| ŠRÁMEK, Martin, Jakub NERADIL, Petra MACIGOVÁ, Peter MÚDRY, Kristýna POLÁŠKOVÁ, Ondřej SLABÝ, Hana NOSKOVÁ, Jaroslav ŠTĚRBA and Renata VESELSKÁ. Effects of Sunitinib and Other Kinase Inhibitors on Cells Harboring a PDGFRB Mutation Associated with Infantile Myofibromatosis. International Journal of Molecular Sciences. Basel: MDPI, vol. 19, No 9, p. 1-16. ISSN 1422-0067. doi:10.3390/ijms19092599. 2018. |
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@article{1498157,
author = {Šrámek, Martin and Neradil, Jakub and Macigová, Petra and Múdry, Peter and Polášková, Kristýna and Slabý, Ondřej and Nosková, Hana and Štěrba, Jaroslav and Veselská, Renata},
article_location = {Basel},
article_number = {9},
doi = {http://dx.doi.org/10.3390/ijms19092599},
keywords = {Infantile myofibromatosis; receptor tyrosine kinases; platelet-derived growth factor receptor; protein kinase inhibitors; sunitinib; erlotinib; FR180204; U0126; targeted therapy},
language = {eng},
issn = {1422-0067},
journal = {International Journal of Molecular Sciences},
title = {Effects of Sunitinib and Other Kinase Inhibitors on Cells Harboring a PDGFRB Mutation Associated with Infantile Myofibromatosis},
url = {https://www.mdpi.com/1422-0067/19/9/2599},
volume = {19},
year = {2018}
}
TY - JOUR
ID - 1498157
AU - Šrámek, Martin - Neradil, Jakub - Macigová, Petra - Múdry, Peter - Polášková, Kristýna - Slabý, Ondřej - Nosková, Hana - Štěrba, Jaroslav - Veselská, Renata
PY - 2018
TI - Effects of Sunitinib and Other Kinase Inhibitors on Cells Harboring a PDGFRB Mutation Associated with Infantile Myofibromatosis
JF - International Journal of Molecular Sciences
VL - 19
IS - 9
SP - 1-16
EP - 1-16
PB - MDPI
SN - 14220067
KW - Infantile myofibromatosis
KW - receptor tyrosine kinases
KW - platelet-derived growth factor receptor
KW - protein kinase inhibitors
KW - sunitinib
KW - erlotinib
KW - FR180204
KW - U0126
KW - targeted therapy
UR - https://www.mdpi.com/1422-0067/19/9/2599
L2 - https://www.mdpi.com/1422-0067/19/9/2599
N2 - Infantile myofibromatosis represents one of the most common proliferative fibrous tumors of infancy and childhood. More effective treatment is needed for drug-resistant patients, and targeted therapy using specific protein kinase inhibitors could be a promising strategy. To date, several studies have confirmed a connection between the p.R561C mutation in gene encoding platelet-derived growth factor receptor beta (PDGFR-beta) and the development of infantile myofibromatosis. This study aimed to analyze the phosphorylation of important kinases in the NSTS-47 cell line derived from a tumor of a boy with infantile myofibromatosis who harbored the p.R561C mutation in PDGFR-beta. The second aim of this study was to investigate the effects of selected protein kinase inhibitors on cell signaling and the proliferative activity of NSTS-47 cells. We confirmed that this tumor cell line showed very high phosphorylation levels of PDGFR-beta, extracellular signal-regulated kinases (ERK) 1/2 and several other protein kinases. We also observed that PDGFR-beta phosphorylation in tumor cells is reduced by the receptor tyrosine kinase inhibitor sunitinib. In contrast, MAPK/ERK kinases (MEK) 1/2 and ERK1/2 kinases remained constitutively phosphorylated after treatment with sunitinib and other relevant protein kinase inhibitors. Our study showed that sunitinib is a very promising agent that affects the proliferation of tumor cells with a p.R561C mutation in PDGFR-beta.
ER -
ŠRÁMEK, Martin, Jakub NERADIL, Petra MACIGOVÁ, Peter MÚDRY, Kristýna POLÁŠKOVÁ, Ondřej SLABÝ, Hana NOSKOVÁ, Jaroslav ŠTĚRBA and Renata VESELSKÁ. Effects of Sunitinib and Other Kinase Inhibitors on Cells Harboring a PDGFRB Mutation Associated with Infantile Myofibromatosis. \textit{International Journal of Molecular Sciences}. Basel: MDPI, vol.~19, No~9, p.~1-16. ISSN~1422-0067. doi:10.3390/ijms19092599. 2018.
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