Role of specific cytochrome P450 isoforms in the conversion of phenoxypropoxybiguanide analogs in human liver microsomes to potent antimalarial dihydrotriazines

Drug Metabolism and Disposition

Volumn 36, Issue 2, 2008, Pages 380-385

  Diaz, Damaris S ^a   Kozar, Michael P ^a   Smith, Kirsten S ^a   Asher, Constance O ^a   Sousa, Jason C ^a   Schiehser, Guy A ^b   Jacobus, David P ^b   Milhous, Wilbur K ^a   Skillman, Donald R ^a   Shearer, Todd W ^a,c  

^a WALTER REED ARMY INSTITUTE OF RESEARCH   (United States)

^b Jacobus Pharmaceutical Co Inc   (United States)

^c GLAXOSMITHKLINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4,6 DIAMINO 1,2 DIHYDRO 2,2 DIMETHYL 1 [3 (2,4,5 TRICHLOROPHENOXY)PROPOXY] 1,3,5 TRIAZINE; ANTIMALARIAL AGENT; BIGUANIDE DERIVATIVE; CYTOCHROME P450 1A2; CYTOCHROME P450 2C19; CYTOCHROME P450 2C9; CYTOCHROME P450 2D6; CYTOCHROME P450 3A4; CYTOCHROME P450 ISOENZYME; DIHYDROTRIAZINE DERIVATIVE; DRUG METABOLITE; FOLIC ACID ANTAGONIST; JPC 2056; JPC 2067; N [3 (2,4,5 TRICHLOROPHENOXY)PROPOXY] N' ISOPROPYLIMIDOCARBONIMIDIC DIAMIDE; PHENOXYPROPOXYBIGUANIDE DERIVATIVE; PROGUANIL; PROTEIN ANTIBODY; UNCLASSIFIED DRUG;

ARTICLE; CONTROLLED STUDY; DRUG METABOLISM; DRUG STRUCTURE; DRUG TRANSFORMATION; GENETIC POLYMORPHISM; HUMAN; HUMAN CELL; IN VITRO STUDY; INFECTION RISK; LIVER MICROSOME; MALARIA; METABOLIC ACTIVATION; PRIORITY JOURNAL; PROTEIN EXPRESSION;

ANTIBODIES, MONOCLONAL; ANTIMALARIALS; CHLOROGUANIDE; CYTOCHROME P-450 ENZYME SYSTEM; HUMANS; MICROSOMES, LIVER; PRODRUGS; PROTEIN ISOFORMS; RECOMBINANT PROTEINS; TRIAZINES;

EID: 38749103881     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.106.013920     Document Type: Article

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