About: Arylazopyrazole AAP1742 Inhibits CDKs and Induces Apoptosis in Multiple Myeloma Cells via Mcl-1 Downregulation

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About: Arylazopyrazole AAP1742 Inhibits CDKs and Induces Apoptosis in Multiple Myeloma Cells via Mcl-1 Downregulation Goto Sponge NotDistinct Permalink

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
rdfs:seeAlso	http://gateway.isiknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=Alerting&SrcApp=Alerting&DestApp=MEDLINE&DestLinkType=FullRecord&UT=24803299
Description	Inhibitors of cyclin-dependent kinases 9 have been developed as potential anticancer drugs for the treatment of multiple myeloma. We have previously prepared a library of arylazo-3,5-diaminopyrazole inhibitors of CDKs. Here, we describe a novel member, AAP1742 (CDK9 inhibition with IC50 =0.28mum), that reduces the viability of multiple myeloma cell lines in low micromolar concentrations. Consistent with inhibition of CDK9, AAP1742 decreases the phosphorylation of RNA polymerase II and inhibits mRNA synthesis of anti-apoptotic proteins Mcl-1, Bcl-2, and XIAP, followed by apoptosis in the RPMI-8226 cell line in a dose- and a time-dependent manner. These results are consistent with the biochemical profile of AAP1742 and further suggest cellular inhibition of CDK9 as a possible target for anticancer drugs. Inhibitors of cyclin-dependent kinases 9 have been developed as potential anticancer drugs for the treatment of multiple myeloma. We have previously prepared a library of arylazo-3,5-diaminopyrazole inhibitors of CDKs. Here, we describe a novel member, AAP1742 (CDK9 inhibition with IC50 =0.28mum), that reduces the viability of multiple myeloma cell lines in low micromolar concentrations. Consistent with inhibition of CDK9, AAP1742 decreases the phosphorylation of RNA polymerase II and inhibits mRNA synthesis of anti-apoptotic proteins Mcl-1, Bcl-2, and XIAP, followed by apoptosis in the RPMI-8226 cell line in a dose- and a time-dependent manner. These results are consistent with the biochemical profile of AAP1742 and further suggest cellular inhibition of CDK9 as a possible target for anticancer drugs. (en)
Title	Arylazopyrazole AAP1742 Inhibits CDKs and Induces Apoptosis in Multiple Myeloma Cells via Mcl-1 Downregulation Arylazopyrazole AAP1742 Inhibits CDKs and Induces Apoptosis in Multiple Myeloma Cells via Mcl-1 Downregulation (en)
skos:prefLabel	Arylazopyrazole AAP1742 Inhibits CDKs and Induces Apoptosis in Multiple Myeloma Cells via Mcl-1 Downregulation Arylazopyrazole AAP1742 Inhibits CDKs and Induces Apoptosis in Multiple Myeloma Cells via Mcl-1 Downregulation (en)
skos:notation	RIV/61389030:_____/14:00433741!RIV15-GA0-61389030
http://linked.open...avai/riv/aktivita	I P
http://linked.open...avai/riv/aktivity	I, P(GA14-19590S), P(GAP305/12/0783), P(LO1204)
http://linked.open...iv/cisloPeriodika	4
http://linked.open...vai/riv/dodaniDat	2015
http://linked.open...aciTvurceVysledku	Jorda, Radek Kryštof, Vladimír Strnad, Miroslav Navrátilová, Jana Hušková, Zlata
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	Ústav experimentální botaniky AV ČR, v. v. i.
http://linked.open...dnocenehoVysledku	4162
http://linked.open...ai/riv/idVysledku	RIV/61389030:_____/14:00433741
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	CAN508; cyclin-dependent kinase; inhibitor (en)
http://linked.open.../riv/klicoveSlovo	cyclin-dependent kinase inhibitor CAN508
http://linked.open...odStatuVydavatele	GB - Spojené království Velké Británie a Severního Irska
http://linked.open...ontrolniKodProRIV	[878CA72D3A4D]
http://linked.open...i/riv/nazevZdroje	Chemical Biology & Drug Design
http://linked.open...in/vavai/riv/obor	EB
http://linked.open...ichTvurcuVysledku	5 (xsd:int)
http://linked.open...cetTvurcuVysledku	7 (xsd:int)
http://linked.open...vavai/riv/projekt	Evaluation of cyclin-dependent kinase inhibitors in cancer cell lines with specific genetic alterations Udržitelný rozvoj výzkumu v Centru regionu Haná Modulation od cyclin-dependent kinases in haematological malignancies
http://linked.open...UplatneniVysledku	2014
http://linked.open...v/svazekPeriodika	84
http://linked.open...iv/tvurceVysledku	Jorda, Radek Kryštof, Vladimír Navrátilová, Jana Strnad, Miroslav Cankař, P. Hušková, Zlata Schütznerová, E.
http://linked.open...ain/vavai/riv/wos	000342978400003
issn	1747-0277
number of pages	7 (xsd:int)
http://bibframe.org/vocab/doi	10.1111/cbdd.12330

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