| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1369849 | Bioorganic & Medicinal Chemistry Letters | 2016 | 4 Pages |
Abstract
A series of leucinol analogs were investigated as leucyl-tRNA synthetase-targeted mTORC1 inhibitors. Among them, compound 5, (S)-4-isobutyloxazolidin-2-one, showed the most potent inhibition on the mTORC1 pathway in a concentration-dependent manner. Compound 5 inhibited downstream phosphorylation of mTORC1 by blocking leucine-sensing ability of LRS, without affecting the catalytic activity of LRS. In addition, compound 5 exhibited cytotoxicity against rapamycin-resistant colon cancer cells, suggesting that LRS has the potential to serve as a novel therapeutic target.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Suyoung Yoon, Jong Hyun Kim, Ina Yoon, Changhoon Kim, Sung-Eun Kim, Yura Koh, Seung Jae Jeong, Jiyoun Lee, Sunghoon Kim, Jeewoo Lee,