Androgen receptor (AR) is essential for the growth and progression of prostate cancer in both hormone-sensitive and hormone-refractory disease. A DNA-binding polyamide that targets the consensus androgen response element binds the prostate-specific antigen (PSA) promoter androgen response element, inhibits androgen-induced expression of PSA and several other AR-regulated genes in cultured prost...

The biodistribution profiles in mice of two pyrrole-imidazole polyamides were determined by PET. Pyrrole-imidazole polyamides are a class of small molecules that can be programmed to bind a broad repertoire of DNA sequences, disrupt transcription factor-DNA interfaces, and modulate gene expression pathways in cell culture experiments. The (18)F-radiolabeled polyamides were prepared by oxime lig...

The weight of a device is an ergonomic criterion as well. Devices that are carried and operated by people may not exceed a weight of 5 kg (11 lbs.). Previously, this was achieved by using lowdensity materials, such as aluminum or polyamide. An additional weight reduction, however, can be obtained through the use of ABS plastics and the FDM process. The density differences of ABS and polyamide d...

The structure of the antifungal metabolite coniothyriomycin was systematically modified by changing the acids of the open chain imide, modification of the hydrophobicity, variation in the degree of saturation, replacement of carbons by nitrogen or oxygen, and incorporation of the open chain molecule into cyclic arrangements. Structure-activity studies showed that antifungal activity was retaine...

We recently developed a new type of pyrrole (Py)-imidazole (Im) polyamide-tetrahydrocyclopropabenzindolone (CBI) conjugate with an indole linker as a stable sequence-specific alkylating agent. In this study, we investigated the gene silencing activities of polyamides A, B and C, which selectively alkylate specific sequences in the promoter region, non-coding strand and coding strand, respective...

This research investigated the direct bonding mechanism of dissimilar materials such as metals and plastic by the conventional hot pressing process. The press area of 4 x 4 mm2 was used for direct bonding. The results of the study showed that titanium was completely bonded to polyamide 66. On the other hand, titanium was not bonded to polystyrene. In the case of bonding material of titanium wit...

The cyclic-imide-hydrolyzing activity of a prokaryotic cyclic-ureide-hydrolyzing enzyme, D-hydantoinase, was investigated. The enzyme hydrolyzed cyclic imides with bulky substituents such as 2-methylsuccinimide, 2-phenylsuccinimide, phthalimide, and 3,4-pyridine dicarboximide to the corresponding half-amides. However, simple cyclic imides without substituents, which are substrates of imidase (i...

Vascular endothelial growth factor (VEGF) and its receptors have been implicated as key factors in tumor angiogenesis that are up-regulated by hypoxia. We evaluated the effects of DNA-binding small molecules on hypoxia-inducible transcription of VEGF. A synthetic pyrrole-imidazole polyamide designed to bind the hypoxia response element (HRE) was found to disrupt hypoxia-inducible factor (HIF) b...