, J. #; Kim, H.S.; Herring, L.; Yu, Y.; Xie, L.; Hu, X.; Chen, X.; Cai, L.; Liu, J.; Aggarwal, A. K.; Wang, G. G.*; Jin, J.* “Discovery of Potent and Selective WDR5 PROTACs as Potential Therapeutic for Pancreatic Cancer” Journal of Medicinal Chemistry, 2023, 66, 16168-16186.
2. Mabir, M.; Yu, X.; Kaniskan, H. U.; Jin, J.* “Chemically Induced Degradation of Epigenetic Targets” Chemical Society Review, 2023, 52(13), 4313-4342.
3. Chen, S.; Chen, Z.; Lu, L.; Zhao, Y.; Zhou, R.; Xie, Q.; Shu, Y.; Lin, J.; Yu, X.*; Wang, Y.* “Discovery of novel BTK PROTACs with improved metabolic stability via linker rigidification strategy” European Journal of Medicinal Chemistry, 2023, 255，115403
4. Yu, X.#,*; Wang, J.#; Gong, W.; Ma, A.; Shen, Y.; Zhang, C.; Liu, X.; Cai, L.; Liu, J.; Wang, G. G.*; Jin, J.* “Dissecting and Targeting Noncanonical Functions of EZH2 in Multiple Myeloma via an EZH2 Degrader” Oncogene, 2023, 42, 994-1009.
Prior to 2022
5. Yu, X.#; Xu, J. #; Cahuzac, K. M.; Xie, L.; Shen, Y.; Liu, J. *; Parsons, R.*; Jin, J.* “Novel Allosteric Inhibitor-derived AKT Proteolysis Targeting Chimeras (PROTACs) Enable Potent and Selective AKT Degradation in KRAS/BRAF Mutant Cells” Journal of Medicinal Chemistry, 2022, 65, 14237-14260.
6. Liu, J.#; Yu, X. #; Chen, H.; Kaniskan, H. U.; Xie, L.; Chen, X.; Jin, J.*; Wei, W.* “TF-DUBTACs Stabilize Tumor Suppressor Transcription Factors” Journal of American Chemical Society, 2022, 144, 12934-12941.
7. Dale, B. #; Anderson, C. #; Park, K. S.; Kaniskan, H. U.; Ma, A.; Shen, Y.; Zhang, C.; Xie, L.; Chen, X.; Yu, X.*; Jin, J.* “Targeting Triple-negative Breast Cancer by a Novel Proteolysis Targeting Chimera (PROTAC) Degrader of Enhancer of Zeste Homolog 2 (EZH2)” ACS Pharmacology & Translational Science, 2022, 5, 491-507.
8. Yu, X. #; Cheng, M. #; Lu, K.; Shen, Y.; Zhong, Y.; Liu, J.*; Xiong, Y.*; Jin, J.* “Exploring Degradation of Mutant and Wild-Type Epidermal Growth Factor Receptors Induced by Proteolysis-Targeting Chimeras” Journal of Medicinal Chemistry, 2022, 65, 8416-8443.
9. Li, D. #; Yu, X.#; Kottur, J.; Gong, W.; Zhang, Z.; Storey, A. J.; Tsai, Y.-H.; Uryu, H.; Shen, Y.; Byrum, S. D.; Edmondson, R. D.; Mackintosh, S. G.; Cai, L.; Liu, Z.; Aggarwal, A. K.; Tackett, A. J.; Liu, J.; Jin, J. *; Wang, G. G.* “Discovery of a dual WDR5 and Ikaros PROTAC degrader as an anti-cancer therapeutic” Oncogene, 2022, 41, 3328-3340.
10. Yu, X.#; Xu, J. #; Shen, Y.; Cahuzac, K. M.; Park, K. S.; Dale, B.; Liu, J. *; Parsons, R.*; Jin, J.* “Discovery of Potent, Selective and In Vivo Efficacious AKT Kinase Protein Degraders via Structure-activity Relationship Studies” Journal of Medicinal Chemistry, 2022, 65, 3644-3666.
11. Wang, J. #; Yu, X.#; Gong, W.; Liu, X.; Park, K. S.; Ma, A.; Tsai, Y.-H.; Shen, Y.; Onikubo, T.; Pi, W.-C.; Allison, D. F.; Liu, J.; Chen, W.-Y.; Cai, L.; Roeder, R. G.; Jin, J. *; Wang, G. G.* “EZH2 non-canonically binds cMyc and p300 through a cryptic transactivation domain to mediate gene activation and promote oncogenesis” Nature Cell Biology, 2022, 24, 383-399.
12. Yu, X.#; Li, D. #; Kottur, J. #; Shen, Y.; Kim, H.S.; Park, K. S.; Tsai, Y.-H.; Gong, W.; Wang, J.; Suzuki, K.; Parker, J.; Herring, L.; Kaniskan, H. U.; Cai, L.; Jain, R.; Liu, J.; Aggarwal, A. K.; Wang, G. G.*; Jin, J.* “A selective WDR5 degrader inhibits acute myeloid leukemia in patient-derived mouse models” Science Translational Medicine, 2021, 13, eabj1578.
13. Yu, X.#; Xu, J. #; Xie, L.; Wang, L.; Shen, Y.; Cahuzac, K. M.; Chen, X.; Liu, J. *; Parsons, R.*; Jin, J.* “Design, Synthesis and Evaluation of Potent, Selective and Bioavailable AKT Kinase Degraders” Journal of Medicinal Chemistry, 2021, 64,18054-18081.
