Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.3109/08039487109094663 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Identification of kinase inhibitors that rule out the CYP27B1-mediated activation of vitamin D: an integrated machine learning and structure-based drug designing approach.
Mol Divers
August 2021
Molecular Modeling Lab, Department of Pharmaceutical Sciences and Drug Research, Punjabi University Patiala, Patiala, Punjab, 147002, India.
CYP27B1, a cytochrome P450-containing hydroxylase enzyme, converts vitamin D precursor calcidiol (25-hydroxycholecalciferol) to its active form calcitriol (1α,25(OH)D). Tyrosine kinase inhibitor such as imatinib is reported to interfere with the activation of vitamin D by inhibiting CYP27B1 enzyme. Consequently, there is a decrease in the serum levels of active vitamin D that in turn may increase the relapse risk among the cancer patients treated with imatinib.
View Article and Find Full Text PDFComparison of cerebral Open Flow Microperfusion and Microdialysis when sampling small lipophilic and small hydrophilic substances.
J Neurosci Methods
January 2019
JOANNEUM RESEARCH Forschungsgesellschaft mbH, HEALTH - Institute for Biomedicine and Health Sciences, Neue Stiftingtalstraße 2, 8010 Graz, Austria. Electronic address:
Background: Assessment of drug concentration in the brain interstitial fluid (ISF) is crucial for development of brain active drugs, which are mainly small, lipophilic substances able to cross the blood-brain barrier (BBB). We aimed to compare the applicability of cerebral Open Flow Microperfusion (cOFM) and Microdialysis (MD) to sample the lipophilic substance amitriptyline (AMI), its metabolites Hydroxyamitriptyline (HYA), Nortriptyline (NOR), Amitriptyline-N-Oxide (ANO), deuterated water (DO) and the hydrophilic substance sodium fluorescein (Naf) in brain ISF. NEW METHOD: cOFM has been refined to yield increased spatial resolution and performance.
View Article and Find Full Text PDFWhat is the contribution of human FMO3 in the N-oxygenation of selected therapeutic drugs and drugs of abuse?
Toxicol Lett
September 2016
Department of Experimental and Clinical Toxicology, Saarland University, Homburg, Germany. Electronic address:
Little is known about the role of flavin-containing monooxygenases (FMOs) in the metabolism of xenobiotics. FMO3 is the isoform in adult human liver with the highest impact on drug metabolism. The aim of the presented study was to elucidate the contribution of human FMO3 to the N-oxygenation of selected therapeutic drugs and drugs of abuse (DOAs).
View Article and Find Full Text PDFInvestigations into sample preparation procedures usually focus on analyte recovery with no information provided about the fate of other components of the sample (matrix). For many analyses, however, and particularly those using liquid chromatography-mass spectrometry (LC-MS), quantitative measurements are greatly influenced by sample matrix. Using the example of the drug amitriptyline and three of its metabolites in serum, we performed a comprehensive investigation of nine commonly used sample clean-up procedures in terms of their suitability for preparing serum samples.
View Article and Find Full Text PDFThe mitochondrial amidoxime reducing component (mARC): involvement in metabolic reduction of N-oxides, oximes and N-hydroxyamidinohydrazones.
ChemMedChem
October 2014
Pharmaceutical Institute, Department of Pharmaceutical & Medicinal Chemistry, Christian-Albrechts-Universität zu Kiel, Gutenbergstrasse 76, 24188 Kiel (Germany).
The mitochondrial amidoxime reducing component (mARC) is a molybdenum-containing enzyme and capable of reducing N-hydroxylated structures such as amidoxime prodrugs. In this study, we tested the involvement of mARC in the reduction of N-oxides (amitriptyline-N-oxide, nicotinamide-N-oxide), oximes ((E)-/(Z)-2,4,6-trimethylacetophenonoxime) and a N-hydroxyamidinohydrazone (guanoxabenz). All groups are reduced by mARC proteins, and the enzymes are therefore involved in the interconversion of N-oxygenated metabolites originating from cytochrome P450s and flavin-containing monooxygenases.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!