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Lacosamide, a novel anti-convulsant drug, shows efficacy with a wide safety margin in rodent models for epilepsy
View on Elsevier
A Novel Automated Lazy Learning QSAR (ALL-QSAR) Approach: Method Development, Applications, and Virtual Screening of Chemical Databases Using Validated ALL-QSAR Models
TLDR
An initial success indicates that ALL-QSAR can be further exploited as a general tool for accurate bioactivity prediction and database screening in drug design and discovery.
View on PubMed
Transcription termination factor rho: the site of bicyclomycin inhibition in Escherichia coli.
TLDR
Findings are consistent with the notion that bicyclomycin expresses its activity by interfering with the polyC-dependent ATPase activity of rho.
View on PubMed
Synthesis and anticonvulsant activities of N-Benzyl-2-acetamidopropionamide derivatives.
TLDR
Evaluation of the individual stereoisomers for 18 demonstrated that the principal anticonvulsant activity resided in the (R)-stereoisomer, and this difference in activity for the two stereochemical isomers surpassed comparable values for other members within this class of compounds.
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Quantitative structure-activity relationship analysis of functionalized amino acid anticonvulsant agents using k nearest neighbor and simulated annealing PLS methods.
TLDR
The development of rigorously validated quantitative structure-activity relationship (QSAR) models for 48 chemically diverse functionalized amino acids with anticonvulsant activity were reported, capable of predicting with reasonable accuracy the activity of 13 novel compounds not included in the original dataset.
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The molecular basis for the mode of action of bicyclomycin.
  • H. Kohn, W. Widger
  • Biology, Chemistry
    Current drug targets. Infectious disorders
  • 1 September 2005
TLDR
Together, the structural and functional studies demonstrate how 1, a modest rho inhibitor, can disrupt the rho molecular machinery thereby leading to a catastrophic effect caused by the untimely overproduction of proteins not normally expressed constitutively, thusleading to a toxic effect on the cells.
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Mutations in the Rho Transcription Termination Factor That Affect RNA Tracking*
TLDR
It is concluded that the secondary RNA-tracking site consists of amino acids whose putative orientation faces the central hole in Rho and in part reside in two clusters of positively charged residues located above and below the ATP hydrolysis domain.
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The inefficiency of incisions of ecteinascidin 743-DNA adducts by the UvrABC nuclease and the unique structural feature of the DNA adducts can be used to explain the repair-dependent toxicities of…
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The Antibiotic Bicyclomycin Affects the Secondary RNA Binding Site of Escherichia coli Transcription Termination Factor Rho*
TLDR
The data suggested that the antibiotic binds to Rho, influencing the secondary RNA binding (tracking) site on Rho and slows the tracking of Rho toward the bound RNA polymerase.
View on Publisher
Translational Stroke Research: Vision and Opportunities
TLDR
Pharmacodynamics, pharmacokinetics, and target engagement in the human brain need to be further developed and optimized for stroke interventions so that drug level in brain tissue, time to initiation, and duration of treatment can be accurately measured in clinical trials.
View on Wolters Kluwer
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