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Specific binding of hoechst 33258 to the d(CGCAAATTTGCG)2 duplex: calorimetric and spectroscopic studies.
TLDR
Molecular interactions, including H-bonding and van der Waals contacts, are found to play only a minor role in stabilizing the resulting complex, a somewhat surprising finding given the emphasis placed on such interactions from structural studies.
Crystal structure of a pentamidine-oligonucleotide complex: implications for DNA-binding properties.
The crystal structure of the complex formed between the dodecanucleotide d(CGCGAATTCGCG)2 and the drug pentamidine, which is active against the Pneumocystis carinii pathogen in AIDS patients, has
Bioactivation of 5-(aziridin-1-yl)-2,4-dinitrobenzamide (CB 1954) by human NAD(P)H quinone oxidoreductase 2: a novel co-substrate-mediated antitumor prodrug therapy.
TLDR
NQO2 is a novel target for prodrug therapy and has a unique activation mechanism that relies on a synthetic co-substrate to activate an apparently latent enzyme, and this agent is synthetically accessible and suitable for further pharmaceutical development.
Intercalative G-Tetraplex Stabilization of Telomeric DNA by a Cationic Porphyrin1
TLDR
Porphyrin binding to DNA sequences from the Oxytricha and human telomeres and a thrombin-binding aptamer is examined by isothermal titration calorimetry (ITC) and spectrophotometry under conditions that favor self-assembly to their respective intermolecular or intramolecular tetraplex structures.
Energetics of DNA intercalation reactions.
TLDR
Analysis showed that the DNA binding behavior of these simple intercalators is driven almost equally by hydrophobic effects and van der Waals contacts within the intercalation site.
Design, synthesis, and evaluation of a novel pyrrolobenzodiazepine DNA-interactive agent with highly efficient cross-linking ability and potent cytotoxicity.
TLDR
A novel sequence-selective pyrrolobenzodiazepine (PBD) dimer 5 (SJG-136) has been developed that comprises two C2-exo-methylene-substituted DC-81 (3) subunits tethered through their C8 positions via an inert propanedioxy linker that is a highly efficient minor groove interstrand DNA cross-linking agent that is 440-fold more potent than melphalan.
Structure of a covalent DNA minor groove adduct with a pyrrolobenzodiazepine dimer: evidence for sequence-specific interstrand cross-linking.
TLDR
This result confirms that template-directed approaches are useful for the design of linked DNA-interactive PBD dimers with viable DNA cross-linking potential and supports recent covalent footprinting studies revealing that this PBDdimer shows a selectivity for embedded base sequences of the type 5'-(pu/py)GATC(py/pu).
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