14. Xu, J. #; Yu, X.#; Martin, T. C.; Bansal, A.; Cheung, K.; Lubin, A.; Stratikopoulos, E.; Cahuzac, K. M.; Wang, L.; Xie, L.; Zhou, R.; Shen, Y.; Wu, X.; Shen, Y.; Qiao, R.; Poulikakos, P.; Chen, X.; Liu, J.; Jin, J.*; Parsons, R.* “AKT degradation selectively inhibits the growth of PI3K/PTEN pathway mutant cancers with wild-type KRAS and BRAF by destabilizing Aurora kinase B” Cancer Discovery, 2021, 11, 3064-3089.
15. Cheng, M. #; Yu, X. #,*; Lu, K.; Xie, L.; Liu, J.; Wang, L.; Meng, F.; Han, X.; Chen, X.; Liu, J.; Xiong, Y.*; Jin, J.* “Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-molecule Degraders” Journal of Medicinal Chemistry, 2020, 63, 1216-1232.
16. Yu, X.; Huang, X. P.*; Kenakin, T. P.; Slocum, S. T.; Chen, X.; Martini, M. L.; Liu, J.*; Jin, J.* “Design, Synthesis and Characterization of Ogerin-Based Positive Allosteric Modulators for G Protein-Coupled Receptor 68 (GPR68)” Journal of Medicinal Chemistry, 2019, 62, 7557-7574.
17. Yu, X. #; Zhang, M. #; Annamalai, T.; Bansod, P.; Narula, G.; Tse-Dinh Y.-C.; Sun, D.* “Synthesis, evaluation, and CoMFA study of fluoroquinophenoxazine derivatives as bacterial topoisomerase IA inhibitors” European Journal of Medicinal Chemistry, 2017, 125, 515-527.
18. Ghosh, A. K.*; Yu, X.; Osswald, H. L.; Agniswamy, J.; Wang, Y. F.; Amano, M.; Weber, I. T.; Mitsuya, H. “Structure-based Design of Potent HIV-1 Protease inhibitors with Modified P1-Biphenyl Ligands: Synthesis, Biological Evaluation, and Enzyme-inhibitor X-ray Structural studies” Journal of Medicinal Chemistry, 2015, 58, 5334-5343.
19. Yu, X.; Sun, D.* “Macrocyclic Drugs and Synthetic Methodologies toward Macrocycles” Molecules, 2013, 18, 6230-6268.
20. Yu, X.; Park, E. -J.; Kondratyuk, T. P.; Pezzuto, J. M.; Sun, D.* “Synthesis of 2-arylindole derivatives and evaluation as nitric oxide synthase and NFkB inhibitiors” Organic & Biomolecular Chemistry, 2012, 10, 8835-8847.
21. Yu, X.; Lu, X.* “Efficient Synthesis of 9-Tosylaminofluorene Derivatives by Boron Trifluoride Etherate-Catalyzed Aza-Friedel-Crafts Reaction of in situ Generated N-Tosylbenzaldimines” Advanced Synthesis & Catalysis, 2011, 353, 569-574.
22. Yu, X.; Lu, X.* “Cationic Palladium Complex-Catalyzed Diastereoselective Tandem Annulation of 2-Iminoarylboronic Acids with Substituted Alkynes: Enantioselective Synthesis of Aminoindene Derivatives by Double Asymmetric Induction” Advanced Synthesis & Catalysis, 2011, 353, 2805-2813.
23. Yu, X.; Lu, X.* “Facile Cu(OTf)2-catalyzed preparation of 9-Tosylaminofluorene derivatives from o-arylated N-Tosylbenzaldimines” Tetrahedron Letters, 2011, 52, 2076-2079.
24. Yu, X.; Lu, X.* “Cationic Palladium-Catalyzed [5+2] Annulation of 2-Acylmethoxyarylboronic Acids and Allenoates: Synthesis of 1-Benzoxepine Derivatives” Journal of Organic Chemistry, 2011, 76, 6350-6355.
25. Yu, X.; Lu, X.* “Cationic Palladium Complex Catalyzed Diastereo- and Enantioselective Tandem Annulation of 2-Formylarylboronic Acids with Allenoates” Organic Letters, 2009, 11, 4366-4369.
专利：
1. Jin, J.; Liu, J.; Parsons, Ramon E.; Xu, J.; Yu, X. Serine Threonine Kinase (AKT) Degradation/disruption compounds and methods of use. PCT Int. Appl. (2019), WO2019173516A1, 20190912.
2. Jin, J.; Wang, G.; Liu, J.; Yu, X.; Li, D. WD40 Repeat Domain Protein (WDR5) Degradation/disruption compounds and methods of use. PCT Int. Appl. (2019), WO2019246570A1, 20191226.
3. Jin, J.; Filizola, M.; Aggarwal, A.; Parekh, S.; Kapoor, A.; Jatiani, S.; Kaniskan, H.; Hu, J.; Shen, Y.; Meng, F.; Qin, L.; Han, Y.; Yu, X.; Zhang, C.; Kumar, P.; Jain, R.; Lee, C. Sox11 Inhibitors for treating mantle cell Lymphoma. PCT Int. Appl. (2021), WO2021257544A1, 20211223.
