Comparison of cytochrome P450 2D6 and variants in terms of drug oxidation rates and substrate inhibition.

abstract：:Thiopurines such as azathioprine, 6-mercaptopurine and 6-thioguanine are antimetabolites that have been used for several decades in the treatment of several diseases including inflammatory bowel diseases. Additional anti-inflammatory properties of these thiopurines have been discovered in recent years. Thiopurine meta...

journal_title：Current drug metabolism

authors： Van Asseldonk DP,de Boer NK,Peters GJ,Veldkamp AI,Mulder CJ,Van Bodegraven AA

更新日期：2009-11-01 00:00:00

abstract：:Early understanding of the metabolic pathway and potential interaction of new drug candidates with other drugs is one of the goals of preclinical studies in the drug discovery process. Although other body organs are involved in drug biotransformation, the liver is the predominant organ of metabolism for a wide range o...

journal_title：Current drug metabolism

authors： Fasinu P,Bouic PJ,Rosenkranz B

更新日期：2012-02-01 00:00:00

abstract：:L-Carnitine has important roles in intermediary metabolism and patients with end-stage renal disease who are undergoing hemodialysis may develop a secondary L-carnitine deficiency. The extent of accumulation of the metabolites trimethylamine and trimethylamine-N-oxide when L-carnitine is administered orally has not be...

journal_title：Current drug metabolism

authors： Bain MA,Faull R,Milne RW,Evans AM

更新日期：2006-10-01 00:00:00

abstract：BACKGROUND:ET-26 hydrochloride is a novel intravenous anesthetic, approved for clinical trials, that produces a desirable sedative-hypnotic effect with stable myocardial performance and mild adrenocortical suppression in rats and beagle dogs. The objective of this study was to assess the absorption, distribution, metab...

journal_title：Current drug metabolism

authors： Zhang YJ,Deng C,Yang J,Gong D,Kang Y,Liu J,Zhang W

更新日期：2019-01-01 00:00:00

abstract：:This review introduces the Noscapine, which is being used as an antitussive drug for a long time has been recently discovered as a novel tubulin-binding, anti-angiogenic anticancer drug that causes cell cycle arrest and induces apoptosis in cancer cells both in vitro as well as in vivo. Noscapine is a multifunctional ...

journal_title：Current drug metabolism

authors： Singh H,Singh P,Kumari K,Chandra A,Dass SK,Chandra R

更新日期：2013-03-01 00:00:00

abstract：:Graphene and its modified nano-composites have gained much attention in recent times in cancer therapy as nanotheranostics due to low production cost, ease in synthesis and physicochemical properties (ultra-large surface area with planar structure and π-π conjugation with the unsaturated and aromatic drugs/biomolecule...

journal_title：Current drug metabolism

authors： Rahman M,Ahmad MZ,Ahmad J,Firdous J,Ahmad FJ,Mushtaq G,Kamal MA,Akhter S

更新日期：2015-01-01 00:00:00

abstract：:For the pharmaceutical industry, one of the challenges in evaluating the risk of future compound attrition at the discovery stage is the successful prediction of the major routes of clearance in humans. For compounds cleared by metabolism, such information will help to avoid the development of compounds that will exhi...

journal_title：Current drug metabolism

authors： Williams JA,Hurst SI,Bauman J,Jones BC,Hyland R,Gibbs JP,Obach RS,Ball SE

更新日期：2003-12-01 00:00:00

abstract：: ...

journal_title：Current drug metabolism

authors： Wei JF

更新日期：2018-01-01 00:00:00

abstract：:Metabolism of xenobiotics is often seen as an exclusive function of the liver, but some current findings support the notion that the lungs, kidneys and intestine may contribute considerably. After the establishment of the use of liver slices as a useful in vitro model to study metabolism and toxicity of xenobiotics, t...

journal_title：Current drug metabolism

authors： de Kanter R,Monshouwer M,Meijer DK,Groothuis GM

更新日期：2002-02-01 00:00:00

abstract：:Molecules exist as three dimensional structures. Therefore they can exist in symmetrical and asymmetrical forms. Molecules with an asymmetric centre are chiral. If the molecule and its mirror image are non-superimposable, the relationship between the two molecules is enantiomeric and the two stereoisomers are enantiom...

