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Identification of the first specific inhibitor of p90 ribosomal S6 kinase (RSK) reveals an unexpected role for RSK in cancer cell proliferation.
TLDR
It is shown that RSK has an unexpected role in proliferation of transformed cells and may be a useful new target for chemotherapeutic agents and SL0101 will provide a powerful new tool to dissect the molecular functions of RSK in cancer cells. Expand
Bleomycin: new perspectives on the mechanism of action.
  • S. Hecht
  • Biology, Medicine
  • Journal of natural products
  • 2000
The bleomycin group antitumor antibiotics have long been of interest as a consequence of their efficacy in the treatment of certain tumors, not to mention their unique structures and properties inExpand
On the mechanism of topoisomerase I inhibition by camptothecin: evidence for binding to an enzyme-DNA complex.
TLDR
Results are consistent with a model in which camptothecin reversibly traps an intermediate involved in DNA unwinding by topoisomerase I and thereby perturbs a set of equilibria, resulting in increased DNA cleavage. Expand
Site-specific cleavage of RNA by Fe(II).bleomycin.
TLDR
RNA cleavage was oxidative, approximately 10-fold more selective than DNA cleavage, and largely unaffected by nonsubstrate RNAs; subsets of nucleotides at the junction of single- and double-stranded regions were especially susceptible to cleavage. Expand
Does oxidative stress contribute to the pathology of Friedreich's ataxia? A radical question
TLDR
It is concluded that oxidative stress does constitute a major contributing factor to FRDA pathology and reaffirms the idea that the rational design of specific small molecule multifunctional antioxidants will benefit FRDA patients. Expand
Identification of Small Molecule Synthetic Inhibitors of DNA Polymerase β by NMR Chemical Shift Mapping*
TLDR
NMR-based mapping techniques can be used in the design of small molecule enzyme inhibitors including those with potential use in a clinical setting, as illustrated by the results of β-pol null mouse fibroblasts. Expand
Eukaryotic mRNA cap binding protein: purification by affinity chromatography on sepharose-coupled m7GDP.
A 24,000-dalton polypeptide that binds strongly and can be specifically crosslinked to the 5'-terminal cap structure m7GpppN in eukaryotic mRNAs has been detected in protein synthesis initiationExpand
Camptothecin: current perspectives.
TLDR
This review summarizes the current status of studies of the mechanism of action of camptothecin, including topoisomerase I inhibition and additional cellular responses, and a systematic evaluation of novel and important analogues of camPTothecin and their contribution to the current structure-activity profile are considered. Expand
Mechanistic plasticity of DNA topoisomerase IB: phosphate electrostatics dictate the need for a catalytic arginine.
TLDR
Findings underscore the importance of transition-state electrostatics in determining the composition of the active site and dictating the balance between strand transferase and hydrolase functions. Expand
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