Skip to main content

Thank you for visiting You are using a browser version with limited support for CSS. To obtain the best experience, we recommend you use a more up to date browser (or turn off compatibility mode in Internet Explorer). In the meantime, to ensure continued support, we are displaying the site without styles and JavaScript.


Split-personality inhibitors

A rationally designed class of mTORC1 inhibitors combines the selectivity of rapamycin with the potency of mTOR kinase inhibitors.

This is a preview of subscription content, access via your institution

Access options

Rent or buy this article

Get just this article for as long as you need it


Prices may be subject to local taxes which are calculated during checkout

Fig. 1: Bi-steric mTORC1 inhibitors combine the selectivity of rapamycin with the potency of mTORKIs.


  1. Saxton, R. A. & Sabatini, D. M. Cell 168, 960–976 (2017).

    Article  CAS  Google Scholar 

  2. Benjamin, D., Colombi, M., Moroni, C. & Hall, M. N. Nat. Rev. Drug Discov. 10, 868–880 (2011).

    Article  CAS  Google Scholar 

  3. Lee, B. J. et al. Nat. Chem. Biol. (2021).

  4. Choo, A.Y., Yoon, S.O., Kim, S.G., Roux, P.P. & Blenis, J. Proc. Natl. Acad. Sci. USA 105, 17414–17419 (2008).

    Article  CAS  Google Scholar 

  5. Feldman, M. E. et al. PLoS Biol. 7, e38 (2009).

    Article  Google Scholar 

  6. Thoreen, C. C. et al. J. Biol. Chem. 284, 8023–8032 (2009).

    Article  CAS  Google Scholar 

  7. Dowling, R. J. et al. Science 328, 1172–1176 (2010).

    Article  CAS  Google Scholar 

  8. Rodrik-Outmezguine, V. S. et al. Nature 534, 272–276 (2016).

    Article  CAS  Google Scholar 

  9. Sarbassov, D. D. et al. Mol. Cell 22, 159–168 (2006).

    Article  CAS  Google Scholar 

  10. Kennedy, B. K. & Lamming, D. W. Cell Metab. 23, 990–1003 (2016).

    Article  CAS  Google Scholar 

Download references

Author information

Authors and Affiliations


Corresponding author

Correspondence to Carson C. Thoreen.

Ethics declarations

Competing interests

The author declares no competing interests.

Rights and permissions

Reprints and Permissions

About this article

Verify currency and authenticity via CrossMark

Cite this article

Thoreen, C.C. Split-personality inhibitors. Nat Chem Biol 17, 1012–1013 (2021).

Download citation

  • Published:

  • Issue Date:

  • DOI:


Quick links

Nature Briefing: Cancer

Sign up for the Nature Briefing: Cancer newsletter — what matters in cancer research, free to your inbox weekly.

Get what matters in cancer research, free to your inbox weekly. Sign up for Nature Briefing: Cancer