Y
Yimin Qian
Researcher at Yale University
Publications - 43
Citations - 3203
Yimin Qian is an academic researcher from Yale University. The author has contributed to research in topics: Ubiquitin ligase & Target protein. The author has an hindex of 21, co-authored 43 publications receiving 2342 citations.
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Journal ArticleDOI
Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4
Jing Lu,Yimin Qian,Martha Altieri,Hanqing Dong,Jing Wang,Kanak Raina,John Hines,James D. Winkler,Andrew P. Crew,Kevin Coleman,Craig M. Crews +10 more
TL;DR: ARV-825 is designed, a hetero-bifunctional PROTAC (Proteolysis Targeting Chimera) that recruits BRD4 to the E3 ubiquitin ligase cereblon, leading to fast, efficient, and prolonged degradation ofBRD4 in all BL cell lines tested.
Journal ArticleDOI
PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer.
Kanak Raina,Jing Lu,Yimin Qian,Martha Altieri,Deborah M. Gordon,Ann Marie Rossi,Jing Wang,Xin Chen,Hanqing Dong,Kam W. Siu,James D. Winkler,Andrew P. Crew,Craig M. Crews,Kevin Coleman +13 more
TL;DR: This study proves that ARV-771, a small-molecule pan-BET degrader based on proteolysis-targeting chimera (PROTAC) technology, demonstrates dramatically improved efficacy in cellular models of CRPC as compared with BET inhibition.
Journal ArticleDOI
The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study
George M. Burslem,Blake E. Smith,Ashton C. Lai,Saul Jaime-Figueroa,Daniel McQuaid,Daniel P. Bondeson,Momar Toure,Hanqing Dong,Yimin Qian,Jing Wang,Andrew P. Crew,John Hines,Craig M. Crews +12 more
TL;DR: The ability to target receptor tyrosine kinases for degradation using the PROTAC technology is demonstrated and the advantages of this degradation-based approach are outlined.
Journal ArticleDOI
MDM2-Recruiting PROTAC Offers Superior, Synergistic Antiproliferative Activity via Simultaneous Degradation of BRD4 and Stabilization of p53.
TL;DR: This is the first report of a PROTAC in which the E3 ligase ligand and targeting warhead combine to exert a synergistic antiproliferative effect, and presents the first BRD4-targeting MDM2-based PROTAC that possesses potent, distinct, and synergistic biological activities associated with both ends of this heterobifunctional molecule.
Journal ArticleDOI
Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1
Andrew P. Crew,Kanak Raina,Hanqing Dong,Yimin Qian,Jing Wang,Dominico Vigil,Yevgeniy V. Serebrenik,Brian D. Hamman,Alicia Morgan,Caterina Ferraro,Kam W. Siu,Taavi K. Neklesa,James D. Winkler,Kevin Coleman,Craig M. Crews +14 more
TL;DR: This article describes a broadly applicable process for identifying degrader hits based on the serine/threonine kinase TANK-binding kinase 1 (TBK1) and has generalized the key structural elements associated with degradation activities.