| Literature DB >> 23808545 |
Qingjie Ding1, Zhuming Zhang, Jin-Jun Liu, Nan Jiang, Jing Zhang, Tina M Ross, Xin-Jie Chu, David Bartkovitz, Frank Podlaski, Cheryl Janson, Christian Tovar, Zoran M Filipovic, Brian Higgins, Kelli Glenn, Kathryn Packman, Lyubomir T Vassilev, Bradford Graves.
Abstract
Restoration of p53 activity by inhibition of the p53-MDM2 interaction has been considered an attractive approach for cancer treatment. However, the hydrophobic protein-protein interaction surface represents a significant challenge for the development of small-molecule inhibitors with desirable pharmacological profiles. RG7112 was the first small-molecule p53-MDM2 inhibitor in clinical development. Here, we report the discovery and characterization of a second generation clinical MDM2 inhibitor, RG7388, with superior potency and selectivity.Entities:
Mesh：
Substances：
Year: 2013 PMID： 23808545 DOI： 10.1021/jm400487c
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446