Title : Exploring the Carbamazepine Interaction with Human Pregnane X Receptor and Effect on ABCC2 Using in Vitro and in Silico Approach.

Pub. Date : 2017 Jul

PMID : 28432535






8 Functional Relationships(s)
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1 Exploring the Carbamazepine Interaction with Human Pregnane X Receptor and Effect on ABCC2 Using in Vitro and in Silico Approach. Carbamazepine nuclear receptor subfamily 1 group I member 2 Homo sapiens
2 METHODS: We investigated the effect of CBZ on expression of ABCC2 and pregnane X receptor (PXR) in HepG2 cell line and compared with hyperforin (agonist of PXR) and ketoconazole (antagonist of PXR) through realtime PCR and western blot assay. Carbamazepine nuclear receptor subfamily 1 group I member 2 Homo sapiens
3 METHODS: We investigated the effect of CBZ on expression of ABCC2 and pregnane X receptor (PXR) in HepG2 cell line and compared with hyperforin (agonist of PXR) and ketoconazole (antagonist of PXR) through realtime PCR and western blot assay. Carbamazepine nuclear receptor subfamily 1 group I member 2 Homo sapiens
4 Molecular docking and dynamic simulation approach was used to understand the interaction of CBZ with PXR. Carbamazepine nuclear receptor subfamily 1 group I member 2 Homo sapiens
5 Molecular dynamic (MD) simulation and in vitro experiment indicated possibility of CBZ to be PXR agonist and PXR residue Gln285 to be important for CBZ-PXR interaction. Carbamazepine nuclear receptor subfamily 1 group I member 2 Homo sapiens
6 Molecular dynamic (MD) simulation and in vitro experiment indicated possibility of CBZ to be PXR agonist and PXR residue Gln285 to be important for CBZ-PXR interaction. Carbamazepine nuclear receptor subfamily 1 group I member 2 Homo sapiens
7 Molecular dynamic (MD) simulation and in vitro experiment indicated possibility of CBZ to be PXR agonist and PXR residue Gln285 to be important for CBZ-PXR interaction. Carbamazepine nuclear receptor subfamily 1 group I member 2 Homo sapiens
8 CONCLUSIONS: CBZ alters the functional activity of ABCC2 through PXR, which in turn can interfere with therapy. Carbamazepine nuclear receptor subfamily 1 group I member 2 Homo sapiens