J
Jin-Jun Liu
Researcher at Hoffmann-La Roche
Publications - 42
Citations - 1406
Jin-Jun Liu is an academic researcher from Hoffmann-La Roche. The author has contributed to research in topics: Cyclin-dependent kinase & Kinase. The author has an hindex of 15, co-authored 42 publications receiving 1226 citations.
Papers
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Journal ArticleDOI
Discovery of RG7388, a Potent and Selective p53-MDM2 Inhibitor in Clinical Development.
Qingjie Ding,Zhuming Zhang,Jin-Jun Liu,Nan Jiang,Jing Zhang,Tina Morgan Ross,Xin-Jie Chu,David Joseph Bartkovitz,Frank John Podlaski,Cheryl Janson,Christian Tovar,Zoran Filipovic,Brian Higgins,Kelli Glenn,Packman Kathryn E,Lyubomir T. Vassilev,Bradford Graves +16 more
TL;DR: The discovery and characterization of a second generation clinical MDM2 inhibitor, RG7388, with superior potency and selectivity is reported, with a significant challenge for the development of small-molecule inhibitors with desirable pharmacological profiles.
Journal ArticleDOI
Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
Binh Thanh Vu,Peter Michael Wovkulich,Giacomo Pizzolato,Allen John Lovey,Qingjie Ding,Nan Jiang,Jin-Jun Liu,Chunlin Zhao,Kelli Glenn,Yang Wen,Christian Tovar,Packman Kathryn E,Lyubomir T. Vassilev,Bradford Graves +13 more
TL;DR: RG7112 is the first clinical small-molecule MDM2 inhibitor designed to occupy the p53-binding pocket ofMDM2, which stabilizes p53 and activates the p 53 pathway, leading to cell cycle arrest, apoptosis, and inhibition or regression of human tumor xenografts.
Patent
Substituted pyrrolidine-2-carboxamides
David Joseph Bartkovitz,Xin-Jie Chu,Qingjie Ding,Nan Jiang,Jin-Jun Liu,Tina Morgan Ross,Jing Zhang,Zhuming Zhang +7 more
TL;DR: In this article, the authors provided compounds of the formula (I) wherein X, Y, R1, R2, R3, R4, R5, R6 and R7 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof.
Journal ArticleDOI
Discovery of Potent and Orally Active p53-MDM2 Inhibitors RO5353 and RO2468 for Potential Clinical Development.
Zhuming Zhang,Xin-Jie Chu,Jin-Jun Liu,Qingjie Ding,Jing Zhang,David Joseph Bartkovitz,Nan Jiang,Prabha Karnachi,Sung-Sau So,Christian Tovar,Zoran Filipovic,Brian Higgins,Kelli Glenn,Packman Kathryn E,Lyubomir T. Vassilev,Bradford Graves +15 more
TL;DR: Two new potent, selective, and orally active p53-MDM2 antagonists are reported, RO5353 and RO2468, as follow-ups with promising potential for clinical development.
Journal ArticleDOI
Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors.
Shaoqing Chen,Li Chen,Nam T. Le,Chunlin Zhao,Achyutharao Sidduri,Jian Ping Lou,Christophe Michoud,Louis Portland,Nicole Jackson,Jin-Jun Liu,Fred Konzelmann,Feng Chi,Christian Tovar,Qing Xiang,Yingsi Chen,Yang Wen,Lyubomir T. Vassilev +16 more
TL;DR: A novel series of quinolinyl-methylene-thiazolinones has been identified as potent and selective cyclin-dependent kinase 1 (CDK1) inhibitors, suggesting a potential use as antitumor agents.