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Xufen Yu
Pharmaceutical Sciences
Fudan University
Shanghai
Language: Chinese, English
Protac
Tumor
Disease
Target Protein
Degraders
E3 Ubiquitin Ligase
Ligands
Gpcr
Agonists
Inhibitors
Areas of Focus
- Development of innovative tumor and other major disease target protein degraders based on PROTAC technology
- Development and application of novel E3 ubiquitin ligase ligands
- Synthesis and chemical biology research of GPCR small molecule agonists, inhibitors, and allosteric modulators with high bioactivity and selectivity
Work Experience
- 2022.10 – Present - Fudan University - Junior Researcher, Doctoral Supervisor
- 2021.01 – 2022.08 - Icahn School of Medicine at Mount Sinai - Lecturer
- 2017.01 – 2020.12 - Icahn School of Medicine at Mount Sinai - Postdoctoral Researcher
- 2013.07 – 2014.07 - Purdue University - Postdoctoral Researcher
- 2011.08 – 2013.07 - University of Hawaii - Postdoctoral Researcher
Academic Background & Achievements
- 2006.09 – 2011.07 Ph.D. in Organic Chemistry: Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences
- 2002.09 – 2006.07 Bachelor's in Applied Chemistry: Anhui University
Publications
- Discovery of Potent and Selective WDR5 PROTACs as Potential Therapeutic for Pancreatic Cancer, 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., 2023
- Chemically Induced Degradation of Epigenetic Targets, Mabir, M.; Yu, X.; Kaniskan, H. U.; Jin, J., 2023
- Discovery of novel BTK PROTACs with improved metabolic stability via linker rigidification strategy, Chen, S.; Chen, Z.; Lu, L.; Zhao, Y.; Zhou, R.; Xie, Q.; Shu, Y.; Lin, J.; Yu, X.; Wang, Y., 2023
- Dissecting and Targeting Noncanonical Functions of EZH2 in Multiple Myeloma via an EZH2 Degrader, Yu, X.; Wang, J.; Gong, W.; Ma, A.; Shen, Y.; Zhang, C.; Liu, X.; Cai, L.; Liu, J.; Wang, G. G.; Jin, J., 2023
- Novel Allosteric Inhibitor-derived AKT Proteolysis Targeting Chimeras (PROTACs) Enable Potent and Selective AKT Degradation in KRAS/BRAF Mutant Cells, Yu, X.; Xu, J.; Cahuzac, K. M.; Xie, L.; Shen, Y.; Liu, J.; Parsons, R.; Jin, J., 2022
- TF-DUBTACs Stabilize Tumor Suppressor Transcription Factors, Liu, J.; Yu, X.; Chen, H.; Kaniskan, H. U.; Xie, L.; Chen, X.; Jin, J.; Wei, W., 2022
- Targeting Triple-negative Breast Cancer by a Novel Proteolysis Targeting Chimera (PROTAC) Degrader of Enhancer of Zeste Homolog 2 (EZH2), Dale, B.; Anderson, C.; Park, K. S.; Kaniskan, H. U.; Ma, A.; Shen, Y.; Zhang, C.; Xie, L.; Chen, X.; Yu, X.; Jin, J., 2022
- Exploring Degradation of Mutant and Wild-Type Epidermal Growth Factor Receptors Induced by Proteolysis-Targeting Chimeras, Yu, X.; Cheng, M.; Lu, K.; Shen, Y.; Zhong, Y.; Liu, J.; Xiong, Y.; Jin, J., 2022
- Discovery of a dual WDR5 and Ikaros PROTAC degrader as an anti-cancer therapeutic, 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., 2022
- Discovery of Potent, Selective and In Vivo Efficacious AKT Kinase Protein Degraders via Structure-activity Relationship Studies, Yu, X.; Xu, J.; Shen, Y.; Cahuzac, K. M.; Park, K. S.; Dale, B.; Liu, J.; Parsons, R.; Jin, J., 2022
- EZH2 non-canonically binds cMyc and p300 through a cryptic transactivation domain to mediate gene activation and promote oncogenesis, 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., 2022
- A selective WDR5 degrader inhibits acute myeloid leukemia in patient-derived mouse models, 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., 2021
- Design, Synthesis and Evaluation of Potent, Selective and Bioavailable AKT Kinase Degraders, Yu, X.; Xu, J.; Xie, L.; Wang, L.; Shen, Y.; Cahuzac, K. M.; Chen, X.; Liu, J.; Parsons, R.; Jin, J., 2021
- AKT degradation selectively inhibits the growth of PI3K/PTEN pathway mutant cancers with wild-type KRAS and BRAF by destabilizing Aurora kinase B, 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., 2021
- Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-molecule Degraders, Cheng, M.; Yu, X.; Lu, K.; Xie, L.; Liu, J.; Wang, L.; Meng, F.; Han, X.; Chen, X.; Liu, J.; Xiong, Y.; Jin, J., 2020
- Design, Synthesis and Characterization of Ogerin-Based Positive Allosteric Modulators for G Protein-Coupled Receptor 68 (GPR68), Yu, X.; Huang, X. P.; Kenakin, T. P.; Slocum, S. T.; Chen, X.; Martini, M. L.; Liu, J.; Jin, J., 2019
- Synthesis, evaluation, and CoMFA study of fluoroquinophenoxazine derivatives as bacterial topoisomerase IA inhibitors, Yu, X.; Zhang, M.; Annamalai, T.; Bansod, P.; Narula, G.; Tse-Dinh Y.-C.; Sun, D., 2017
- Structure-based Design of Potent HIV-1 Protease inhibitors with Modified P1-Biphenyl Ligands: Synthesis, Biological Evaluation, and Enzyme-inhibitor X-ray Structural studies, Ghosh, A. K.; Yu, X.; Osswald, H. L.; Agniswamy, J.; Wang, Y. F.; Amano, M.; Weber, I. T.; Mitsuya, H., 2015
- Macrocyclic Drugs and Synthetic Methodologies toward Macrocycles, Yu, X.; Sun, D., 2013
- Synthesis of 2-arylindole derivatives and evaluation as nitric oxide synthase and NFkB inhibitors, Yu, X.; Park, E. -J.; Kondratyuk, T. P.; Pezzuto, J. M.; Sun, D., 2012
- Efficient Synthesis of 9-Tosylaminofluorene Derivatives by Boron Trifluoride Etherate-Catalyzed Aza-Friedel-Crafts Reaction of in situ Generated N-Tosylbenzaldimines, Yu, X.; Lu, X., 2011
- Cationic Palladium Complex-Catalyzed Diastereoselective Tandem Annulation of 2-Iminoarylboronic Acids with Substituted Alkynes: Enantioselective Synthesis of Aminoindene Derivatives by Double Asymmetric Induction, Yu, X.; Lu, X., 2011
- Facile Cu(OTf)2-catalyzed preparation of 9-Tosylaminofluorene derivatives from o-arylated N-Tosylbenzaldimines, Yu, X.; Lu, X., 2011
- Cationic Palladium-Catalyzed [5+2] Annulation of 2-Acylmethoxyarylboronic Acids and Allenoates: Synthesis of 1-Benzoxepine Derivatives, Yu, X.; Lu, X., 2011
- Cationic Palladium Complex Catalyzed Diastereo- and Enantioselective Tandem Annulation of 2-Formylarylboronic Acids with Allenoates, Yu, X.; Lu, X., 2009
