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Statements

Subject Item
n2:RIV%2F00216208%3A11160%2F13%3A10196566%21RIV14-MSM-11160___
rdf:type
n16:Vysledek skos:Concept
rdfs:seeAlso
http://pubs.acs.org/doi/full/10.1021/jm401465m
dcterms:description
The synthetic chemical nuclease, [Cu(1,10-phenanthroline)(2)](2+), has stimulated research within metallonuclease development and in the area of cytotoxic metallodrug design. Our analysis reveals, however, that this agent is %22promiscuous%22 as it binds both dsDNA and protein biomolecules, without specificity, and induces general toxicity to a diversity of cell lineages. Here, we describe the synthesis and characterization of small-molecule metallonucleases containing the redox-active cation, [Cu(RCOO)(1,10-phen)(2)](+), where 1,10-phen = 1,10-phenanthroline and R = -H, -CH3, -C2H5, -CH(CH3)(2), and -C(CH3)(3). The presence of coordinated carboxylate groups in the complex cation functions to enhance dsDNA recognition, reduce serum albumin binding, and offer control of toxicity toward human cancer cells, Gram positive and negative bacteria, and fungal pathogens. The induction of genomic dsDNA breaks (DSBs) were identified in ovarian adenocarcinoma cells using immunodetection of gamma-H2AX. Formate, acetate, and pivalate functionalized complexes induced DSBs in a higher percentage of cells compared with [Cu(1,10-phen)(2)](2+), which supports the importance of inner-sphere modification toward enhancing targeted biological application. The synthetic chemical nuclease, [Cu(1,10-phenanthroline)(2)](2+), has stimulated research within metallonuclease development and in the area of cytotoxic metallodrug design. Our analysis reveals, however, that this agent is %22promiscuous%22 as it binds both dsDNA and protein biomolecules, without specificity, and induces general toxicity to a diversity of cell lineages. Here, we describe the synthesis and characterization of small-molecule metallonucleases containing the redox-active cation, [Cu(RCOO)(1,10-phen)(2)](+), where 1,10-phen = 1,10-phenanthroline and R = -H, -CH3, -C2H5, -CH(CH3)(2), and -C(CH3)(3). The presence of coordinated carboxylate groups in the complex cation functions to enhance dsDNA recognition, reduce serum albumin binding, and offer control of toxicity toward human cancer cells, Gram positive and negative bacteria, and fungal pathogens. The induction of genomic dsDNA breaks (DSBs) were identified in ovarian adenocarcinoma cells using immunodetection of gamma-H2AX. Formate, acetate, and pivalate functionalized complexes induced DSBs in a higher percentage of cells compared with [Cu(1,10-phen)(2)](2+), which supports the importance of inner-sphere modification toward enhancing targeted biological application.
dcterms:title
Regulating Bioactivity of Cu2+ Bis-1,10-phenanthroline Artificial Metallonucleases with Sterically Functionalized Pendant Carboxylates Regulating Bioactivity of Cu2+ Bis-1,10-phenanthroline Artificial Metallonucleases with Sterically Functionalized Pendant Carboxylates
skos:prefLabel
Regulating Bioactivity of Cu2+ Bis-1,10-phenanthroline Artificial Metallonucleases with Sterically Functionalized Pendant Carboxylates Regulating Bioactivity of Cu2+ Bis-1,10-phenanthroline Artificial Metallonucleases with Sterically Functionalized Pendant Carboxylates
skos:notation
RIV/00216208:11160/13:10196566!RIV14-MSM-11160___
n16:predkladatel
n20:orjk%3A11160
n3:aktivita
n12:I
n3:aktivity
I
n3:cisloPeriodika
21
n3:dodaniDat
n4:2014
n3:domaciTvurceVysledku
n19:6556981
n3:druhVysledku
n11:J
n3:duvernostUdaju
n9:S
n3:entitaPredkladatele
n18:predkladatel
n3:idSjednocenehoVysledku
102066
n3:idVysledku
RIV/00216208:11160/13:10196566
n3:jazykVysledku
n17:eng
n3:klicovaSlova
10-phenanthroline; 1; histone H2AX; strand breaks; anticancer activity; copper(II) complexes; DNA-binding; chemical nucleases; in-vitro; cancer-cell-lines; carbon-hydrogen bonds
n3:klicoveSlovo
n10:copper%28II%29%20complexes n10:DNA-binding n10:chemical%20nucleases n10:cancer-cell-lines n10:carbon-hydrogen%20bonds n10:histone%20H2AX n10:in-vitro n10:1 n10:10-phenanthroline n10:strand%20breaks n10:anticancer%20activity
n3:kodStatuVydavatele
US - Spojené státy americké
n3:kontrolniKodProRIV
[135543276866]
n3:nazevZdroje
Journal of Medicinal Chemistry
n3:obor
n15:FR
n3:pocetDomacichTvurcuVysledku
1
n3:pocetTvurcuVysledku
10
n3:rokUplatneniVysledku
n4:2013
n3:svazekPeriodika
56
n3:tvurceVysledku
Howe, Orla McKee, Vickie Kellett, Andrew Rochford, Garret McCann, Malachy Barron, Niall Gathergood, Nicholas Colleran, John Pour, Milan Prisecaru, Andreea
n3:wos
000327111100030
s:issn
0022-2623
s:numberOfPages
17
n14:doi
10.1021/jm401465m
n5:organizacniJednotka
11160