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@ARTICLE{Malchers:285132,
author = {F. Malchers and L. Nogova and M. H. van Attekum and L. Maas
and J. Brägelmann and C. Bartenhagen and L. Girard and G.
Bosco and I. Dahmen and S. Michels and C. E. Weeden and A.
H. Scheel and L. Meder and K. Golfmann and P. Schuldt and J.
Siemanowski and J. Rehker and S. Merkelbach-Bruse and R.
Menon and O. Gautschi and J. M. Heuckmann and E. Brambilla
and M.-L. Asselin-Labat and T. Persigehl and J. D. Minna and
H. Walczak and R. T. Ullrich and M. Fischer and H. C.
Reinhardt and J. Wolf and R. Büttner and M. Peifer and J.
George and R. K. Thomas$^*$},
title = {{S}omatic rearrangements causing oncogenic ectodomain
deletions of {FGFR}1 in squamous cell lung cancer.},
journal = {The journal of clinical investigation},
volume = {133},
number = {21},
issn = {0021-9738},
address = {Ann Arbor, Mich.},
publisher = {ASCJ},
reportid = {DKFZ-2023-02256},
pages = {e170217},
year = {2023},
abstract = {The discovery of frequent 8p11-p12 amplifications in
squamous cell lung cancer (SQLC) has fueled hopes that
FGFR1, located inside this amplicon, might be a therapeutic
target. In a clinical trial, only $11\%$ of patients with
8p11 amplification (detected by FISH) responded to FGFR
kinase inhibitor treatment. To understand the mechanism of
FGFR1 dependency, we performed deep genomic characterization
of 52 SQLCs with 8p11-p12 amplification, including 10 tumors
obtained from patients who had been treated with FGFR
inhibitors. We discovered somatically altered variants of
FGFR1 with deletion of exons 1-8 that resulted from
intragenic tail-to-tail rearrangements. These
ectodomain-deficient FGFR1 variants (ΔEC-FGFR1) were
expressed in the affected tumors and were tumorigenic in
both in vitro and in vivo models of lung cancer.
Mechanistically, breakage-fusion-bridges were the source of
8p11-p12 amplification, resulting from frequent head-to-head
and tail-to-tail rearrangements. Generally, tail-to-tail
rearrangements within or in close proximity upstream of
FGFR1 were associated with FGFR1 dependency. Thus, the
genomic events shaping the architecture of the 8p11-p12
amplicon provide a mechanistic explanation for the emergence
of FGFR1-driven SQLC. Specifically, we believe that FGFR1
ectodomain-deficient and FGFR1-centered amplifications
caused by tail-to-tail rearrangements are a novel somatic
genomic event that might be predictive of therapeutically
relevant FGFR1 dependency.},
keywords = {Humans / Lung Neoplasms: drug therapy / Lung Neoplasms:
genetics / Lung Neoplasms: pathology / Gene Amplification /
Carcinoma, Non-Small-Cell Lung: drug therapy / Carcinoma,
Non-Small-Cell Lung: genetics / Carcinoma, Squamous Cell:
genetics / Carcinoma, Squamous Cell: pathology / Receptor,
Fibroblast Growth Factor, Type 1: genetics / Receptor,
Fibroblast Growth Factor, Type 1: metabolism / Protein
Kinase Inhibitors: pharmacology / Epithelial Cells:
metabolism / Drug therapy (Other) / Genetics (Other) / Lung
cancer (Other) / Oncology (Other) / Receptor, Fibroblast
Growth Factor, Type 1 (NLM Chemicals) / Protein Kinase
Inhibitors (NLM Chemicals) / FGFR1 protein, human (NLM
Chemicals)},
cin = {HD01},
ddc = {610},
cid = {I:(DE-He78)HD01-20160331},
pnm = {899 - ohne Topic (POF4-899)},
pid = {G:(DE-HGF)POF4-899},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:37606995},
pmc = {pmc:PMC10617767},
doi = {10.1172/JCI170217},
url = {https://inrepo02.dkfz.de/record/285132},
}