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Article
A liquid chromatography-tandem mass spectrometry analysis of nine cytochrome P450 probe drugs and their corresponding metabolites in human serum and urine
Cocktail phenoty** using specific probe drugs for cytochrome P450 (CYP) enzymes provides information on the real-time activity of multiple CYPs. We investigated different sample preparation techniques and va...
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Article
Ultrafast protein structure-based virtual screening with Panther
Molecular docking is by far the most common method used in protein structure-based virtual screening. This paper presents Panther, a novel ultrafast multipurpose docking tool. In Panther, a simple shape-electr...
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Article
In Vivo-In Vitro-In Silico Pharmacokinetic Modelling in Drug Development
Although clinical drug trials are indispensable in providing an appropriate background for dosage recommendations, they can provide mechanistic pharmacokinetic information only indirectly with the help of cert...
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Article
Inhibition and induction of human cytochrome P450 enzymes: current status
Variability of drug metabolism, especially that of the most important phase I enzymes or cytochrome P450 (CYP) enzymes, is an important complicating factor in many areas of pharmacology and toxicology, in drug...
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Article
Novel Cyclic Phosphate Prodrug Approach for Cytochrome P450-activated Drugs Containing an Alcohol Functionality
A cyclic phosphate prodrug of a descriptive molecule containing an alcohol functionality was designed, synthesized and characterized in vitro as a cytochrome P450 (CYP) -selective prodrug.
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Article
Use of an online surveillance system for screening drug interactions in prescriptions in community pharmacies
Computerised surveillance systems have become available for screening potential adverse drug interactions during drug prescribing and dispensing. The purpose of this study was to analyse the frequency and prof...
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Article
The expression of cytochrome P450 enzymes in human breast tumours and normal breast tissue
Environmental chemicals are one of the risk factors in breast cancer genesis. Cytochrome P450 (CYP) enzymes play a major role in the activation of these chemicals. Using highly specific and sensitive reverse t...
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Article
Accelerated apoptosis and low Bcl-2 expression associated with neuroendocrine differentiation predict shortened survival in operated large cell carcinoma of the lung
In order to test the hypothesis that increased apoptotic activity is connected with neuroendocrine differentiation and low differentiation degree in large cell carcinoma (LCLC) and is regulated by bcl-2 family...
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Article
Induction of CYP2A5 by pyrazole and its derivatives in mouse primary hepatocytes
Mouse liver CYP2A5 is induced by several structurally unrelated compounds. In intact mouse liver, pyrazole (PYR) and 4-hydroxypyrazole (4-OH) induce selectively the expression of CYP2A5 while expression of ot...
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Chapter and Conference Paper
Expression of Xenobiotic-Metabolizing Cytochrome P450s in Human Pulmonary Tissues
The purpose of the study was to obtain a comprehensive picture of the expression of cytochrome P450s (CYP) in the human lung, broncho-alveolar macrophages (BAM), and peripheral blood lymphocytes. The methods u...
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Article
Regulation of CYP2A5 induction by porphyrinogenic agents in mouse primary hepatocytes
All cytochrome P450 (CYP) enzymes contain heme as a prosthetic group. In contrast to other CYP enzymes, murine CYP2A5 is upregulated in vivo by several agents that disturb cellular heme balance. To test the h...
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Article
Expression of cytochrome P 450 3A enzymes in human lung: a combined RT-PCR and immunohistochemical analysis of normal tissue and lung tumours
We have previously demonstrated expression of cytochrome P 450 3A (CYP3A) protein in pulmonary carcinomas and surrounding normal tissue, using immunohistochemistry. These results suggested that different CYP3A...
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Article
Up-regulation of CYP2A5 expression by porphyrinogenic agents in mouse liver
Coumarin 7-hydroxylase (COH) activity is catalyzed by the Cyp2a-5 gene product (CYP2A5 enzyme) in mice. Mouse hepatic CYP2A5 expression is often increased in conditions in which other P450 forms are repressed,...
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Article
The role of CYP enzymes in cocaine-induced liver damage
Cocaine is hepatotoxic in several species, including man. A high dose of cocaine produces metabolismdependent, mainly pericentral, liver damage. At 24h after a single dose of cocaine, mouse hepatic P450 conten...
