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成果及论文

(#Co-first author &*Co-corresponding author)


1.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.


2.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. 


3.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. 


4.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)


5.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, 24, 3328-3340. 


6.Wang, J. #; Yu, X.#; Gong, W.; Liu, X.; Park, K. S.; Ma, A.; Tsai, Y.-H.; Shen, Y.; Onikubo, T.; Allison, D. F.; Liu, J.; Chen, W. Y.; Cai, L.; Roeder, R. G.; Jin, J. *; Wang, G. G.* “EZH2 noncanonically binds cMyc and p300 through a cryptic transactivation domain to mediate gene activation and promote oncogenesis” Nature Cell Biology, 2022, 24,384-399. 


7.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. 


8.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.  


9.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. 


10.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.; Yao, S.; 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. 


11.Cheng, M.#; Yu, X. #,*; Lu, K.; Xie, L.; 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. 


12.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. 


13.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. 


14.Prior, A. M.#; Yu, X.#; Park, E.-J.; Kondratyuk, T. P.; Lin, Y.; Pezzuto, J. M; Sun, D.* “Structure-activity relationship and docking studies of synthetic 2-arylindole derivatives determined with aromatase and quinone reductase 1” Bioorganic & Medicinal Chemistry Letter, 2017, 27, 5393-5399.  


15.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. 


16.Yu, X.; Sun, D.* “Macrocyclic Drugs and Synthetic Methodologies toward Macrocycles” Molecules, 2013, 18, 6230-6268.


17.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 NFB inhibitiors” Organic & Biomolecular Chemistry, 2012, 10, 8835-8847. 


18.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. 


19.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. 


20.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. 


21.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. 


22.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. 

专利申请

1.专利名:Sox11 Inhibitors for treating mantle cell Lymphoma,申请人: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.专利申请号:PCT Int. Appl. (2021), WO2021257544A1, 授权日期:2021-12-23.


2.专利名:WD40 Repeat Domain Protein (WDR5) Degradation/disruption compounds and methods of use,申请人:Jin, J.; Wang, G.; Liu, J.; Yu, X.; Li, D. 专利申请号:PCT Int. Appl. (2019), WO2019246570A1, 授权日期:2019-12-26.


3.专利名:Serine Threonine Kinase (AKT) Degradation/disruption compounds and methods of use,申请人:Jin, J.; Liu, J.; Parsons, Ramon E.; Xu, J.; Yu, X. 专利申请号:PCT Int. Appl. (2019), WO2019173516A1, 授权日期:2019-09-12.