About: Simple, mammalian cell-based assay for identification of inhibitors of the ErkMAP kinase pathway.

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About: Simple, mammalian cell-based assay for identification of inhibitors of the ErkMAP kinase pathway. Goto Sponge NotDistinct Permalink

An Entity of Type : http://linked.opendata.cz/ontology/domain/vavai/Vysledek, within Data Space : linked.opendata.cz associated with source document(s)

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
Description	The Erk MAP kinase pathway contributes to tumor development and thus represents an important therapeutic target. Several inhibitors of the Erk pathway are presently being evaluated in clinical trials for cancer, but show limited efficiency thus warranting discovery of more potent inhibitors. We have developed a novel mammalian cell-based assay that should facilitate the identification of such compounds by screening molecular libraries. In rat chondrosarcoma (RCS) cells, treatment with fibroblast growth factor 2 (FGF2) leads to sustained activation of the Erk pathway, resulting in growth arrest with more than an 80% cell count difference between control and FGF2-treated cells after 72 h of treatment. The extent of both Erk activation and the growth arrest can be precisely modulated by the FGF2 dose. We also demonstrate that FGF2-mediated activation of the Erk pathway is robust and has only a limited sensitivity to the available MEK inhibitors. The Erk MAP kinase pathway contributes to tumor development and thus represents an important therapeutic target. Several inhibitors of the Erk pathway are presently being evaluated in clinical trials for cancer, but show limited efficiency thus warranting discovery of more potent inhibitors. We have developed a novel mammalian cell-based assay that should facilitate the identification of such compounds by screening molecular libraries. In rat chondrosarcoma (RCS) cells, treatment with fibroblast growth factor 2 (FGF2) leads to sustained activation of the Erk pathway, resulting in growth arrest with more than an 80% cell count difference between control and FGF2-treated cells after 72 h of treatment. The extent of both Erk activation and the growth arrest can be precisely modulated by the FGF2 dose. We also demonstrate that FGF2-mediated activation of the Erk pathway is robust and has only a limited sensitivity to the available MEK inhibitors. (en)
Title	Simple, mammalian cell-based assay for identification of inhibitors of the ErkMAP kinase pathway. Simple, mammalian cell-based assay for identification of inhibitors of the ErkMAP kinase pathway. (en)
skos:prefLabel	Simple, mammalian cell-based assay for identification of inhibitors of the ErkMAP kinase pathway. Simple, mammalian cell-based assay for identification of inhibitors of the ErkMAP kinase pathway. (en)
skos:notation	RIV/00216224:14310/07:00067364!RIV14-MSM-14310___
http://linked.open...avai/riv/aktivita	Z
http://linked.open...avai/riv/aktivity	Z(AV0Z50040507), Z(AV0Z50040702), Z(MSM0021622430)
http://linked.open...iv/cisloPeriodika	4
http://linked.open...vai/riv/dodaniDat	2014
http://linked.open...aciTvurceVysledku	Pejchalová, Kateřina Krejčí, Pavel
http://linked.open.../riv/druhVysledku	J - Článek v odborném periodiku
http://linked.open...iv/duvernostUdaju	S - Úplné a pravdivé údaje nepodléhající ochraně podle zvláštních právních předpisů
http://linked.open...titaPredkladatele	Masarykova univerzita / Přírodovědecká fakulta
http://linked.open...dnocenehoVysledku	449817
http://linked.open...ai/riv/idVysledku	RIV/00216224:14310/07:00067364
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	Erk; inhibitor; FGFR3; growth arrest; screening; library (en)
http://linked.open.../riv/klicoveSlovo	growth arrest library screening inhibitor FGFR3 Erk
http://linked.open...odStatuVydavatele	NL - Nizozemsko
http://linked.open...ontrolniKodProRIV	[59815DB32818]
http://linked.open...i/riv/nazevZdroje	Investigational New Drugs
http://linked.open...in/vavai/riv/obor	ED
http://linked.open...ichTvurcuVysledku	2 (xsd:int)
http://linked.open...cetTvurcuVysledku	3 (xsd:int)
http://linked.open...UplatneniVysledku	2007
http://linked.open...v/svazekPeriodika	25
http://linked.open...iv/tvurceVysledku	Krejčí, Pavel Wilcox, William R. Pejchalová, Kateřina
http://linked.open...ain/vavai/riv/wos	000247275600013
http://linked.open...n/vavai/riv/zamer	Biophysics of dynamic structures and functions of biological systems Genome and epigenome: 1D and 3D Structure, Dynamics, Interactions with Proteins and Functions Functional and molecular characteristics of cancer and normal stem cells - identification of targets for novel therapeutics and therapeutic strategies
issn	0167-6997
number of pages	5 (xsd:int)
http://bibframe.org/vocab/doi	10.1007/s10637-007-9054-7
http://localhost/t...ganizacniJednotka	14310

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