About: A Casein kinase 1/Checkpoint kinase 1 pyrazolo-pyridine protein kinase inhibitor as novel activator of the p53 pathway

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About: A Casein kinase 1/Checkpoint kinase 1 pyrazolo-pyridine protein kinase inhibitor as novel activator of the p53 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)

Attributes	Values
rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
rdfs:seeAlso	http://dx.doi.org/10.1016/j.bmcl.2013.08.046
Description	Reactivation of the wild-type p53 pathway is one key goal aimed at developing targeted therapeutics in the cancer research field. Although most p53 protein kinases form ´p53-activating´ signals, there are few kinases whose action can contribute to the inhibition of p53, as Casein kinase 1 (CK1) and Checkpoint kinase 1 (CHK1). Here we report on a pyrazolo-pyridine analogue showing activity against both CK1 and CHK1 kinases that lead to p53 pathway stabilisation, thus having pharmacological similarities to the p53-activator Nutlin-3. These data demonstrate the emerging potential utility of multivalent kinase inhibitors. Reactivation of the wild-type p53 pathway is one key goal aimed at developing targeted therapeutics in the cancer research field. Although most p53 protein kinases form ´p53-activating´ signals, there are few kinases whose action can contribute to the inhibition of p53, as Casein kinase 1 (CK1) and Checkpoint kinase 1 (CHK1). Here we report on a pyrazolo-pyridine analogue showing activity against both CK1 and CHK1 kinases that lead to p53 pathway stabilisation, thus having pharmacological similarities to the p53-activator Nutlin-3. These data demonstrate the emerging potential utility of multivalent kinase inhibitors. (en)
Title	A Casein kinase 1/Checkpoint kinase 1 pyrazolo-pyridine protein kinase inhibitor as novel activator of the p53 pathway A Casein kinase 1/Checkpoint kinase 1 pyrazolo-pyridine protein kinase inhibitor as novel activator of the p53 pathway (en)
skos:prefLabel	A Casein kinase 1/Checkpoint kinase 1 pyrazolo-pyridine protein kinase inhibitor as novel activator of the p53 pathway A Casein kinase 1/Checkpoint kinase 1 pyrazolo-pyridine protein kinase inhibitor as novel activator of the p53 pathway (en)
skos:notation	RIV/00209805:_____/13:#0000426!RIV14-GA0-00209805
http://linked.open...avai/riv/aktivita	I P
http://linked.open...avai/riv/aktivity	I, P(ED2.1.00/03.0101), P(GAP301/11/1678), P(GBP206/12/G151)
http://linked.open...iv/cisloPeriodika	20
http://linked.open...vai/riv/dodaniDat	2014
http://linked.open...aciTvurceVysledku	Vojtěšek, Bořivoj Nekulová, Marta
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	Masarykův onkologický ústav
http://linked.open...dnocenehoVysledku	58461
http://linked.open...ai/riv/idVysledku	RIV/00209805:_____/13:#0000426
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	kinase inhibitor; p53 Pathway activation; casein kinase 1; checkpoint kinase 1 (en)
http://linked.open.../riv/klicoveSlovo	casein kinase 1 checkpoint kinase 1 kinase inhibitor p53 Pathway activation
http://linked.open...odStatuVydavatele	US - Spojené státy americké
http://linked.open...ontrolniKodProRIV	[637594E7D23F]
http://linked.open...i/riv/nazevZdroje	Bioorganic and Medicinal Chemistry Letters
http://linked.open...in/vavai/riv/obor	EB
http://linked.open...ichTvurcuVysledku	2 (xsd:int)
http://linked.open...cetTvurcuVysledku	9 (xsd:int)
http://linked.open...vavai/riv/projekt	Center of novel approaches to bioanalysis and molecular diagnostics Regional Centre for Applied Molecular Oncology (RECAMO) The role of the chaperone system in malignant transformation and response to anti-cancer therapy
http://linked.open...UplatneniVysledku	2013
http://linked.open...v/svazekPeriodika	23
http://linked.open...iv/tvurceVysledku	Vojtěšek, Bořivoj Nekulová, Miroslava
http://linked.open...ain/vavai/riv/wos	000324304000021
issn	0960-894X
number of pages	8 (xsd:int)
http://bibframe.org/vocab/doi	10.1016/j.bmcl.2013.08.046

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