journal_title：Current drug metabolism

authors： Landoni MF,Soraci A

更新日期：2001-03-01 00:00:00

abstract：:Bioavailability of orally administered drugs can be influenced by a number of factors including release from the formulation, dissolution, stability in the gastrointestinal (GI) environment, permeability through the gut wall and first-pass gut wall and hepatic metabolism. Although there are various enzymes in the gut ...

journal_title：Current drug metabolism

authors： Darwich AS,Neuhoff S,Jamei M,Rostami-Hodjegan A

更新日期：2010-11-01 00:00:00

abstract：:Since conventional therapeutic approaches in cancer are highly invasive they hardly prolong patient survival for more than few months. Having the ability to stimulate both cellular and humoural immune responses, immunisation with naked plasmid DNA encoding tumour-associated antigens or tumour-specific antigens has rec...

journal_title：Current drug metabolism

authors： Chiarella P,Fazio VM,Signori E

更新日期：2013-03-01 00:00:00

abstract：:To understand the sophisticated dynamic behaviors of drug elution and permeation in the gastrointestinal tract (GIT), researchers have tried to reemerge it by employing various in vitro experimental models. However, official in vitro apparatuses routinely used for quality control purposes, employ simple, non-physiolog...

journal_title：Current drug metabolism

authors： Li Z,He X

更新日期：2015-01-01 00:00:00

abstract：:In vitro models of the liver using isolated primary hepatocytes have been used as screens for measuring the metabolism, toxicity and efficacy of xenobiotics, for studying hepatocyte proliferation, and as bioartificial liver support systems. Yet, primary isolated hepatocytes rapidly lose liver specific functions when m...

journal_title：Current drug metabolism

authors： Sivaraman A,Leach JK,Townsend S,Iida T,Hogan BJ,Stolz DB,Fry R,Samson LD,Tannenbaum SR,Griffith LG

更新日期：2005-12-01 00:00:00

abstract：BACKGROUND:Increasing incidences of type 2 diabetes make it necessary to have a better understanding of the risk factors for its prediction. Taking a note of resilience in risk factors, dynamics of the emerging factors other than traditional ones are showing a great interest in recent years which imprints a significant...

journal_title：Current drug metabolism

authors： Yadav D,Cho KH

更新日期：2018-01-01 00:00:00

abstract：:Work on human immortalized cell lines is not considered research on human subjects, but does involve biohazards. It has also been estimated that about 80% of human cell lines are the kind of cells that they are expected. Cells that are cultured directly from a subject are referred to as primary cells. Clonetics is the...

journal_title：Current drug metabolism

authors： Gomase VS,Tagore S,Changbhale SS,Kale KV

更新日期：2008-03-01 00:00:00

abstract：BACKGROUND:Drug-induced cholestasis is a risk factor in the progression of drug candidates, and poses a serious health hazard if not detected before going into a human. Intrahepatic accumulation of Bile Acids (BAs) represents a characteristic phenomenon associated with drug-induced cholestasis. METHODS:This review wil...

journal_title：Current drug metabolism

authors： Chatterjee S,Annaert P

更新日期：2018-01-01 00:00:00

abstract：:A number of studies have appeared recently on the underlying mechanisms of liposome-cell interactions under in vitro conditions, in which isolated cell populations or cell lines were used. However, our knowledge of how liposomes interact with cells and the parameters that influence this in vivo is limited. We will sum...

journal_title：Current drug metabolism

authors： Ishida T,Harashima H,Kiwada H

更新日期：2001-12-01 00:00:00

abstract：:New chemical entities are routinely screened in vitro and in vivo for their ability to induce cytochrome P450s (CYP), other drug-metabolizing enzymes and possibly transporters in an attempt to more accurately predict clinical parameters such as drug-drug interactions and clearance in humans. Some of these potential th...

journal_title：Current drug metabolism

authors： Mankowski DC,Ekins S

更新日期：2003-10-01 00:00:00

abstract：BACKGROUND:Various transporters, including efflux transporters and uptake transporters, play an important role in the pharmacokinetics of drugs. Currently, studies suggest that several antibiotics also serve as substrates for transporters. In addition, these antibiotics are usually combined with other drugs to treat di...

