摘要:
The present invention relates to the use of analogs of creatine, such as cyclocreatine, as antiviral agents. Analogs of creatine can be used as antiviral agents against a variety of viruses, particularly DNA viruses, such as Herpes viruses (e.g., HSV-1, HSV-2, cytomegaloviruses, Varicella-Zoster virus) and adenovirus. The invention further relates to creatine analogs including four classes of creatine analogs selected as candidate antiviral compounds: (1) creatine analogs that can be phosphorylated by creatine kinase but differ in their phosphoryl group transfer potential, (2) bisubstrate inhibitors of creatine kinase comprising covalently linked structural analogs of adenosine triphosphate (ATP) and creatine, (3) creatine analogs which can act as irreversible inhibitors of creatine kinase, and (4) N-phosphorocreatine analogs bearing non-transferable moieties which mimic the N-phosphoryl group.
摘要:
A method of inhibiting growth, transformation and/or metastasis of mammalian cells, particularly epithelial cells, in which activity of at least one enzyme, which participates in purine metabolism or regulation of nucleotide levels or the relative ratios of their phosphorylated states, is elevated. In particular, a method of inhibiting transformation, growth and/or metastasis of mammalian cells in which a DNA tumor virus, a DNA tumor virus factor or other factor which has an equivalent effect on cells has acted.
摘要:
The present invention provides methods for high-throughput screening for bioactive compounds, in particular those that bind to RNA sequences involved in the pathogenesis of disease or in regulation of a physiological function. The methods involve measuring the conformation of an RNA target in the presence and absence of test ligands, and identifying as a ligand any test ligand that causes a measurable change in target RNA conformation.
摘要:
The present invention provides methods for screening for bioactive compounds, in particular those that bind to RNA sequences involved in the pathogenesis of disease or in regulation of a physiological function. The methods involve assessing the stability and/or the conformation of an RNA target in the presence and absence of test ligands, and identifying as a ligand any test ligand that causes a measurable change in target RNA stability and/or conformation. In a preferred embodiment, the effect of a ligand on target RNA stability and/or conformation is assessed by measuring the fluorescence polarization of a fluorescently labeled probe.
摘要:
The present invention provides methods for screening for bioactive compounds, in particular those that bind to RNA sequences involved in the pathogenesis of disease or in regulation of a physiological function. The methods involve assessing the stability and/or the conformation of an RNA target in the presence and absence of test ligands, and identifying as a ligand any test ligand that causes a measurable change in target RNA stability and/or conformation. In a preferred embodiment, the effect of a ligand on target RNA stability and/or conformation is assessed by measuring the fluorescence polarization of a fluorescently labeled probe.
摘要:
The present invention provides methods for high-throughput screening for bioactive compounds, in particular those that bind to RNA sequences involved in the pathogenesis of disease or in regulation of a physiological function. The methods involve measuring the conformation of an RNA target in the presence and absence of test ligands, and identifying as a ligand any test ligand that causes a measurable change in target RNA conformation.