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@PHDTHESIS{HnleKreidler:286019,
author = {S. Hänle-Kreidler$^*$},
title = {{C}haracterization of novel substrates of {SCF}-{FBXW}7 in
mitotic cell fate regulation},
volume = {--},
school = {Universität Heidelberg},
type = {Dissertation},
address = {Heidelberg},
publisher = {---},
reportid = {DKFZ-2023-02596},
isbn = {not applicable},
series = {Dissertation},
pages = {138},
year = {2023},
note = {not applicable; Dissertation, Universität Heidelberg,
2023},
abstract = {Protein ubiquitylation is a post-translational
modification, which can control various cellular processes.
Ubiquitin is conjugated to a substrate by an enzymatic
cascade comprising so-called ubiquitin writers: E1, E2 and
E3 enzymes. More of the ubiquitin-code is continuously
uncovered and functional relationships are established. The
induction of proteasomal degradation is probably the most
prominent function of protein ubiquitylation. The E3
ubiquitin ligases convey specificity by facilitating the
substrate interaction. SKP1-CUL1-F-box protein complexes
belong to the RING E3 ubiquitin ligases and are one of the
largest groups of the over 600 human E3 ubiquitin ligases.
Their substrate receptors, the F-box proteins, are
interchangeable and they can therefore target a vast number
of substrates. FBXW7 is one of the best characterized F-box
proteins and acts as a tumor suppressor by targeting
oncogenes like c-Myc, Cyclin E1 and NOTCH1 for degradation.
Being the most frequently mutated F-box protein in human
cancers, FBXW7 loss-of-function or deletion result in
increased tumor proliferation and chemoresistance.
FBXW7-deficiency promotes mitotic slippage in response to
antimicrotubule drugs and the identification of FBXW7
substrates responsible for this phenotype remains a major
task.In the presented thesis, I aimed at identifying novel
substrates of FBXW7 which are involved in mitotic slippage
to better understand mitotic cell fate regulation. Using a
proteomics approach, I identified the Histone 3 lysine 4
methyltransferase complex component WDR5 as FBXW7 candidate
substrates and showed that FBXW7 regulates WDR5 protein
levels by ubiquitylation. I verified that FBXW7 and WDR5
interact in-vivo and in-vitro and found that the
overexpression of WDR5 and Cyclin E1 can promote mitotic
slippage. Reciprocally, the depletion of WDR5 and Cyclin E1
reduced mitotic slippage induced by knockdown of FBXW7 and
significantly reduced polyploidization after mitotic
slippage. Although the methyltransferase enzymatic subunit
KMT2D is a substrate of FBXW7 and cooperates with WDR5,
knockdown of KMT2D did not affect mitotic cell
fate.Collectively, I identified WDR5 as a novel substrate of
FBXW7 and showed that the FBXW7 substrates WDR5 and Cyclin
E1 can promote mitotic slippage and are required for
drug-induced polyploidy. My results help to better
understand the mechanisms underlying chemotherapy resistance
caused by treatment of cancers with antimicrotubule drugs.},
cin = {F045},
cid = {I:(DE-He78)F045-20160331},
pnm = {316 - Infektionen, Entzündung und Krebs (POF4-316)},
pid = {G:(DE-HGF)POF4-316},
typ = {PUB:(DE-HGF)3 / PUB:(DE-HGF)11},
urn = {---},
url = {https://inrepo02.dkfz.de/record/286019},
}