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Characterization and Structural Analysis of Novel Mutations in Human Immunodeficiency Virus Type 1 Reverse Transcriptase Involved in the Regulation of Resistance to Nonnucleoside Inhibitors
Mutations beyond those currently known to confer resistance should be considered for a better prediction of clinical response to reverse transcriptase inhibitors and for the development of more efficient new-generation NNRTIs.
Chalcones: a valid scaffold for monoamine oxidases inhibitors.
The docking technique provided new insight on the inhibition mechanism and the rational drug design of more potent/selective hMAO inhibitors based on the chalcone scaffold.
SI113, a SGK1 inhibitor, potentiates the effects of radiotherapy, modulates the response to oxidative stress and induces cytotoxic autophagy in human glioblastoma multiforme cells
SGK1 is over-expressed in highly malignant gliomas and that the treatment with SI113 leads to a significant increase in caspase-mediated apoptotic cell death in GBM cell lines but not in normal fibroblasts, suggesting a new therapeutic strategy either alone or in combination with radiotherapy.
HCV Genotypes Are Differently Prone to the Development of Resistance to Linear and Macrocyclic Protease Inhibitors
Background Because of the extreme genetic variability of hepatitis C virus (HCV), we analyzed whether specific HCV-genotypes are differently prone to develop resistance to linear and macrocyclic…
Hepatitis C Virus Genetic Variability and the Presence of NS5B Resistance-Associated Mutations as Natural Polymorphisms in Selected Genotypes Could Affect the Response to NS5B Inhibitors
- V. D. di Maio, V. Cento, F. Ceccherini‐Silberstein
- BiologyAntimicrobial Agents and Chemotherapy
- 3 March 2014
The genetic variability among HCV genotypes, particularly with the presence of polymorphisms at NNI resistance positions, could affect their responsiveness to NS5B inhibitors and help to provide patients with the full efficacy of NNI-containing regimens.
The mechanisms of pharmacokinetic food-drug interactions - A perspective from the UNGAP group.
Quercetin as the active principle of Hypericum hircinum exerts a selective inhibitory activity against MAO-A: extraction, biological analysis, and computational study.
The methanol extract from Hypericum hircinum leaves exhibited in vitro inhibition of monoamine oxidases (MAO) and quercetin was the only compound with a selective inhibitory activity against MAO-A, with an IC50 value of 0.010 microM.
N-myristoylation determines dual targeting of mammalian NADH-cytochrome b(5) reductase to ER and mitochondrial outer membranes by a mechanism of kinetic partitioning
It is found that myristoylation interferes with interaction of the nascent chain with signal recognition particle, so that a portion of the fledgling chains escapes from cotranslational integration into the ER and can be post-translationally targeted to the mitochondrial outer membrane.
A new series of flavones, thioflavones, and flavanones as selective monoamine oxidase-B inhibitors.
GBPM: GRID-based pharmacophore model: concept and application studies to protein-protein recognition
The GBPM capability to identify interaction areas in complexes deriving pharmacophore models from three-dimensional molecular structure information is evaluated and the results obtained show the capabilities of this new bioinformatic method.