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@ARTICLE{ValdezCapuccino:290343,
author = {L. Valdez Capuccino and T. Kleitke and B. Szokol and L.
Svajda and F. Martin and F. Bonechi and M. Krekó and S.
Azami and A. Montinaro and Y. Wang and V. Nikolov and L.
Kaiser and D. Bonasera and J. Saggau and T. Scholz and A.
Schmitt and F. Beleggia and A. Reinhardt$^*$ and J. George
and G. Liccardi and H. Walczak and J. Tóvári and J.
Brägelmann and J. Montero and M. L. Sos$^*$ and L. Őrfi
and N. Peltzer},
title = {{CDK}9 inhibition as an effective therapy for small cell
lung cancer.},
journal = {Cell death $\&$ disease},
volume = {15},
number = {5},
issn = {2041-4889},
address = {London [u.a.]},
publisher = {Nature Publishing Group},
reportid = {DKFZ-2024-01070},
pages = {345},
year = {2024},
abstract = {Treatment-naïve small cell lung cancer (SCLC) is typically
susceptible to standard-of-care chemotherapy consisting of
cisplatin and etoposide recently combined with PD-L1
inhibitors. Yet, in most cases, SCLC patients develop
resistance to first-line therapy and alternative therapies
are urgently required to overcome this resistance. In this
study, we tested the efficacy of dinaciclib, an FDA-orphan
drug and inhibitor of the cyclin-dependent kinase (CDK) 9,
among other CDKs, in SCLC. Furthermore, we report on a newly
developed, highly specific CDK9 inhibitor, VC-1, with
tumour-killing activity in SCLC. CDK9 inhibition displayed
high killing potential in a panel of mouse and human SCLC
cell lines. Mechanistically, CDK9 inhibition led to a
reduction in MCL-1 and cFLIP anti-apoptotic proteins and
killed cells, almost exclusively, by intrinsic apoptosis.
While CDK9 inhibition did not synergise with chemotherapy,
it displayed high efficacy in chemotherapy-resistant cells.
In vivo, CDK9 inhibition effectively reduced tumour growth
and improved survival in both autochthonous and syngeneic
SCLC models. Together, this study shows that CDK9 inhibition
is a promising therapeutic agent against SCLC and could be
applied to chemo-refractory or resistant SCLC.},
keywords = {Cyclin-Dependent Kinase 9: antagonists $\&$ inhibitors /
Cyclin-Dependent Kinase 9: metabolism / Small Cell Lung
Carcinoma: drug therapy / Small Cell Lung Carcinoma:
pathology / Humans / Animals / Lung Neoplasms: drug therapy
/ Lung Neoplasms: pathology / Cell Line, Tumor / Mice /
Pyridinium Compounds: pharmacology / Pyridinium Compounds:
therapeutic use / Indolizines: pharmacology / Cyclic
N-Oxides: pharmacology / Apoptosis: drug effects / Bridged
Bicyclo Compounds, Heterocyclic: pharmacology / Bridged
Bicyclo Compounds, Heterocyclic: therapeutic use / Protein
Kinase Inhibitors: pharmacology / Protein Kinase Inhibitors:
therapeutic use / CDK9 protein, human (NLM Chemicals) /
dinaciclib (NLM Chemicals)},
cin = {ED01 / MU01},
ddc = {570},
cid = {I:(DE-He78)ED01-20160331 / I:(DE-He78)MU01-20160331},
pnm = {899 - ohne Topic (POF4-899)},
pid = {G:(DE-HGF)POF4-899},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:38769311},
doi = {10.1038/s41419-024-06724-4},
url = {https://inrepo02.dkfz.de/record/290343},
}