About: Cytotoxicity, cellular uptake, and DNA interactions of new monodentate ruthenium(II) complexes containing terphenyl arenes

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About: Cytotoxicity, cellular uptake, and DNA interactions of new monodentate ruthenium(II) complexes containing terphenyl arenes Goto Sponge NotDistinct Permalink

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
Description	We have compared the cancer cell cytotoxicity, cell uptake, and DNA binding properties of the isomeric terphenyl complexes [(6-arene)Ru(en)Cl]+, where the arene is ortho- (2), meta- (3), or para-terphenyl (1) (o-, m-, or p-terp). Complex 1, the X-ray crystal structure of which confirms that it has the classical ?piano-stool? geometry, has a similar potency to cisplatin but is not cross-resistant and has a much higher activity than 2 or 3. The extent of Ru uptake into A2780 or A2780cis cells does not correlate with potency. Complex 1 binds to DNA rapidly and quantitatively, preferentially to guanine residues, and causes significant DNA unwinding. Circular and linear dichroism, competitive binding experiments with ethidium bromide, DNA melting, and surface-enhanced Raman spectroscopic data are consistent with combined intercalative and monofunctional (coordination) binding mode of complex 1. This unusual DNA binding mode may therefore make a major contribution to the high potency of complex 1. We have compared the cancer cell cytotoxicity, cell uptake, and DNA binding properties of the isomeric terphenyl complexes [(6-arene)Ru(en)Cl]+, where the arene is ortho- (2), meta- (3), or para-terphenyl (1) (o-, m-, or p-terp). Complex 1, the X-ray crystal structure of which confirms that it has the classical ?piano-stool? geometry, has a similar potency to cisplatin but is not cross-resistant and has a much higher activity than 2 or 3. The extent of Ru uptake into A2780 or A2780cis cells does not correlate with potency. Complex 1 binds to DNA rapidly and quantitatively, preferentially to guanine residues, and causes significant DNA unwinding. Circular and linear dichroism, competitive binding experiments with ethidium bromide, DNA melting, and surface-enhanced Raman spectroscopic data are consistent with combined intercalative and monofunctional (coordination) binding mode of complex 1. This unusual DNA binding mode may therefore make a major contribution to the high potency of complex 1. (en)
Title	Cytotoxicity, cellular uptake, and DNA interactions of new monodentate ruthenium(II) complexes containing terphenyl arenes Cytotoxicity, cellular uptake, and DNA interactions of new monodentate ruthenium(II) complexes containing terphenyl arenes (en)
skos:prefLabel	Cytotoxicity, cellular uptake, and DNA interactions of new monodentate ruthenium(II) complexes containing terphenyl arenes Cytotoxicity, cellular uptake, and DNA interactions of new monodentate ruthenium(II) complexes containing terphenyl arenes (en)
skos:notation	RIV/61989592:15310/08:00005500!RIV10-MSM-15310___
http://linked.open...avai/riv/aktivita	P Z
http://linked.open...avai/riv/aktivity	P(1QS500040581), P(GA203/06/1239), P(IAA400040803), P(KAN200200651), P(LC06030), P(ME08017), P(NR8562), P(OC08003), Z(AV0Z50040507), Z(AV0Z50040702), Z(MSM6198959216)
http://linked.open...iv/cisloPeriodika	17
http://linked.open...vai/riv/dodaniDat	2010
http://linked.open...aciTvurceVysledku	Brabec, Viktor Kašpárková, Jana
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	Univerzita Palackého v Olomouci / Přírodovědecká fakulta
http://linked.open...dnocenehoVysledku	361899
http://linked.open...ai/riv/idVysledku	RIV/61989592:15310/08:00005500
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	DNA interactions; ruthenium; anticancer (en)
http://linked.open.../riv/klicoveSlovo	anticancer DNA interactions ruthenium
http://linked.open...odStatuVydavatele	US - Spojené státy americké
http://linked.open...ontrolniKodProRIV	[C5058A8D90C1]
http://linked.open...i/riv/nazevZdroje	Journal of Medicinal Chemistry
http://linked.open...in/vavai/riv/obor	BO
http://linked.open...ichTvurcuVysledku	2 (xsd:int)
http://linked.open...cetTvurcuVysledku	10 (xsd:int)
http://linked.open...vavai/riv/projekt	Metallodrugs, design and mechansim of action Platinum Metal Complexes as DNA-Protein Cross-Linking Agents Structure, recognition, and processing of DNA damage by metal-based compounds of biological significance Nanoparticulate and supramolecular systems for targeted drug delivery Biomolecular centre Inhibition of telomerase by transition metal complexes. A new concept of antitumor drug design Mechanistic studies related to targeted cancer chemotherapy with light-activated platinum and ruthenium antitumor agents Tolerance and bypass of DNA damage by metal-based anticancer drugs
http://linked.open...UplatneniVysledku	2008
http://linked.open...v/svazekPeriodika	51
http://linked.open...iv/tvurceVysledku	Brabec, Viktor Kašpárková, Jana Zerzánková, Lenka Nováková, Olga Vrána, Oldřich Halámiková, Anna Bugarcic, Tijana Sadler, Peter Habtemariam, Abraha Pardone, Simon
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 Modulation of signalling and regulatory pathways in normal and cancer cells
issn	0022-2623
number of pages	10 (xsd:int)
http://localhost/t...ganizacniJednotka	15310

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