HepG2 cells with recombinant cytochrome P450 enzyme overexpression: Their use and limitation as in vitro liver model

2019 ◽  
Vol 5 (1) ◽  
pp. 55-64 ◽  
Author(s):  
S. Steinbrecht ◽  
S. Kammerer ◽  
J.-H. Küpper
Keyword(s):  
Cytochrome P450 ◽  
Hepg2 Cells ◽  
Cytochrome P450 Enzyme ◽  
Liver Model ◽  
P450 Enzyme ◽  
Enzyme Overexpression

scholarly journals Hepatic and hippocampal cytochrome P450 enzyme overexpression during spontaneous recurrent seizures

Epilepsia ◽  
2017 ◽  
Vol 59 (1) ◽  
pp. 123-134 ◽  
Author(s):  
Leonie Runtz ◽  
Benoit Girard ◽  
Marion Toussenot ◽  
Julie Espallergues ◽  
Alexis Fayd'Herbe De Maudave ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Cytochrome P450 Enzyme ◽  
P450 Enzyme ◽  
Spontaneous Recurrent Seizures ◽  
Enzyme Overexpression

2020 FDA Drug-drug Interaction Guidance: A Comparison Analysis and Action Plan by Pharmaceutical Industrial Scientists

2020 ◽  
Vol 21 (6) ◽  
pp. 403-426 ◽  
Author(s):  
Sirimas Sudsakorn ◽  
Praveen Bahadduri ◽  
Jennifer Fretland ◽  
Chuang Lu
Keyword(s):  
Cytochrome P450 ◽  
Drug Interaction ◽  
Drug Interactions ◽  
Action Plan ◽  
European Medicines Agency ◽  
Cytochrome P450 Enzyme ◽  
Interaction Studies ◽  
P450 Enzyme ◽  
Us Fda

Background: In January 2020, the US FDA published two final guidelines, one entitled “In vitro Drug Interaction Studies - Cytochrome P450 Enzyme- and Transporter-Mediated Drug Interactions Guidance for Industry” and the other entitled “Clinical Drug Interaction Studies - Cytochrome P450 Enzyme- and Transporter-Mediated Drug Interactions Guidance for Industry”. These were updated from the 2017 draft in vitro and clinical DDI guidance. Methods: This study is aimed to provide an analysis of the updates along with a comparison of the DDI guidelines published by the European Medicines Agency (EMA) and Japanese Pharmaceuticals and Medical Devices Agency (PMDA) along with the current literature. Results: The updates were provided in the final FDA DDI guidelines and explained the rationale of those changes based on the understanding from research and literature. Furthermore, a comparison among the FDA, EMA, and PMDA DDI guidelines are presented in Tables 1, 2 and 3. Conclusion: The new 2020 clinical DDI guidance from the FDA now has even higher harmonization with the guidance (or guidelines) from the EMA and PMDA. A comparison of DDI guidance from the FDA 2017, 2020, EMA, and PMDA on CYP and transporter based DDI, mathematical models, PBPK, and clinical evaluation of DDI is presented in this review.

scholarly journals Endocannabinoid turnover in GtoPdb v.2021.3

2021 ◽  
Vol 2021 (3) ◽  
Author(s):  
Stephen P.H. Alexander ◽  
Patrick Doherty ◽  
Christopher J. Fowler ◽  
Jürg Gertsch ◽  
Mario Van der Stelt
Keyword(s):  
Cytochrome P450 ◽  
Phospholipase D ◽  
Cytochrome P450 Enzyme ◽  
Facilitated Diffusion ◽  
In Vitro Experiments ◽  
Diacylglycerol Lipase ◽  
P450 Enzyme ◽  
Key Enzyme

The principle endocannabinoids are 2-acylglycerol esters, such as 2-arachidonoylglycerol (2-AG), and N-acylethanolamines, such as anandamide (N-arachidonoylethanolamine, AEA). The glycerol esters and ethanolamides are synthesised and hydrolysed by parallel, independent pathways. Mechanisms for release and re-uptake of endocannabinoids are unclear, although potent and selective inhibitors of facilitated diffusion of endocannabinoids across cell membranes have been developed [28]. FABP5 (Q01469) has been suggested to act as a canonical intracellular endocannabinoid transporter in vivo [17]. For the generation of 2-arachidonoylglycerol, the key enzyme involved is diacylglycerol lipase (DAGL), whilst several routes for anandamide synthesis have been described, the best characterized of which involves N-acylphosphatidylethanolamine-phospholipase D (NAPE-PLD, [70]). A transacylation enzyme which forms N-acylphosphatidylethanolamines has been identified as a cytosolic enzyme, PLA2G4E (Q3MJ16) [62]. In vitro experiments indicate that the endocannabinoids are also substrates for oxidative metabolism via cyclooxygenase, lipoxygenase and cytochrome P450 enzyme activities [5, 23, 72].

scholarly journals Endocannabinoid turnover (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database

2019 ◽  
Vol 2019 (4) ◽  
Author(s):  
Stephen P.H. Alexander ◽  
Patrick Doherty ◽  
Christopher J. Fowler ◽  
Jürg Gertsch ◽  
Mario Van der Stelt
Keyword(s):  
Cytochrome P450 ◽  
Phospholipase D ◽  
Cytochrome P450 Enzyme ◽  
Facilitated Diffusion ◽  
In Vitro Experiments ◽  
Diacylglycerol Lipase ◽  
P450 Enzyme ◽  
Key Enzyme

The principle endocannabinoids are 2-acylglycerol esters, such as 2-arachidonoylglycerol (2-AG), and N-acylethanolamines, such as anandamide (N-arachidonoylethanolamine, AEA). The glycerol esters and ethanolamides are synthesised and hydrolysed by parallel, independent pathways. Mechanisms for release and re-uptake of endocannabinoids are unclear, although potent and selective inhibitors of facilitated diffusion of endocannabinoids across cell membranes have been developed [19]. FABP5 (Q01469) has been suggested to act as a canonical intracellular endocannabinoid transporter in vivo [12]. For the generation of 2-arachidonoylglycerol, the key enzyme involved is diacylglycerol lipase (DAGL), whilst several routes for anandamide synthesis have been described, the best characterized of which involves N-acylphosphatidylethanolamine-phospholipase D (NAPE-PLD, [49]). A transacylation enzyme which forms N-acylphosphatidylethanolamines has recently been identified as a cytosolic enzyme, PLA2G4E (Q3MJ16) [43]. In vitro experiments indicate that the endocannabinoids are also substrates for oxidative metabolism via cyclooxygenase, lipoxygenase and cytochrome P450 enzyme activities [4, 16, 51].

scholarly journals Validation of in vitro methods for human cytochrome P450 enzyme induction: Outcome of a multi-laboratory study

2019 ◽  
Vol 60 ◽  
pp. 212-228 ◽  
Author(s):  
Camilla Bernasconi ◽  
Olavi Pelkonen ◽  
Tommy B. Andersson ◽  
Judy Strickland ◽  
Iwona Wilk-Zasadna ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Enzyme Induction ◽  
Laboratory Study ◽  
Cytochrome P450 Enzyme ◽  
In Vitro Methods ◽  
Human Cytochrome ◽  
P450 Enzyme ◽  
Human Cytochrome P450 Enzyme
Sign in / Sign up

Export Citation Format

Share Document