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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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