Z
Zhaomin Liu
Researcher at University of Michigan
Publications - 6
Citations - 706
Zhaomin Liu is an academic researcher from University of Michigan. The author has contributed to research in topics: Protein degradation & Proteolysis targeting chimera. The author has an hindex of 5, co-authored 6 publications receiving 343 citations.
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Journal ArticleDOI
A Potent and Selective Small-Molecule Degrader of STAT3 Achieves Complete Tumor Regression In Vivo
Longchuan Bai,Haibin Zhou,Renqi Xu,Yujun Zhao,Krishnapriya Chinnaswamy,Donna McEachern,Jianyong Chen,Chao Yie Yang,Zhaomin Liu,Mi Wang,Liu Liu,Hui Jiang,Bo Wen,Praveen Kumar,Jennifer L. Meagher,Duxin Sun,Jeanne A. Stuckey,Shaomeng Wang +17 more
TL;DR: SD-36 achieves complete and long-lasting tumor regression in multiple xenograft mouse models at well-tolerated dose schedules and is a promising cancer therapeutic strategy.
Journal ArticleDOI
Discovery of ERD-308 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Estrogen Receptor (ER).
Jiantao Hu,Biao Hu,Mingliang Wang,Fuming Xu,Bukeyan Miao,Chao Yie Yang,Mi Wang,Zhaomin Liu,Daniel F. Hayes,Krishnapriya Chinnaswamy,James Delproposto,Jeanne A. Stuckey,Shaomeng Wang +12 more
TL;DR: This work describes the design, synthesis, and extensive structure-activity relationship (SAR) studies of small-molecule ERα degraders based on the proteolysis targeting chimeras (PROTAC) concept, and finds ERD-308 induces more complete ER degradation than fulvestrant, the only approved selective ER degrader (SERD).
Journal ArticleDOI
Structure-Based Discovery of SD-36 as a Potent, Selective, and Efficacious PROTAC Degrader of STAT3 Protein.
Haibin Zhou,Longchuan Bai,Renqi Xu,Yujun Zhao,Jianyong Chen,Donna McEachern,Krishnapriya Chinnaswamy,Bo Wen,Lipeng Dai,Praveen Kumar,Chao Yie Yang,Zhaomin Liu,Mi Wang,Liu Liu,Jennifer L. Meagher,Han Yi,Duxin Sun,Jeanne A. Stuckey,Shaomeng Wang +18 more
TL;DR: SD-36 is a potent, selective and efficacious STAT3 degrader based upon the proteolysis targeting chimera (PROTAC) concept and achieves nanomolar cell growth inhibitory activity in leukemia and lymphoma cell lines with high levels of phosphorylated STAT3.
Journal ArticleDOI
Simple Structural Modifications Converting a Bona fide MDM2 PROTAC Degrader into a Molecular Glue Molecule: A Cautionary Tale in the Design of PROTAC Degraders.
TL;DR: This study provides the first example that simple structural modifications can convert a bona fide PROTAC degrader into a molecular glue compound, which has a completely different mechanism of action.
Journal ArticleDOI
Discovery of M-808 as a Highly Potent, Covalent, Small-Molecule Inhibitor of the Menin–MLL Interaction with Strong In Vivo Antitumor Activity
Shilin Xu,Angelo Aguilar,Liyue Huang,Tianfeng Xu,Ke Zheng,Donna McEachern,Sally Przybranowski,Caroline Foster,Kaitlin P Zawacki,Zhaomin Liu,Krishnapriya Chinnaswamy,Jeanne A. Stuckey,Shaomeng Wang +12 more
TL;DR: Determination of the co-crystal structure of M-808 in complex with menin provides a structural basis for their high-affinity, covalent interactions and represents a promising,covalent menin inhibitor for further optimization and evaluation.