Effective and selective targeting of leukemia cells using a TORC1/2 kinase inhibitor

Janes MR, Limon JJ, So L, Chen J, Lim RJ, Chavez MA, Vu C, Lilly MB, Mallya S, Ong ST, Konopleva M, …, Fruman DA · 2010 · Nature medicine · Atlas ID JAN2010

What this study shows

The ATP-competitive TORC1/2 inhibitor PP242 selectively kills leukemia cells, with much weaker effects on the proliferation and function of normal lymphocytes.

Abstract

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Targeting the mammalian target of rapamycin (mTOR) protein is a promising strategy for cancer therapy. The mTOR kinase functions in two complexes, TORC1 (target of rapamycin complex-1) and TORC2 (target of rapamycin complex-2); however, neither of these complexes is fully inhibited by the allosteric inhibitor rapamycin or its analogs. We compared rapamycin with PP242, an inhibitor of the active site of mTOR in both TORC1 and TORC2 (hereafter referred to as TORC1/2), in models of acute leukemia harboring the Philadelphia chromosome (Ph) translocation.

Read the full abstract on PubMed →

At a glance

Evidence type	M Molecular — cells, biochemistry, structure Marked M because it is molecular or in-vitro work (model: Leukemia cells; mouse) rather than a whole-organism health-outcome study. That is often exactly where causal biology gets established -- the code says which system the finding was shown in, and nothing about how good the work is.
Study type	5 - Mechanistic / In Vitro
Model system	Leukemia cells; mouse
Journal	Nature medicine
Year	2010
Peer reviewed	Yes
Record last updated	2026-10-01
Source	DOI 10.1038/nm.2091 · PMID 20072130 · Free full text (PMC4017764)

Extracted findings

These fields were extracted from the paper with AI assistance and have not been checked against the source. Read them as a pointer into the paper, not as curated claims; where they disagree with the curated summary above, the curated summary stands.

Intervention	PP242 (ATP-competitive TORC1/2 inhibitor) vs rapamycin
Target	mTORC1 & mTORC2
Model	Leukemia cells; mouse (Ph+ ALL)
Effect	TORC1/2 active-site inhibition selectively targets leukemia cells more effectively than rapamycin

In the Atlas

Links in the pathway map

Supports ATP-competitive mTOR inhibitors inhibits mTORC1
Supports ATP-competitive mTOR inhibitors inhibits mTORC2

Cite this paper

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Janes, M. R., Limon, J. J., So, L., Chen, J., Lim, R. J., Chavez, M. A., Vu, C., Lilly, M. B., Mallya, S., Ong, S. T., Konopleva, M., Martin, M. B., Ren, P., Liu, Y., Rommel, C., & Fruman, D. A. (2010). Effective and selective targeting of leukemia cells using a TORC1/2 kinase inhibitor. Nature medicine. https://doi.org/10.1038/nm.2091

@article{JAN2010,
  author       = {Janes, M. R. and Limon, J. J. and So, L. and Chen, J. and Lim, R. J. and Chavez, M. A. and Vu, C. and Lilly, M. B. and Mallya, S. and Ong, S. T. and Konopleva, M. and Martin, M. B. and Ren, P. and Liu, Y. and Rommel, C. and Fruman, D. A.},
  title        = {{Effective and selective targeting of leukemia cells using a TORC1/2 kinase inhibitor}},
  journal      = {Nature medicine},
  year         = {2010},
  doi          = {10.1038/nm.2091},
  note         = {PMID: 20072130},
}

Cite this Atlas record

The record is the Atlas's own work — the evidence label, the extracted findings and the links. It is cited as part of the dataset, not as the paper.

Barton, O. (2026). Oliver's mTOR Atlas (record JAN2010) [Data set]. https://mtor-atlas.org/study/JAN2010/ · Dataset DOI 10.5281/zenodo.22059963

@misc{atlas_JAN2010,
  author       = {Barton, Oliver},
  title        = {{Oliver's mTOR Atlas}, record JAN2010},
  howpublished = {Data set},
  year         = {2026},
  url          = {https://mtor-atlas.org/study/JAN2010/},
  doi          = {10.5281/zenodo.22059963}
}

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