many anticancer drugs in clinical use interact with dna through intercalation, which is process that starts with the transfer of the intercalating molecule from an aqueous environment to the hydrophobic space between two adjacent dna base pairs. in general, intercalatig agents are two types: monofunctional and bifunctional. monofunctional intercalators contain one intercalating unit and bifunct...

A novel bimetallic conjugate combining a rhodium intercalator that selectively binds DNA mismatches and a reactive cis-platinum analogue that targets DNA by coordination has been prepared. The site-selectivity of the bimetallic complex in forming coordination adducts is examined using mismatched and well-matched oligonucleotides of different sequences. The results indicate that through the bifu...

Many anticancer drugs in clinical use interact with DNA through intercalation, which is process that starts with the transfer of the intercalating molecule from an aqueous environment to the hydrophobic space between two adjacent DNA base pairs. In general, intercalatig agents are two types: monofunctional and bifunctional. Monofunctional intercalators contain one intercalating unit and Bifunct...

Many anticancer drugs in clinical use interact with DNA through intercalation, which is process that starts with the transfer of the intercalating molecule from an aqueous environment to the hydrophobic space between two adjacent DNA base pairs. In general, intercalatig agents are two types: monofunctional and bifunctional. Monofunctional intercalators contain one intercalating unit and Bifunct...

A conjugate of a DNA mismatch-specific rhodium intercalator, containing the bulky chrysenediimine ligand, and an aniline mustard has been prepared, and targeting of mismatches in DNA by this conjugate has been examined. The preferential alkylation of mismatched over fully matched DNA is found by a mobility shift assay at concentrations where untethered organic mustards show little reaction. The...

A b s t r a c t . Oligonucleotides can be designed to bind to oligopurine.oligopyrimidine sequences of double-helical DNA. Binding occurs in the major groove and a triple helix is formed. Bifunctional oligonucleotide-intercalator conjugates have an increased affinity due to intercalation either at the triplex-duplex junction or within the triple-helical structure. Some intercalating agents can ...

We have examined the binding of luzopeptin, an antitumor antibiotic, to five DNA fragments of varying base composition. The drug forms a tight, possibly covalent, complex with the DNA causing a reduction in mobility on nondenaturing polyacrylamide gels and some smearing of the bands consistent with intramolecular cross-linking of DNA duplexes. DNAase I and micrococcal nuclease footprinting expe...

Ditercalinium, an antitumor bifunctional intercalator which forms a high affinity reversible complex with DNA, was found to be specifically cytotoxic for polA and lig7 E. coli strains. In the polA strain, the cytotoxic effect of ditercalinium was suppressed by the uvrA mutation. DNA single strand breaks accumulated in presence of ditercalinium at high temperature in lig7 strains but not in polA...