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@ARTICLE{White:306549,
author = {M. White and M. L. Mills and L. M. Millett and K. Gilroy
and Y. Hong and L. B. Zeiger and R. J. Simpson and S. M.
Corry and A. Ligeza and T. R. M. Lannagan and S. Susanti and
R. A. Ridgway and A. S. Yazgili and L. Grzesiak and R.
Amirkhah and C. A. Ford and N. Vlahov and H. Tovell and L.
Officer-Jones and C. Ficken and R. Pennie and A. K.
Najumudeen and A. Raven and N. Nasreddin and E. Chauhan and
A. S. Papanastasiou and C. Nixon and V. Morrison and R.-F.
Jackstadt$^*$ and J. S. Graham and C. J. Miller and S. J.
Ross and S. T. Barry and V. Pavet and R. H. Wilson and J. Le
Quesne and P. D. Dunne and S. Tejpar and S. Leedham and A.
D. Campbell and O. J. Sansom},
title = {{MAPK}-driven epithelial cell plasticity drives colorectal
cancer therapeutic resistance.},
journal = {Nature},
volume = {650},
number = {8102},
issn = {0028-0836},
address = {London [u.a.]},
publisher = {Nature Publ. Group},
reportid = {DKFZ-2025-02614},
pages = {748-758},
year = {2026},
note = {2026 Feb;650(8102):748-758},
abstract = {The colorectal epithelium is rapidly renewing, with
remarkable capacity to regenerate following injury. In
colorectal cancer (CRC), this regenerative capacity can be
co-opted to drive epithelial plasticity. While oncogenic
MAPK signalling in CRC is common, with frequent mutations of
both KRAS $(40-50\%)$ and BRAF $(10\%)1,$ inhibition of this
pathway typically drives resistance clinically. Given the
development of KRAS inhibitors, and licensing of BRAF
inhibitor combinations2-4, we have interrogated key
mechanisms of resistance to these agents in advanced
preclinical CRC models. We show that oncogenic MAPK
signalling induces epithelial state changes in vivo, driving
adoption of a regenerative/revival stem like population,
while inhibition leads to rapid transcriptional remodeling
of both Kras- and Braf-mutant tumours, favoring a
Wnt-associated, canonical stem phenotype. This drives acute
therapeutic resistance in Kras- and delayed resistance in
Braf-driven models. Importantly, where plasticity is
restrained, such as in early metastatic disease, or through
targeting ligand-dependent Wnt-pathway Rnf43 mutations,
marked therapeutic responses are observed. This explains the
super response to BRAF+EGFR targeted therapies previously
observed in a BRAF/RNF43 co-mutant patient population,
highlighting the criticality of cellular plasticity in
therapeutic response. Together, our data provides clear
insight into the mechanisms underpinning resistance to MAPK
targeted therapies in CRC. Moreover, strategies that aim to
corral stem cell fate, restrict epithelial plasticity or
intervene when tumours lack heterogeneity may improve
therapeutic efficacy of these agents.},
cin = {A013},
ddc = {500},
cid = {I:(DE-He78)A013-20160331},
pnm = {311 - Zellbiologie und Tumorbiologie (POF4-311)},
pid = {G:(DE-HGF)POF4-311},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:41286180},
doi = {10.1038/s41586-025-09916-w},
url = {https://inrepo02.dkfz.de/record/306549},
}