mTOR Inhibitor and Autophagy Inducer

mTOR inhibition by Torin 1

Torin 1 is a potent and selective ATP-competitive inhibitor of mTOR (mammalian target of Rapamycin) kinase [1]. It is the catalytic subunit of two functionally distinct complexes (mTORc1 and mTORc2) that coordinately promote cell growth, proliferation, and survival. The multi-component mTOR complexes are comprised of different binding partners that confer separate functions.

More details

Mode of action:

Unlike classical mTOR inhibitors such as Rapamycin, Torin 1 is able to effectively block phosphorylation of mTORc1 and mTORc2 [2].

Torin 1 is an effective inducer of autophagy, as inhibition of mTOR mimics cellular starvation by blocking signals required for cell growth and proliferation [3, 4].

Interestingly, Torin 1 has also been shown to have cytotoxic and cytostatic effects in rapamycin-resistant cells [5].

Key features:

A potent mTOR inhibitor
Blocks phosphorylation of mTORc1 and mTORc2
An autophagy inducer

Read our review on Autophagy and Innate Immunity

References:

1. Liu Q. et al., 2010. Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a highly potent, selective Mammalian Target of Rapamycin (mTOR) inhibitor for the treatment of cancer. Med Chem. 53(19):7146-55.
2. Thoreen C.C. et al., 2009. An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycin-resistant functions of mTORC1. J Biol Chem. 284(12):8023‑32.
3. Jung C.H. et al., 2010. mTOR regulation of autophagy. FEBS Lett. 584(7):1287-95.
4. Wang R.C. et al., 2012. Akt-mediated regulation of autophagy and tumorigenesis through Beclin 1 phosphorylation. Science 338(6109):956-9.
5. Park S. et al., 2016. Rapamycin-resistant and torin-sensitive mTOR signaling promotes the survival and proliferation of leukemic cells. BMB Rep. 49(1): 63‑68.

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