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Nature
Article
License: implied-oa
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PubMed Central
Other literature type . 2011
Data sources: PubMed Central
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Nature
Article . 2011 . Peer-reviewed
License: Springer TDM
Data sources: Crossref
Nature
Article . 2011
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SCFFBW7 regulates cellular apoptosis by targeting MCL1 for ubiquitylation and destruction

Authors: Steven P. Gygi; Ronald A. DePinho; Alan Tseng; Shavali Shaik; Thomas Look; Alan W. Lau; Jon C. Aster; +13 Authors

SCFFBW7 regulates cellular apoptosis by targeting MCL1 for ubiquitylation and destruction

Abstract

The effective use of targeted therapy is highly dependent on the identification of responder patient populations. Loss of FBW7, which encodes a tumour-suppressor protein, is frequently found in various types of human cancer, including breast cancer, colon cancer and T-cell acute lymphoblastic leukaemia (T-ALL). In line with these genomic data, engineered deletion of Fbw7 in mouse T cells results in T-ALL, validating FBW7 as a T-ALL tumour suppressor. Determining the precise molecular mechanisms by which FBW7 exerts antitumour activity is an area of intensive investigation. These mechanisms are thought to relate in part to FBW7-mediated destruction of key proteins relevant to cancer, including Jun, Myc, cyclin E and notch 1 (ref. 9), all of which have oncoprotein activity and are overexpressed in various human cancers, including leukaemia. In addition to accelerating cell growth, overexpression of Jun, Myc or notch 1 can also induce programmed cell death. Thus, considerable uncertainty surrounds how FBW7-deficient cells evade cell death in the setting of upregulated Jun, Myc and/or notch 1. Here we show that the E3 ubiquitin ligase SCF(FBW7) (a SKP1-cullin-1-F-box complex that contains FBW7 as the F-box protein) governs cellular apoptosis by targeting MCL1, a pro-survival BCL2 family member, for ubiquitylation and destruction in a manner that depends on phosphorylation by glycogen synthase kinase 3. Human T-ALL cell lines showed a close relationship between FBW7 loss and MCL1 overexpression. Correspondingly, T-ALL cell lines with defective FBW7 are particularly sensitive to the multi-kinase inhibitor sorafenib but resistant to the BCL2 antagonist ABT-737. On the genetic level, FBW7 reconstitution or MCL1 depletion restores sensitivity to ABT-737, establishing MCL1 as a therapeutically relevant bypass survival mechanism that enables FBW7-deficient cells to evade apoptosis. Therefore, our work provides insight into the molecular mechanism of direct tumour suppression by FBW7 and has implications for the targeted treatment of patients with FBW7-deficient T-ALL.

Country
United States
Keywords

Niacinamide, F-Box-WD Repeat-Containing Protein 7, Pyridines, Molecular Sequence Data, Cell-Line-Tumor, F-Box-Proteins, 610, Apoptosis, Cell Cycle Proteins, Precursor T-Cell Lymphoblastic Leukemia-Lymphoma, Cell-Cycle-Proteins, Article, Piperazines, Nitrophenols, Glycogen Synthase Kinase 3, Mice, Tumor-Suppressor-Proteins, Cell Line, Tumor, Animals, Humans, Amino Acid Sequence, Phosphorylation, Glycogen-Synthase-Kinase-3, Molecular-Sequence-Data, Sulfonamides, Proto-Oncogene-Proteins-c-bcl-2, F-Box Proteins, Phenylurea Compounds, Benzenesulfonates, Biphenyl Compounds, Ubiquitin-Protein-Ligases, Precursor-T-Cell-Lymphoblastic-Leukemia-Lymphoma, SKP-Cullin-F-Box-Protein-Ligases, Myeloid Cell Leukemia Sequence 1 Protein, Biphenyl-Compounds, Protein-Binding

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citations
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Citations provided by BIP!
popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
BIP!Popularity provided by BIP!
influence
This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Influence provided by BIP!
impulse
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
BIP!Impulse provided by BIP!
571
Top 1%
Top 1%
Top 0.1%
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