-
Article
Open AccessCorrection to: Progesterone receptor membrane component 1 regulates lipid homeostasis and drives oncogenic signaling resulting in breast cancer progression
An amendment to this paper has been published and can be accessed via the original article.
-
Article
Open AccessDifferential effects on human cytochromes P450 by CRISPR/Cas9-induced genetic knockout of cytochrome P450 reductase and cytochrome b5 in HepaRG cells
HepaRG cells are increasingly accepted as model for human drug metabolism and other hepatic functions. We used lentiviral transduction of undifferentiated HepaRG cells to deliver Cas9 and two alternative sgRNA...
-
Reference Work Entry In depth
P450 Monooxygenase System
-
Article
Open AccessProgesterone receptor membrane component 1 regulates lipid homeostasis and drives oncogenic signaling resulting in breast cancer progression
PGRMC1 (progesterone receptor membrane component 1) is a highly conserved heme binding protein, which is overexpressed especially in hormone receptor-positive breast cancer and plays an important role in breas...
-
Article
Copy number variation profiling in pharmacogenes using panel-based exome resequencing and correlation to human liver expression
Structural variants including copy number variations (CNV) have gained widespread attention, especially in pharmacogenomics but for several genes functional relevance and clinical evidence are still lacking. D...
-
Living Reference Work Entry In depth
P450 Monooxygenase System
-
Article
Open AccessThe formation of estrogen-like tamoxifen metabolites and their influence on enzyme activity and gene expression of ADME genes
Tamoxifen, a standard therapy for breast cancer, is metabolized to compounds with anti-estrogenic as well as estrogen-like action at the estrogen receptor. Little is known about the formation of estrogen-like ...
-
Article
Methyleugenol DNA adducts in human liver are associated with SULT1A1 copy number variations and expression levels
Methyleugenol is a rodent hepatocarcinogen occurring in many herbs and spices as well as essential oils used for flavoring. Following metabolic activation by cytochromes P450 (CYPs) and sulfotransferases (SULT...
-
Article
Association between CYP2E1 polymorphisms and risk of differentiated thyroid carcinoma
Differentiated thyroid carcinoma (DTC) results from complex interactions between genetic and environmental factors. Known etiological factors include exposure to ionizing radiations, previous thyroid diseases,...
-
Article
Open AccessPathobiochemical signatures of cholestatic liver disease in bile duct ligated mice
Disrupted bile secretion leads to liver damage characterized by inflammation, fibrosis, eventually cirrhosis, and hepatocellular cancer. As obstructive cholestasis often progresses insidiously, markers for the...
-
Article
Pregnane X receptor activation and silencing promote steatosis of human hepatic cells by distinct lipogenic mechanisms
In addition to its well-characterized role in the regulation of drug metabolism and transport by xenobiotics, pregnane X receptor (PXR) critically impacts on lipid homeostasis. In mice, both ligand-dependent ...
-
Article
Open AccessThe truncated splice variant of peroxisome proliferator-activated receptor alpha, PPARα-tr, autonomously regulates proliferative and pro-inflammatory genes
The peroxisome proliferator-activated receptor alpha (PPARα) controls lipid/energy homeostasis and inflammatory responses. The truncated splice variant PPARα-tr was suggested to exert a dominant negative funct...
-
Article
Open AccessTargeted epigenome editing of an endogenous locus with chromatin modifiers is not stably maintained
DNA methylation and histone 3 lysine 9 (H3K9) methylation are considered as epigenetic marks that can be inherited through cell divisions. To explore the functional consequences and stability of these modifica...
-
Article
Open AccessGenetics is a major determinant of expression of the human hepatic uptake transporter OATP1B1, but not of OATP1B3 and OATP2B1
Organic anion transporting polypeptide (OATP) 1B1, OATP1B3, and OATP2B1 (encoded by SLCO1B1, SLCO1B3, SLCO2B1) mediate the hepatic uptake of endogenous compounds like bile acids and of drugs, for example, the lip...
-
Article
Open AccessDNA methylation is associated with downregulation of the organic cation transporter OCT1 (SLC22A1) in human hepatocellular carcinoma
Organic cation transporters (OCTs) determine not only physiological processes but are also involved in the cellular uptake of anticancer agents. Based on microarray analyses in hepatocellular carcinoma (HCC), SLC...
-
Article
Open AccessA systems biology approach to dynamic modeling and inter-subject variability of statin pharmacokinetics in human hepatocytes
The individual character of pharmacokinetics is of great importance in the risk assessment of new drug leads in pharmacological research. Amongst others, it is severely influenced by the properties and inter-i...
-
Article
Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation
We investigated the elimination routes for the 200 drugs that are sold most often by prescription count in the United States. The majority (78%) of the hepatically cleared drugs were found to be subject to oxi...
-
Article
Functional study of the 830C>G polymorphism of the human carboxylesterase 2 gene
Carboxylesterase 2 (CES2) is involved in the activation of the anticancer drug irinotecan to its active metabolite SN-38. We previously identified a single nucleotide polymorphism (SNP), with an allele frequen...
-
Article
Non-synonymous polymorphisms in the human SLCO1B1 gene: an in vitro analysis of SNP c.1929A>C
Polymorphisms in the SLCO1B1 gene encoding the human hepatocellular uptake transporter OATP1B1 can be associated with alterations in transporter properties and may affect the pharmacokinetics of drugs transported...
-
Reference Work Entry In depth
P450 Mono-oxygenase System
