Journal article
Discovery of 2,4-dimethoxypyridines as novel autophagy inhibitors
Autophagy is a catabolic process, which mediates degradation of cellular components and has important roles in health and disease. Therefore, small molecule modulators of autophagy are in great demand. Herein, we describe a phenotypic high-content screen for autophagy inhibitors, which led to the discovery of a dimethoxypyridine-based class of autophagy inhibitors, which derive from previously reported, natural product-inspired MAP4K4 inhibitors.
Comprehensive structure-activity relationship studies led to a potent compound, and biological validation experiments indicated that the mode of action was upstream or independent of mTOR
Language: | English |
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Publisher: | Elsevier Science |
Year: | 2018 |
Pages: | 4531-4537 |
ISSN: | 00404020 and 14645416 |
Types: | Journal article |
DOI: | 10.1016/j.tet.2018.07.021 |
ORCIDs: | Laraia, Luca |