(#Co-first author &*Co-corresponding author)
2024
26. Velez, J.; Dale, B.; Park, K. S.; Kaniskan, H. U.; Yu, X.*; Jin, J.* “Discovery of a novel, highly potent EZH2 PROTAC degrader for targeting non-canonical oncogenic functions of EZH2” European Journal of Medicinal Chemistry, 2024, 267, 116154.
2023
25. 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.
24. 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.
23. 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
Pior to 2022
22.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.
21.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.
20.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.
19.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)
18.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.
17.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.
16.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.
15.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.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.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.
12.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.
11.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.
10.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.
9.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.
8.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.
7.Yu, X.; Sun, D.* “Macrocyclic Drugs and Synthetic Methodologies toward Macrocycles” Molecules, 2013, 18, 6230-6268.
6.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 NFB inhibitiors” Organic & Biomolecular Chemistry, 2012, 10, 8835-8847.
5.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.
4.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.
3.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.
2.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.
1.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.
