Use of in vitro pregnane X receptor assays to assess CYP3A4 induction potential of drug candidates.
Jones
Stacey A
SA
Department of Nuclear Receptor Functional Analysis, High Throughput Biology, GlaxoSmithKline, Inc., Research Triangle Park, North Carolina 27709, USA.
Moore
Linda B
LB
Wisely
G Bruce
GB
Kliewer
Steven A
SA
D000469:Alkaline Phosphatase / Q000235:genetics / Q000378:metabolism; D000818:Animals; D001665:Binding Sites; D015500:Chloramphenicol O-Acetyltransferase / Q000235:genetics / Q000378:metabolism; D051544:Cytochrome P-450 CYP3A; D003577:Cytochrome P-450 Enzyme System / Q000378:metabolism*; D015195:Drug Design; D004341:Drug Evaluation; D004791:Enzyme Inhibitors / Q000378:metabolism; D004800:Enzymes, Immobilized; D005786:Gene Expression Regulation / Q000187:drug effects*; D017930:Genes, Reporter; D006801:Humans; D010957:Plasmids / Q000235:genetics / Q000378:metabolism; D000077297:Pregnane X Receptor; D011485:Protein Binding; D011487:Protein Conformation; D018160:Receptors, Cytoplasmic and Nuclear / Q000235:genetics / Q000378:metabolism*; D011987:Receptors, Steroid / Q000235:genetics / Q000378:metabolism*
D004791:Enzyme Inhibitors; D004800:Enzymes, Immobilized; D000077297:Pregnane X Receptor; D018160:Receptors, Cytoplasmic and Nuclear; D011987:Receptors, Steroid; D003577:Cytochrome P-450 Enzyme System; C104464:CYP3A protein, human; D051544:Cytochrome P-450 CYP3A; C510163:CYP3A4 protein, human; D015500:Chloramphenicol O-Acetyltransferase; D000469:Alkaline Phosphatase