DNA nanotechnology offers the potential for the creation of molecular assemblies with nanometer scale resolution. Although DNA provides an ideal material for the construction of 2-dimensional and 3-dimensional assemblies it lacks the functionality needed for many desired applications. Pyrrole-imidazole polyamides capable of programmable binding to specific DNA sequences provide a unique solutio...

Pyrrole-imidazole (Py-Im) polyamides are high affinity DNA-binding small molecules that can inhibit protein-DNA interactions. In VCaP cells, a human prostate cancer cell line overexpressing both AR and the TMPRSS2-ERG gene fusion, an androgen response element (ARE)-targeted Py-Im polyamide significantly downregulates AR driven gene expression. Polyamide exposure to VCaP cells reduced proliferat...

RNA polymerase II (pol II) encounters numerous barriers during transcription elongation, including DNA strand breaks, DNA lesions, and nucleosomes. Pyrrole-imidazole (Py-Im) polyamides bind to the minor groove of DNA with programmable sequence specificity and high affinity. Previous studies suggest that Py-Im polyamides can prevent transcription factor binding, as well as interfere with pol II ...

The wide use of thermoplastics has put higher demands on designers to conduct more accurate and increasingly sophisticated analysis of materials in order to ensure the performance of the molded parts under the end-use conditions characterized by varying humidity, temperature, and dynamic load or deformation. One of the key aspects in thermoplastic analysis is to apply correct material property ...

Three-ring polyamides containing pyrrole (Py) and imidazole (Im) amino acids covalently coupled by γ-aminobutyric acid (γ) form six-ring hairpins that recognize five-base-pair sequences in the minor groove of DNA. Selective chiral substitution of the “γ-turn” enhances the properties of polyamide hairpins with regard to DNA affinity and sequence specificity. Polyamides of core sequence compositi...

N-Methylpyrrole (Py)-N-methylimidazole (Im) polyamides are small organic molecules that can recognize predetermined DNA sequences with high sequence specificity. As many eukaryotic promoter regions contain highly GC-rich sequences, it is valuable to synthesize and characterize Py-Im polyamides that recognize GC-rich motifs. In this study, we synthesized four hairpin Py-Im polyamides 1-4, which ...

(54) POLYAMIDES FOR NUCLEICACID CI2N IS/II (2006.01) DELIVERY A 6LX 3L/705 (2006.01) C7H 2L/04 (2006.01) (76) Inventor: Theresa M. Reineke, Blacksburg, C08G 69/48 (2006.01) VA (US) C08G 63/9. (2006.01) C7H 2L/02 (2006.01) Correspondence Address: A63L/7II (2006.01) DINSMORE & SHOHL, LLP CI2N IS/00 (2006.01) 1900 CHEMED CENTER, 255 EAST FIFTH A63L/7088 (2006.01) STREET CINCINNATI, OH 45202 (US) (...

We describe the identification of small-molecule G-quadruplex ligands using a direct ELISA screen of a one-bead-one-compound library of unnatural polyamides displayed on a branched linker with a biotin tag. This general purpose parallel screen for small molecule-oligonucleotide interactions was validated by surface plasmon resonance and ELISA of resynthesized compounds. Linear polyamides displa...