58 research outputs found
AMP-activated Protein Kinase α2 Subunit Is Required for the Preservation of Hepatic Insulin Sensitivity by n-3 Polyunsaturated Fatty Acids
Role of Appetite-Regulating Peptides in the Pathophysiology of Addiction: Implications for Pharmacotherapy
PSY27 COST-EFFECTIVENESS OF ANTIGUNGAL PROPHYLAXIS WITH POSACONAZOLE VERSUS STANDARD AZOLE THERAPY IN THE PREVENTION OF INVASIVE FUNGAL INFECTIONS AMONG HIGH RISK HAEMATOLOGY PATIENTS IN CZECH REPUBLIC
PHP86 ADHERENCE OF PHARMACOECONOMIC STUDIES SUBMITTED FOR THE REIMBURSEMENT AND PRICING SYSTEM IN 2008 TO THE CZECH PHARMACOECONOMIC GUIDELINES
PIN27 COST-EFFECTIVENESS OF LINEZOLID VS. VANCOMYCIN AND TEICOPLANIN IN METHICILLIN-RESISTANT STAPHYLOCOCCUS AUREUS INFECTIONS IN CZECH REPUBLIC
PDB24 COST EFFECTIVENESS ANALYSIS OF SWITCHING PATIENTS WITH POORLY CONTROLLED TYPE 2 DIABETES TO BIPHASIC INSULIN ASPART 30 FROM BIPHASIC HUMAN INSULIN 30 IN THE CZECH SETTING
Nucleotide and Glutathione Adducts and DNA Modifications by Cisplatin Analogue [PtCl2(cis-1,4-DACH)].
Cytotoxicity, cellular uptake, glutathione and DNA interactions of an antitumor large-ring PtII chelate complex incorporating the cis-1,4-diaminocyclohexane carrier ligand
International audienceEarlier studies have described promising antitumor activity of a large-ring chelate complex [PtCl(-1,4-DACH)] (DACH = diaminocyclohexane). Encouraging antitumor activity of this analogue of cisplatin prompted us to perform studies focused on the mechanistic basis of pharmacological effects of this complex. Four early steps in the mechanism of biological activity of cisplatin have been delineated: cell entry, reactions with sulfur-containing compounds, platinum–DNA binding along with processing platinated DNA by proteins (enzymes) and DNA repair. Here, we describe comparative experiments (involving also cisplatin) revealing: (i) improved cytotoxicity (3.4 – 5.4-fold) of [PtCl(-1,4-DACH)] in human tumor ovarian cell lines; (ii) enhanced cellular uptake (∼1.5-fold) of [PtCl(-1,4-DACH)]; (iii) somewhat enhanced rate of reactions of [PtCl(-1,4-DACH)] with glutathione (∼1.5-fold), but a similar rate of reactions with metallothionenin-2; (iv) enhanced rate of DNA binding of [PtCl(-1,4-DACH)] in cell-free media (∼2-fold); (v) similar sequence preference of DNA binding of [PtCl(-1,4-DACH)] in cell-free media; (vi) identical DNA interstrand crosslinking efficiency (6%); (vii) similar bending (32 °) and enhanced local unwinding (∼1.5-fold) induced in DNA by the major 1,2-GG-intrastrand crosslink; (viii) markedly enhanced inhibiting effects of DNA adducts of [PtCl(-1,4-DACH)] on processivity of DNA polymerase; and (ix) a slightly lower efficiency of DNA repair systems to remove the adducts of [PtCl(-1,4-DACH)] from DNA
Detection by Elisa Test of Antibodies to Human Papillomavirus (HPV) Type 16 E7 Oncoprotein in Patients with Benign or Malignant Papillomas from Skin or Mucosa
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