Carboxymefloquine, the major metabolite of the antimalarial drug mefloquine, induces drug-metabolizing enzyme and transporter expression by activation of pregnane X receptor

Antimicrobial Agents and Chemotherapy

Volumn 59, Issue 1, 2015, Pages 96-104

  Piedade, Rita ^a   Traub, Stefanie ^a   Bitter, Andreas ^a   Nüssler, Andreas K ^b   Gil, José P ^c,d,e   Schwab, Matthias ^a,f   Burk, Oliver ^a  

^a DR MARGARETE FISCHER BOSCH INSTITUTE OF CLINICAL PHARMACOLOGY   (Germany)

^b UNIVERSITY OF TÜBINGEN   (Germany)

^c KAROLINSKA INSTITUTE   (Sweden)

^d UNIVERSITY OF LISBON   (Portugal)

^e BINGHAMTON UNIVERSITY   (United States)

^f UNIVERSITY HOSPITAL TÜBINGEN   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

CARBOXYMEFLOQUINE; CYTOCHROME P450 2B6; CYTOCHROME P450 3A4; DRUG METABOLITE; MEFLOQUINE; MESSENGER RNA; PREGNANE X RECEPTOR; SMALL INTERFERING RNA; UNCLASSIFIED DRUG; ANTIMALARIAL AGENT; CYTOCHROME P450 2B6 INDUCER; PROTEIN BINDING; RO 21-5104; STEROID RECEPTOR;

ARTICLE; CONCENTRATION (PARAMETERS); CONTROLLED STUDY; DRUG RECEPTOR BINDING; ENZYME INDUCTION; GENE EXPRESSION; GENE SILENCING; HUMAN; HUMAN CELL; LIGAND BINDING; LIVER CELL; PROMOTER REGION; PROTEIN EXPRESSION; REPORTER GENE; AGONISTS; ANALOGS AND DERIVATIVES; ANIMAL; CELL LINE; CHLOROCEBUS AETHIOPS; COS 1 CELL LINE; DRUG EFFECTS; DRUG INTERACTION; DRUG RESISTANCE; GENETICS; HEPG2 CELL LINE; MALARIA; METABOLISM; RNA INTERFERENCE; TRANSPORT AT THE CELLULAR LEVEL;

ANIMALS; ANTIMALARIALS; BIOLOGICAL TRANSPORT; CELL LINE; CERCOPITHECUS AETHIOPS; COS CELLS; CYTOCHROME P-450 CYP2B6; CYTOCHROME P-450 CYP2B6 INDUCERS; DRUG INTERACTIONS; DRUG RESISTANCE; HEP G2 CELLS; HEPATOCYTES; HUMANS; MALARIA; MEFLOQUINE; PROTEIN BINDING; RECEPTORS, STEROID; RNA INTERFERENCE; RNA, SMALL INTERFERING;

EID: 84920110967     PISSN: 00664804     EISSN: 10986596     Source Type: Journal    
DOI: 10.1128/AAC.04140-14     Document Type: Article

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