Proteomics

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Structurally related hydrazone-based metal complexes with different antitumor activities variably induce apoptotic cell death

ABSTRACT: Three new complexes bearing the tridentate hydrazone-based ligand 2-(2-(1-(pyridin-2-yl)ethylidene)hydrazinyl)pyridine (L) were synthesized and structurally characterized. Biological tests indicate that the Zn(II) complex [ZnCl2(L)] • 0.5 H2O is of low cytotoxicity against the hepatocellular carcinoma cell line HepG2. In contrast, the Cu(II) and Mn(II) complexes [CuCl2(L)] and [MnCl2(L)(OH2)] • H2O are highly cytotoxic with EC50 values of 1.25 0.01 M and 20 1 M, respectively. A quantitative proteome analysis reveals that treatment of the cells with the Cu(II) complex leads to a significantly altered abundance of 102 apoptosis-related proteins, whereas 38 proteins were up- or down-regulated by the Mn(II) complex. A closer inspection of those proteins regulated only by the Cu(II) complex suggests that the superior cytotoxic activity of this complex is likely to be related to an initiation of caspase-independent cell death (CICD).

INSTRUMENT(S): LTQ Orbitrap Elite

ORGANISM(S): Homo Sapiens (human)

TISSUE(S): Cell Culture

SUBMITTER: Dominik Andre Meger  

LAB HEAD: Dominik A. Megger

PROVIDER: PXD005507 | Pride | 2017-05-03

REPOSITORIES: Pride

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Action DRS
OEII15601.mgf Mgf
OEII15601.msf Msf
OEII15601.mzid.gz Mzid
OEII15601.pride.mgf.gz Mgf
OEII15601.pride.mztab.gz Mztab
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Structurally related hydrazone-based metal complexes with different antitumor activities variably induce apoptotic cell death.

Megger Dominik A DA   Rosowski Kristin K   Radunsky Christian C   Kösters Jutta J   Sitek Barbara B   Müller Jens J  

Dalton transactions (Cambridge, England : 2003) 20170401 14

Three new complexes bearing the tridentate hydrazone-based ligand 2-(2-(1-(pyridin-2-yl)ethylidene)hydrazinyl)pyridine (L) were synthesized and structurally characterized. Biological tests indicate that the Zn(ii) complex [ZnCl<sub>2</sub>(L)] is of low cytotoxicity against the hepatocellular carcinoma cell line HepG2. In contrast, the Cu(ii) and Mn(ii) complexes [CuCl<sub>2</sub>(L)] and [MnCl<sub>2</sub>(L)] are highly cytotoxic with EC<sub>50</sub> values of 1.25 ± 0.01 μM and 20 ± 1 μM, resp  ...[more]

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