Bioorganic and Medicinal Chemistry Letters p. 3038 - 3041 (2016)
Update date:2022-08-05
Topics:
Yoon, Suyoung
Kim, Jong Hyun
Yoon, Ina
Kim, Changhoon
Kim, Sung-Eun
Koh, Yura
Jeong, Seung Jae
Lee, Jiyoun
Kim, Sunghoon
Lee, Jeewoo
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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