Abstract:
:Luminogenic cytochrome P450 (CYP) assays couple CYP enzyme activity to firefly luciferase luminescence in a technology called P450-Glo(TM) (Promega). Luminogenic substrates are used in assays of human CYP1A1, -1A2, -1B1, -2C8, -2C9, -2C19, -2D6, -2J2, -3A4, -3A7, -4A11, -4F3B, -4F12 and -19. The assays detect dose-dependent CYP inhibition by test compounds against recombinant CYP enzymes or liver microsomes. Induction or inhibition of CYP activities in cultured hepatocytes is measured in a nonlytic approach that leaves cells intact for additional analysis. Luminogenic CYP assays offer advantages of speed and safety over HPLC and radiochemical-based methods. Compared with fluorogenic methods the approach offers advantages of improved sensitivity and decreased interference between optical properties of test compound and CYP substrate. These homogenous assays are sensitive and robust tools for high-throughput CYP screening in early drug discovery.
journal_name
Expert Opin Drug Metab Toxicoljournal_title
Expert opinion on drug metabolism & toxicologyauthors
Cali JJ,Ma D,Sobol M,Simpson DJ,Frackman S,Good TD,Daily WJ,Liu Ddoi
10.1517/17425255.2.4.629subject
Has Abstractpub_date
2006-08-01 00:00:00pages
629-45issue
4eissn
1742-5255issn
1744-7607journal_volume
2pub_type
杂志文章,评审abstract:INTRODUCTION:Raltegravir was the first available integrase inhibitor for treating HIV-positive patients. This review aims to provide an overview of its role in the management of HIV-1 infection, highlighting its key pharmacokinetic and pharmacodynamic properties. AREAS COVERED:This review covers material searched and ...
journal_title:Expert opinion on drug metabolism & toxicology
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abstract:INTRODUCTION:Due to their multiple effects, glucocorticoids (GCs) have versatile medical uses. They can regulate many xenobiotic-metabolizing enzymes of the cytochrome P450 (CYP) superfamily, and thus, influence pharmacotherapy. AREAS COVERED:The aim of this paper is to summarize the molecular effects of GCs on CYP as...
journal_title:Expert opinion on drug metabolism & toxicology
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abstract:INTRODUCTION:Pediatric critical illness and associated alterations in organ function can change drug pharmacokinetics (PK). Extracorporeal membrane oxygenation (ECMO), a life-saving therapy for severe cardiac and/or respiratory failure, causes additional PK alterations that affect drug disposition. AREAS COVERED:The p...
journal_title:Expert opinion on drug metabolism & toxicology
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journal_title:Expert opinion on drug metabolism & toxicology
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journal_title:Expert opinion on drug metabolism & toxicology
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journal_title:Expert opinion on drug metabolism & toxicology
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journal_title:Expert opinion on drug metabolism & toxicology
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journal_title:Expert opinion on drug metabolism & toxicology
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journal_title:Expert opinion on drug metabolism & toxicology
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journal_title:Expert opinion on drug metabolism & toxicology
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journal_title:Expert opinion on drug metabolism & toxicology
pub_type: 杂志文章,评审
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更新日期:2008-11-01 00:00:00
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journal_title:Expert opinion on drug metabolism & toxicology
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更新日期:2008-12-01 00:00:00
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journal_title:Expert opinion on drug metabolism & toxicology
pub_type: 杂志文章,评审
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更新日期:2009-01-01 00:00:00
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journal_title:Expert opinion on drug metabolism & toxicology
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更新日期:2008-08-01 00:00:00
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journal_title:Expert opinion on drug metabolism & toxicology
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更新日期:2008-10-01 00:00:00
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journal_title:Expert opinion on drug metabolism & toxicology
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更新日期:2015-01-01 00:00:00
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journal_title:Expert opinion on drug metabolism & toxicology
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更新日期:2013-02-01 00:00:00
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journal_title:Expert opinion on drug metabolism & toxicology
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journal_title:Expert opinion on drug metabolism & toxicology
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journal_title:Expert opinion on drug metabolism & toxicology
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journal_title:Expert opinion on drug metabolism & toxicology
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journal_title:Expert opinion on drug metabolism & toxicology
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journal_title:Expert opinion on drug metabolism & toxicology
pub_type: 杂志文章,评审
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更新日期:2016-06-01 00:00:00
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journal_title:Expert opinion on drug metabolism & toxicology
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journal_title:Expert opinion on drug metabolism & toxicology
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journal_title:Expert opinion on drug metabolism & toxicology
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journal_title:Expert opinion on drug metabolism & toxicology
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