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Titolo:
STABLE EXPRESSION OF HUMAN CYTOCHROME-P450 3A4 IN V79 CELLS AND ITS APPLICATION FOR METABOLIC PROFILING OF ERGOT DERIVATIVES
Autore:
RAUSCHENBACH R; GIESCHEN H; HUSEMANN M; SALOMON B; HILDEBRAND M;
Indirizzi:
SCHERING AG,INST PHARMACOKINET,RES LABS D-13342 BERLIN GERMANY SCHERING AG,INST PHARMACOKINET,RES LABS D-13342 BERLIN GERMANY
Titolo Testata:
European journal of pharmacology. Environmental toxicology and pharmacology section
fascicolo: 3, volume: 293, anno: 1995,
pagine: 183 - 190
SICI:
0926-6917(1995)293:3<183:SEOHC3>2.0.ZU;2-E
Fonte:
ISI
Lingua:
ENG
Soggetto:
CHINESE-HAMSTER-CELLS; HUMAN-LIVER; NIFEDIPINE OXIDASE; CDNA; GENE; SEQUENCE; ENZYME; IDENTIFICATION; SPECIFICITIES; PURIFICATION;
Keywords:
HETEROLOGOUS EXPRESSION; CYTOCHROME P450 3A4; V79 CHINESE HAMSTER CELL; TESTOSTERONE; ERGOT DERIVATIVE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
43
Recensione:
Indirizzi per estratti:
Citazione:
R. Rauschenbach et al., "STABLE EXPRESSION OF HUMAN CYTOCHROME-P450 3A4 IN V79 CELLS AND ITS APPLICATION FOR METABOLIC PROFILING OF ERGOT DERIVATIVES", European journal of pharmacology. Environmental toxicology and pharmacology section, 293(3), 1995, pp. 183-190

Abstract

Expression of human cytochrome P450 (CYP) in heterologous cells is a means of specifically studying the role of these enzymes in drug metabolism. The complete cDNA encoding CYP3A4 (PCN1) was inserted into an expression vector containing the strong myeloproliferative sarcoma virus promoter in combination with the enhancer of the cytomegalovirus andstably expressed in V79 Chinese hamster cells. The presence of genomically integrated CYP3A4 cDNA cell clones was confirmed by polymerase chain reaction analysis. Transcription was detected by reverse transcribed polymerase chain reaction analysis. Functional expression could bedemonstrated by conversion of testosterone to the specific 6 beta-hydroxylated product. In recombinant V79 cells expressing CYP3A4 about 6%of the substrate was converted to 6 beta-hydroxytestosterone. The metabolism of two dopaminergic ergot derivatives was investigated in liverecombinant V79 cells. Both lisuride and terguride were monodeethylated.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 19/01/20 alle ore 20:20:32