| Literature DB >> 25658656 |
Zachary Miller1, Keun-Sik Kim, Do-Min Lee, Vinod Kasam, Si Eun Baek, Kwang Hyun Lee, Yan-Yan Zhang, Lin Ao, Kimberly Carmony, Na-Ra Lee, Shou Zhou, Qingquan Zhao, Yujin Jang, Hyun-Young Jeong, Chang-Guo Zhan, Wooin Lee, Dong-Eun Kim, Kyung Bo Kim.
Abstract
We performed a virtual screen of ∼340 000 small molecules against the active site of proteasomes followed by in vitro assays and subsequent optimization, yielding a proteasome inhibitor with pyrazole scaffold. The pyrazole-scaffold compound displayed excellent metabolic stability and was highly effective in suppressing solid tumor growth in vivo. Furthermore, the effectiveness of this compound was not negatively impacted by resistance to bortezomib or carfilzomib.Entities:
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Year: 2015 PMID： 25658656 DOI： 10.1021/jm501344n
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446