Identification of a Novel Oxadiazole Inhibitor of Mammalian Target of Rapamycin
- Identification of a Novel Oxadiazole Inhibitor of Mammalian Target of Rapamycin
- 허우영; 임선우; 김의정; 이효민
- Mammalian target of rapamycin; Screening; mTOR; Inhibitor; 2,3-Dihydro-1,3,4-oxadiazole
- Issue Date
- Bulletin of the Korean Chemical Society
- VOL 41, NO 3-303
- We performed a biochemical screen against mTOR using in‐ house small molecule library. Two novel, structurally distinct hits were identified. Among them, a novel oxadiazole scaffold compound (2) suppressed the phosphorylation of both S6K1 and Akt1 in HeLa cells. Docking study suggested that 2 is ATP‐ competitive and shows a pi‐ pi interaction with Trp2239 and hydrogen bonds with Trp2239 and Thr2245. Through derivatization, a slightly more potent analogue (2a) was identified with IC50 of 9.6 μM. Our study provides a starting point for discovery of novel potent mTOR inhibitors.
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