Hairpin polyamides are synthetic oligomers that fold and bind to specific DNA sequences in a programmable manner. Internal side-by-side pairings of the aromatic amino acids N-methylpyrrole (Py), N-methylimidazole (Im), and Nmethylhydroxypyrrole (Hp) confer the ability to distinguish between all four WatsonCrick base pairs in the minor groove of B-form DNA. In a broad search to expand the hetero...

Enzymes are powerful tools in organic synthesis that are able to catalyse a wide variety of selective chemical transformations under mild and environmentally friendly conditions. Enzymes such as the lipases have also found applications in the synthesis and degradation of polymeric materials. However, the use of these natural catalysts in the synthesis and the post-synthetic modification of dend...

The use of urinary and/or biliary excretion data was considered as an alternative approach if the bioanalytical method lacked the appropriate sensitivity to adequately characterize the serum or plasma concentration-time profile. This approach is used for the analysis of plasma concentration-time profile under the lower limit of quantification (LLOQ) of various analytical instruments. The object...

Fluorescent methods for the sequence specific detection of DNA are vital to unraveling the functional, three-dimensional significance of the linear human genome. The ability of minor groove-binding polyamides to specifically target predetermined DNA sequences, without sample denaturation, in biologically relevant condensed states and protein complexes, offers appreciable advantages relative to ...

In this paper, we demonstrate the use of synthetic polyamide probes to fluorescently label heterochromatic regions on human chromosomes for discrimination in cytogenetic preparations and by flow cytometry. Polyamides bind to the minor groove of DNA in a sequence-specific manner. Unlike conventional sequence-specific DNA or RNA probes, polyamides can recognize their target sequence without the n...

BACKGROUND Three-ring polyamides containing N-methylimidazole and N-methylpyrrole amino acids bind sequence-specifically to double-helical DNA by forming side-by-side complexes in the minor groove. Simple pairing rules relate the amino-acid sequence of a pyrrole-imidazole polyamide to its expected DNA target site, and polyamides that target a wide variety of DNA sequences have been synthesized....

Polyamides composed of four amino acids, imidazole (Im), pyrrole (Py), hydroxypyrrole (Hp), and beta-alanine (beta), are synthetic ligands that form highly stable complexes in the minor groove of DNA. Although specific pairing rules within the 2:1 motif can be used to distinguish the four Watson. Crick base pairs, a comparable recognition code for 1:1 polyamide:DNA complexes had not been descri...

Pyrrole-imidazole (Py-Im) polyamides are a class of programmable DNA minor groove binders capable of modulating the activity of DNA-binding proteins and affecting changes in gene expression. Estrogen receptor alpha (ERα) is a ligand-activated hormone receptor that binds as a homodimer to estrogen response elements (ERE) and is a driving oncogene in a majority of breast cancers. We tested a sele...

The discrimination of the four Watson-Crick base pairs by minor groove DNA-binding polyamides have been attributed to the specificity of three five-membered aromatic amino acid subunits, 1-methyl-1H-imidazole (Im), 1-methyl-1H-pyrrole (Py), and 3-hydroxy-1H-pyrrole (Hp) paired four different ways. The search for additional ring pairs that demonstrate DNA-sequence specificity has led us to a new...

Aliphatic polyamides (nylons) constitute a family of polymers with outstanding properties and multiple applications. Despite the intensive research studies carried out nylons, there are still unsolved questions concerning crystallization processes, crystalline structures, polymorphic transitions, morphologies. Constrains imposed by strong intermolecular interactions affect amorphous state, rigi...