journal_title：Current drug metabolism

authors： Hua WJ,Hua WX,Jian Z,Wei PH,Ni LY,Hua LY,Wen CD,Ying Z,Li C

更新日期：2016-01-01 00:00:00

abstract：:Infection with the human immunodeficiency virus type 1 (HIV) results in a chronic infection that progressively cripples the host immune defenses. HIV infection is associated with increased tryptophan (trp) catabolism by the cytokine-inducible enzyme indoleamine 2,3-dioxygenase (IDO). IDO has powerful immune suppressiv...

journal_title：Current drug metabolism

authors： Boasso A,Shearer GM

更新日期：2007-04-01 00:00:00

abstract：:Chronic heart failure (CHF) is now recognized as a multisystem disorder with increased sympathetic tone, hormonal derangements, an anabolic/catabolic imbalance, endothelial dysfunction, and systemic low-grade inflammation affecting various organ systems. Pro-inflammatory cytokines appear to play important roles in tha...

journal_title：Current drug metabolism

authors： Sandek A,Anker SD,von Haehling S

更新日期：2009-01-01 00:00:00

abstract：BACKGROUND:Clinical studies during pregnancy are rare due to ethical and practical limitations. Giving pregnant females the same dosing regimen used in adult males or nonpregnant females is inappropriate. Pregnancy physiologically-based pharmacokinetic modeling is a powerful tool that can be used to refine pharmacother...

journal_title：Current drug metabolism

authors： Alsmadi MM,Idkaidek N

更新日期：2018-01-01 00:00:00

abstract：BACKGROUND:Colorectal cancer is the third important cause of cancer-associated deaths across the world. Hence, there is an urgent need for understanding the complete mechanism associated with colorectal cancer, which in turn can be utilized toward early detection as well as the treatment of colorectal cancer in humans....

journal_title：Current drug metabolism

authors： Gupta MK,Vadde R,Sarojamma V

更新日期：2019-01-01 00:00:00

abstract：BACKGROUND:The metabolic/biotransformation pathways of atypical antipsychotics (aripiprazole, clozapine, iloperidone, olanzapine, paliperidone, quetiapine, risperidone, and ziprasidone) have been characterized and reviewed. However, comparisons of excretory pathways remain unexplored. OBJECTIVE:To analyze the excretio...

journal_title：Current drug metabolism

authors： Sheehan JJ,Sliwa JK,Amatniek JC,Grinspan A,Canuso CM

更新日期：2010-07-01 00:00:00

abstract：:5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT) belongs to a group of naturally-occurring psychoactive indolealkylamine drugs. It acts as a nonselective serotonin (5-HT) agonist and causes many physiological and behavioral changes. 5-MeO-DMT is O-demethylated by polymorphic cytochrome P450 2D6 (CYP2D6) to an active metab...

journal_title：Current drug metabolism

authors： Shen HW,Jiang XL,Winter JC,Yu AM

更新日期：2010-10-01 00:00:00

abstract：:The Cytochrome P450 4A subfamily is one of eighteen subfamilies in the CYP4 family and presently consists of twenty individual forms in nine different mammalian species. The major substrates for CYP4A forms are fatty acids, but recent studies have shown other non-fatty acid substrates may be metabolized by specific CY...

journal_title：Current drug metabolism

authors： Okita RT,Okita JR

更新日期：2001-09-01 00:00:00

abstract：:We report here a comprehensive evaluation of the effects of culture duration on the gene expression of P450 isoforms, uptake transporters and efflux transporters in human hepatocyte cultured in the absence and presence of the prototypical proinflammatory cytokine, interleukin-6 (IL-6). Primary collagen-matrigel sandwi...

journal_title：Current drug metabolism

authors： Yang Q,Doshi U,Li N,Li AP

更新日期：2012-09-01 00:00:00

abstract：BACKGROUND:In recent times, herbals or phytomedicines have become very popular due to their global acceptance as a complementary and alternative remedy. While modern drugs are commercially available only after laboratory validations, clinical trials, as well as approval from drug regulatory authorities, majority of the...

journal_title：Current drug metabolism

authors： Parvez MK,Rishi V

更新日期：2019-01-01 00:00:00

abstract：:We present a review of recent investigations of anticancer drug bexarotene in this article. As one of the novel synthetic analogs of retinoids, bexarotene selectively binds to and activates the retinoid X receptor (RXRs) subfamilies, exerting a prophylactic and therapeutic effect on a large series of tumors in vitro a...

journal_title：Current drug metabolism

authors： Qi L,Guo Y,Zhang P,Cao X,Luan Y

更新日期：2016-01-01 00:00:00