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Statements

Subject Item
n2:RIV%2F00209805%3A_____%2F13%3A%230000426%21RIV14-GA0-00209805
rdf:type
n5:Vysledek skos:Concept
rdfs:seeAlso
http://dx.doi.org/10.1016/j.bmcl.2013.08.046
dcterms: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.
dcterms: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
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
skos:notation
RIV/00209805:_____/13:#0000426!RIV14-GA0-00209805
n5:predkladatel
n6:ico%3A00209805
n3:aktivita
n18:I n18:P
n3:aktivity
I, P(ED2.1.00/03.0101), P(GAP301/11/1678), P(GBP206/12/G151)
n3:cisloPeriodika
20
n3:dodaniDat
n4:2014
n3:domaciTvurceVysledku
n17:9637419 n17:3403149
n3:druhVysledku
n16:J
n3:duvernostUdaju
n20:S
n3:entitaPredkladatele
n8:predkladatel
n3:idSjednocenehoVysledku
58461
n3:idVysledku
RIV/00209805:_____/13:#0000426
n3:jazykVysledku
n9:eng
n3:klicovaSlova
kinase inhibitor; p53 Pathway activation; casein kinase 1; checkpoint kinase 1
n3:klicoveSlovo
n7:p53%20Pathway%20activation n7:kinase%20inhibitor n7:checkpoint%20kinase%201 n7:casein%20kinase%201
n3:kodStatuVydavatele
US - Spojené státy americké
n3:kontrolniKodProRIV
[637594E7D23F]
n3:nazevZdroje
Bioorganic and Medicinal Chemistry Letters
n3:obor
n19:EB
n3:pocetDomacichTvurcuVysledku
2
n3:pocetTvurcuVysledku
9
n3:projekt
n10:GAP301%2F11%2F1678 n10:GBP206%2F12%2FG151 n10:ED2.1.00%2F03.0101
n3:rokUplatneniVysledku
n4:2013
n3:svazekPeriodika
23
n3:tvurceVysledku
Nekulová, Miroslava Vojtěšek, Bořivoj
n3:wos
000324304000021
s:issn
0960-894X
s:numberOfPages
8
n12:doi
10.1016/j.bmcl.2013.08.046