Use of in vitro pregnane X receptor assays to assess CYP3A4 induction potential of drug candidates

Methods Enzymol. 2002:357:161-70. doi: 10.1016/s0076-6879(02)57675-8.

Authors

Stacey A Jones¹, Linda B Moore, G Bruce Wisely, Steven A Kliewer

Affiliation

¹ Department of Nuclear Receptor Functional Analysis, High Throughput Biology, GlaxoSmithKline, Inc., Research Triangle Park, North Carolina 27709, USA.

PMID: 12424907
DOI: 10.1016/s0076-6879(02)57675-8

No abstract available

MeSH terms

Alkaline Phosphatase / genetics
Alkaline Phosphatase / metabolism
Animals
Binding Sites
Chloramphenicol O-Acetyltransferase / genetics
Chloramphenicol O-Acetyltransferase / metabolism
Cytochrome P-450 CYP3A
Cytochrome P-450 Enzyme System / metabolism*
Drug Design
Drug Evaluation*
Enzyme Inhibitors / metabolism
Enzymes, Immobilized
Gene Expression Regulation / drug effects*
Genes, Reporter
Humans
Plasmids / genetics
Plasmids / metabolism
Pregnane X Receptor
Protein Binding
Protein Conformation
Receptors, Cytoplasmic and Nuclear / genetics
Receptors, Cytoplasmic and Nuclear / metabolism*
Receptors, Steroid / genetics
Receptors, Steroid / metabolism*

Substances

Enzyme Inhibitors
Enzymes, Immobilized
Pregnane X Receptor
Receptors, Cytoplasmic and Nuclear
Receptors, Steroid
Cytochrome P-450 Enzyme System
CYP3A protein, human
Cytochrome P-450 CYP3A
CYP3A4 protein, human
Chloramphenicol O-Acetyltransferase
Alkaline Phosphatase