DNA minor groove binders
DNA minor groove binders-inspired by nature
... Two molecules of this compound bind side-by-side in the minor groove however, MGBs containing one or more heterocyclic rings other than pyrrole 100 because of the bulky “isopropyl” of th[r] ...
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Four pyrrole derivatives used as building blocks in the synthesis of minor groove binders
... amido)-N-[2-(morpholin-4-yl)ethyl]-1H-pyrrole-2-carboxamide}, are inter- mediates used in the synthesis of modified DNA minor-groove binders. In all four compounds, the nitro groups lie in the ...
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Four pyrrole derivatives used as building blocks in the synthesis of minor-groove binders
... amido)-N-[2-(morpholin-4-yl)ethyl]-1H-pyrrole-2-carboxamide}, are inter- mediates used in the synthesis of modified DNA minor-groove binders. In all four compounds, the nitro groups lie in the ...
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Entropic binding mode preference in cooperative homo-dimeric drug-DNA recognition
... molecule DNA minor groove binders (MGBs), involving the formation of a dimer in free solution followed by the binding of that dimer to DNA, which contrasts with the sequential or ...
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Minor groove binders: some recent research in drug development
... for DNA specific ...the minor groove of DNA at regions with four or five AT base pairs, ...for DNA and at the same time should have sequence selectivity so that these new compounds can ...
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The antibacterial drug MGB-BP3 : from discovery to clinical trial
... Strathclyde minor groove binders against other infectious organisms, particularly parasites, was also being ...effective minor groove binders did not show toxicity to the animals ...
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An evaluation of minor groove binders as anti-fungal and anti-mycobacterial therapeutics
... troublesome cell walls because it generates dicationic MGBs. The systematic structural variations in this study examine whether the inclusion of lipophilic moieties, such as thiazoles and alkyl side chains, are important ...
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An evaluation of minor groove binders as anti-Trypanosoma brucei brucei therapeutics
... At Strathclyde we have developed a collection of MGBs which are structurally based on the natural product distamycin. This compound is built from N-methylpyrrole amino acid amides and has an amidine end group (Fig. 2). ...
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Minor groove binders for DNA as antitypanosomal agents : the veterinary context
... to minor groove binding drugs from Strathclyde (S-MGBs) which is important because compounds useful in the field must have activity across the range of infectious species so that ...
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An evaluation of minor groove binders as anti-lung cancer therapeutics
... groove of the DNA where the drug interferes with the genetic transcription. These modifications result in variations in the product from crucial genes involved in cell-cycle replications and finally induce ...
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Design, synthesis and antibacterial activity of minor groove binders: the role of non-cationic tail groups
... to DNA but also penetration of the bacterial cell ...this minor groove binder rather than any intrinsic property of the ...Nevertheless, minor groove binders with both ...
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Ranking ligand affinity for the DNA minor groove by experiment and simulation
... the DNA minor groove it has become possible to develop tailored approaches to drug ...with DNA specificities and affinities comparable to DNA-binding proteins and have allowed ...
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Dinuclear polypyridyl ruthenium(II) complexes as stereoselective probes of nucleic acid secondary structures
... unique DNA sequence in the human genome would require an incredibly complex drug able to recognise a sequence of some 15-16 bases † ...acid binders in use today. These ligands are typically polyamide ...
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Thiazotropsin aggregation and its relationship to molecular recognition in the DNA minor groove
... the DNA minor groove and classical small molecule DNA binders including Hoechst 33258 [1-234567] berenil [8,9] netropsin [10] distamycin A [11,12] and their derivatives ( ...peptide ...
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Superresolution imaging of single DNA molecules using stochastic photoblinking of minor groove and intercalating dyes
... phage DNA ( DNA) is a double-stranded template of 48,502 base pai rs with 12 base pair single stranded ‘sticky ends’ that allow for base-pairing type modifications at each ...and DNA repair ([10]). ...
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Comparative effects of A.T and G.C sequence selective DNA minor groove binding agents
... of DNA cleavage over a wide range of ligand ...involving minor groove binders and DNA processing enzymes demonstrate inhibition of the proteins, there are some reports of an increase in ...
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Sequence-selective minor groove recognition of a DNA duplex containing synthetic genetic components
... impact minor groove ...other minor groove binders such as Hoechst33258 in complex with A-tract dsDNA ...uences groove width but also reduces allosteric modulation in a DNA ...
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2D-IR spectroscopy shows that optimised DNA minor groove binding of Hoechst33258 follows an induced fit model
... of DNA is the anti-parallel helix where the major and minor grooves provide sites for sequence-selective binding of proteins and small ...double-stranded DNA (dsDNA) sequences by transcription ...
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Selectivity in anti-infective minor groove binders
... feature that determines selectivity is access of the S-MGB to the DNA of the target organism which requires passing through the external cell membrane or cell wall. Experiments have shown that S-MGBs containing ...
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Why antibacterial minor groove binders are a good thing
... MGB-BP-3 is a lipophilic molecule that is known to undergo self-association in aqueous solution. Self association of MGB-BP-3 and its relatives has been studied in detail by NMR spectroscopy (Parkinson et.al. Med. Chem. ...
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