Reference : CCT196969 effectively inhibits growth and survival of melanoma brain metastasis cells

	Document type :	Scientific journals : Article
	Discipline(s) :	Life sciences : Biochemistry, biophysics & molecular biology
	To cite this reference:	http://hdl.handle.net/10993/54416

Title :	CCT196969 effectively inhibits growth and survival of melanoma brain metastasis cells
Language :	English
Author, co-author :	Reigstad, Agathe [University of Bergen - UiB > Department of Biomedicine]
	Herdlevær, Christina Frantzen [University of Bergen - UiB > Department of Biomedicine]
	Rigg, Emma [University of Bergen - UiB > Department of Biomedicine]
	Hoang, Tuyen [University of Bergen - UiB > Department of Biomedicine]
	Bjørnstad, Ole Vidhammer [University of Bergen - UiB > Department of Biomedicine]
	Aasen, Synnøve Nymark [University og Bergen - UiB > Department of Biomedicine > > ; Western Norway University of Applied Sciences > Faculty of Health and Social Sciences]
	Preis, Jasmin Renate [University of Luxembourg > Faculty of Science, Technology and Medicine (FSTM) > Department of Life Sciences and Medicine (DLSM) >]
	Haan, Claude [University of Luxembourg > Faculty of Science, Technology and Medicine (FSTM) > Department of Life Sciences and Medicine (DLSM) >]
	Sundstrøm, Terje [HaukelHaukeland University Hospital > Department of Neurosurgery > > ; University of Bergen - UiB > Department of Clinical Medicine]
	Thorsen, Frits [University of Bergen - UiB > Department of Biomedicine > > ; University of Bergen - UiB > Department of Biomedicine > Molecular Imaging Center]
Publication date :	9-Sep-2022
Journal title :	PLoS ONE
Publisher :	Public Library of Science
Peer reviewed :	Yes
e-ISSN :	1932-6203
City :	San Franscisco
Country :	United States - California
Abstract :	[en] Melanomas frequently metastasize to the brain. Despite recent progress in the treatment of melanoma brain metastasis, therapy resistance and relapse of disease remain unsolved challenges. CCT196969 is a SRC family kinase (SFK) and Raf proto-oncogene, serine/thre onine kinase (RAF) inhibitor with documented effects in primary melanoma cell lines in vitro and in vivo. Using in vitro cell line assays, we studied the effects of CCT196969 in multiple melanoma brain metastasis cell lines. The drug effectively inhibited proliferation, migration, and survival in all examined cell lines, with viability IC50 doses in the range of 0.18–2.6 μM. Western blot analysis showed decreased expression of p-ERK, p-MEK, p-STAT3 and STAT3 upon CCT196969 treatment. Furthermore, CCT196969 inhibited viability in two B Raf Proto-Oncogene (BRAF) inhibitor resistant metastatic melanoma cell lines. Further in vivo studies should be performed to determine the treatment potential of CCT196969 in patients with treatment-naïve and resistant melanoma brain metastasis.
Permalink :	http://hdl.handle.net/10993/54416
DOI :	10.1371/journal.pone.0273711
Other URL :	http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0273711

	File(s) associated to this reference
	Fulltext file(s): File Commentary Version Size Access Open access Registad, Preis, et al. CCT inh growth of melanoma brain metastasis. PLOS 2022.pdf Publisher postprint 2.59 MB View/Open

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