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@article{927129,
author = {Krejčí, Pavel and Murakami, Shunichi and Procházková, Jiřina and Trantírek, Lukáš and Chlebová, Katarína and Ouyang, Zhufeng and Aklian, Anie and Smutný, Jiří and Bryja, Vítězslav and Kozubík, Alois and Wilcox, Wiliam R.},
article_number = {27},
doi = {http://dx.doi.org/10.1074/jbc.M109.083626},
keywords = {ERK MAP KINASE; ACTIVATING MUTATIONS; PROLIFERATION; SURAMIN; PATHWAY; DIFFERENTIATION; ACHONDROPLASIA; ASSOCIATION; ANTAGONIST; EXPRESSION},
language = {eng},
issn = {0021-9258},
journal = {J. Biol. Chem.},
title = {Nf449 is a novel inhibitor of fibroblast growth factor receptor 3 (fgfr3) signaling active in chondrocytes and multiple myeloma cells},
volume = {285},
year = {2010}
}
TY - JOUR
ID - 927129
AU - Krejčí, Pavel - Murakami, Shunichi - Procházková, Jiřina - Trantírek, Lukáš - Chlebová, Katarína - Ouyang, Zhufeng - Aklian, Anie - Smutný, Jiří - Bryja, Vítězslav - Kozubík, Alois - Wilcox, Wiliam R.
PY - 2010
TI - Nf449 is a novel inhibitor of fibroblast growth factor receptor 3 (fgfr3) signaling active in chondrocytes and multiple myeloma cells
JF - J. Biol. Chem.
VL - 285
IS - 27
SP - 20644-20653
EP - 20644-20653
SN - 00219258
KW - ERK MAP KINASE
KW - ACTIVATING MUTATIONS
KW - PROLIFERATION
KW - SURAMIN
KW - PATHWAY
KW - DIFFERENTIATION
KW - ACHONDROPLASIA
KW - ASSOCIATION
KW - ANTAGONIST
KW - EXPRESSION
N2 - The FGFR3 receptor tyrosine kinase represents an attractive target for therapy due to its role in several human disorders, including skeletal dysplasias, multiple myeloma, and cervical and bladder carcinomas. By using molecular library screening, we identified a compound named NF449 with inhibitory activity toward FGFR3 signaling. In cultured chondrocytes and murine limb organ culture, NF449 rescued FGFR3-mediated extracellular matrix loss and growth inhibition, which represent two major cellular phenotypes of aberrant FGFR3 signaling in cartilage. Similarly, NF449 antagonized FGFR3 action in the multiple myeloma cell lines OPM2 and KMS11. In cell-free kinase assays, NF449 inhibited the kinase activity of both wild type and a disease-associated FGFR3 mutant (K650E) in a fashion that appeared non-competitive with ATP.
ER -
KREJČÍ, Pavel, Shunichi MURAKAMI, Jiřina PROCHÁZKOVÁ, Lukáš TRANTÍREK, Katarína CHLEBOVÁ, Zhufeng OUYANG, Anie AKLIAN, Jiří SMUTNÝ, Vítězslav BRYJA, Alois KOZUBÍK and Wiliam R. WILCOX. Nf449 is a novel inhibitor of fibroblast growth factor receptor 3 (fgfr3) signaling active in chondrocytes and multiple myeloma cells. \textit{J. Biol. Chem.}. 2010, vol.~285, No~27, p.~20644-20653. ISSN~0021-9258. Available from: https://dx.doi.org/10.1074/jbc.M109.083626.
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