[PDF] Top 20 Biological Activity of Pyrrole-Imidazole Polyamides in vivo

... Effects on tumor size Although there are no published reports on the growth of T47D-KBluc xenografts in mice, data from parental T47D xenografts show a slow, linear growth pattern rather than exponential (48). To better ... See full document

... biological activity. Some of the pub- lished studies, both in vitro and in vivo, show negative effects of exposure to manganese, mainly on the nervous system, whereas other data suggest that it is ... See full document

... -aryl polyamides show decreased solubility relative to β - amino compounds owing to their reduced charge at physiological ...Py-Im polyamides on gene expression in living ...in vivo, and thereby ... See full document

... in vivo, and suggest that this non-toxic antagonist could be used to block AHR activity either induced acutely by environmental ligands or chronically during a variety of pathological ... See full document

... enzyme activity or disrupt binding enjoy a large degree of commercial success, pyrrole-imidazole polyamides (“PIPs”) and their accurate DNA base pair recognition [ 1 – 5 ] provide a promising ... See full document

... 71 4.1 Introduction In order for DNA-binding molecules to be useful tools for gene regulation, they must be able to access DNA in biological systems. DNA in eukaryotic organisms exists in a highly condensed form ... See full document

... RCS-binding polyamides targeted to the HIV LTR can inhibit LSF binding to the RCS in vitro and can increase expression of the ...system. Pyrrole-imidazole poly- amides, which are synthetic ... See full document

... been synthesized to pursue higher specificity with the aim of realizing the great potential of such compounds in biological and clinical areas. Among several types of PIPs, we designed and synthesized hairpin and ... See full document

... antitumor activity of three different alkylating ImPy cisplatin, and nitrogen mustards, and they are routinely diamide conjugates 1–3 utilizing high-resolution dena- used in ...antitumor activity of ... See full document

... Abstract Pyrrole-Imidazole (Py-Im) polyamides are programmable, sequence specific DNA minor groove binding ...various polyamides can be used to modulate the transcriptional programs of ... See full document

... 15. Johnston HJ, Hutchison GR, Christensen FM, Aschberger K, Stone V (2010) The biological mechanisms and physicochemical characteristics responsible for driving fullerene toxicity. Toxicol Sci 114:162 – 182 16. ... See full document

... with activity against enzalutamide-resistant CaP in cell and animal ...transcriptional activity, is more potent than enzalutamide and bicalutamide in cell culture, and is active against enzalutamide ... See full document

... medicine. Pyrrole-imidazole polyamides are a class of synthetic ligands that can be programmed to bind the minor groove of specific DNA ...Py-Im polyamides can be programmed to bind a large ... See full document

... alkylating activity of four Py–Im polyamide conjugates in targeting the KRAS codon 12 G12D and G12V mutation ...Py–Im polyamides displayed high reactivity for the target site; conjugate 4 displayed the ... See full document

... retain activity against enzalutamide- resistant prostate cancers where ligand binding domain antagonists are ...A pyrrole-imidazole (Py-Im) polyamide designed to bind the consensus androgen response ... See full document

... Pyrrole-Imidazole polyamides (PAs) are a family of minor groove binding ligands which have proven ability to organize non-natural functionality along DNA nanostructures with high affinity and ... See full document

... Minor -groove binding transcription factors, such as TBP (Figure 1.3), LEF-l, and TAX, have been excellent targets for polyamide inhibition, resulting in inhibition of RNA [r] ... See full document

... and biological methods to control directly expression of selected endogenous genes could have broad implications for human ...interaction. Polyamides containing N-methylimidazole (Im) and N-methylpyrrole ... See full document

... Keywords: Imidazole, Heterocyclic Ring, Biological activity. INTRODUCTION During the past decade, the concept of Imidazoline (I) receptors has been developed and gained consensus. Different rank ... See full document

... 3.1 Introduction The previous chapter detailed the evidence for polyamide-induced replication stress in an asynchronous population of DU145 human prostate carcinoma cells (1). This low-level stress was sufficient to ... See full document