The DOI matches its Crossref record; 43 of the 43 references it cites were found in a registry or an index.
Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia
Open accessAbstract
Summary Translocations involving the Mixed Lineage Leukemia (MLL) gene result in human acute leukemias with very poor prognosis. The leukemogenic activity of MLL fusion proteins is critically dependent on their direct interaction with menin, a product of the MEN1 gene. Here, we present the first small molecule inhibitors of the menin-MLL fusion protein interaction that specifically bind to menin with nanomolar affinities. These compounds effectively reverse MLL fusion protein-mediated leukemic transformation by downregulating the expression of target genes required for MLL fusion protein oncogenic activity. They also selectively block proliferation and induce both apoptosis and differentiation of leukemia cells harboring MLL translocations. Identification of these compounds provides a new tool for better understanding MLL-mediated leukemogenesis and represents a new approach for studying the role of menin as an oncogenic cofactor of MLL fusion proteins. Our findings also highlight a new therapeutic strategy for aggressive leukemias with MLL rearrangements.
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MLL translocations specify a distinct gene expression profile that distinguishes a unique leukemia
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Menin Associates with a Trithorax Family Histone Methyltransferase Complex and with the Hoxc8 Locus
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Bushweller, J. H. (2019) · Nature Reviews Cancer · doi:10.1038/s41568-019-0196-7 · Cited by 919
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Gain-of-function p53 mutants co-opt chromatin pathways to drive cancer growth
Zhu, J., Sammons, M. A., Donahue, G., Dou, Z., Vedadi, M., Getlik, M., Barsyte-Lovejoy, D., Al-awar, R., Katona, B. W., Shilatifard, A., et al. (2015) · Nature · doi:10.1038/nature15251 · Cited by 493
Advances in Targeting ‘Undruggable’ transcription Factors With Small Molecules
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Metadata
- Authors
- Grembecka, J., He, S., Shi, A., Purohit, T., Muntean, A. G., Sorenson, R. J., Showalter, H. D., Murai, M. J., Belcher, A. M., Hartley, T., Hess, J. L., & Cierpicki, T.
- Venue
- Nature Chemical Biology
- Published
- 2012-01-29
- Volume
- 8
- Issue
- 3
- Pages
- 277-284
- ISSN
- 1552-4450 (ISSN-L)
- 1552-4469
- OpenAlex
- W1990739246
- Cited by
- 462
- References
- 43
- FWCI
- 21.90
- Type
- journal article
- Language
- en
- Open access
- green
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- Grembecka, J., He, S., Shi, A., Purohit, T., Muntean, A. G., Sorenson, R. J., Showalter, H. D., Murai, M. J., Belcher, A. M., Hartley, T., Hess, J. L., & Cierpicki, T. (2012). Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia. Nature Chemical Biology. https://doi.org/10.1038/nchembio.773
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