کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1369849 | 981791 | 2016 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery of (S)-4-isobutyloxazolidin-2-one as a novel leucyl-tRNA synthetase (LRS)-targeted mTORC1 inhibitor
ترجمه فارسی عنوان
کشف (S) -4-isobutyloxazolidin-2-one به عنوان یک مهارکننده mTORC1 هدفمند از leucyl-tRNA synthetase (LRS)
دانلود مقاله + سفارش ترجمه
دانلود مقاله ISI انگلیسی
رایگان برای ایرانیان
کلمات کلیدی
لنفوسیت، مهارکننده mTORC1؛ Leucinol
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
چکیده انگلیسی
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.
Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 26, Issue 13, 1 July 2016, Pages 3038–3041
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 26, Issue 13, 1 July 2016, Pages 3038–3041
نویسندگان
Suyoung Yoon, Jong Hyun Kim, Ina Yoon, Changhoon Kim, Sung-Eun Kim, Yura Koh, Seung Jae Jeong, Jiyoun Lee, Sunghoon Kim, Jeewoo Lee,