Characterization of an etoposide-glutathione conjugate derived from metabolic activation by human cytochrome p450.

abstract：:Vasopressin (AVP) and its receptors play a pivotal role in maintaining body homeostasis under physiological and pathophysiological conditions. As a consequence, the vasopressin system has emerged as an important target for both diagnostic and therapeutic applications in a number of medical conditions. Stoichiometric g...

journal_title：Current drug metabolism

authors： Szczepanska-Sadowska E,Zera T,Sosnowski P,Cudnoch-Jedrzejewska A,Puszko A,Misicka A

更新日期：2017-01-01 00:00:00

abstract：:The transcription factor networks that regulate basal and xenobiotic-modulated expression of the hepatic sulfotransferases affect the dynamics of xenobiotic detoxication, carcinogen bioactivation and metabolic homeostasis. Emerging evidence suggests that liver-enriched transcription factors, the aryl hydrocarbon (Ah) ...

journal_title：Current drug metabolism

authors： Runge-Morris M,Kocarek TA

更新日期：2005-08-01 00:00:00

abstract：:Part I of this article published in the previous issue of Current Drug Metabolism discussed the substrate specificity, inhibitor selectivity and structure-activity relationship (SAR) of human CYP2C9. The features of CYP2C9 pharmacophore and SAR models have been elaborated. Part II of this article will address the homo...

journal_title：Current drug metabolism

authors： Mo SL,Zhou ZW,Yang LP,Wei MQ,Zhou SF

更新日期：2009-12-01 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

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:Glioblastoma multiforme, one of the most aggressive brain tumors, has a very poor clinical outcome. Despite the introduction of the alkylating reagent temozolomide (TMZ) to surgery and radiotherapy, the survival of patients could only be modestly increased up to less than 15 months. Therefore, innovative tre...

journal_title：Current drug metabolism

authors： Shevtsov M,Multhoff G

更新日期：2016-01-01 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：:The present study was designed to investigate the hepatic disposition of the prodrug AM365 and the generated antiviral guanosine analogue, AM188 in the isolated perfused rat liver (IPL). The livers of rats (n=12) were isolated and perfused with Krebs-Henseleit pH 7.4 buffer to which AM365 was added as a bolus to achie...

journal_title：Current drug metabolism

authors： Wang J,Nation RL,Evans AM,Cox S,Shackleford D

更新日期：2005-10-01 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：:During the lifetime, our cells encounter many challenges to their own existence. The survival of organisms and cells depends on the interplay within a complex, yet precisely orchestrated network of proteins. Since the discovery of the Rel/NF-kappaB family of transcription factors, the research has never come to a stop...

journal_title：Current drug metabolism

authors： Zineldeen DH,Uranishi H,Okamoto T

更新日期：2010-03-01 00:00:00

abstract：:With the recent advancement in nanoscience and nanotechnology, there is a growing demand for assessment of the toxicological effects of nano materials to humans and other biological systems. And a predictive toxicology approach that uses in vitro screening assays in conjunction with in vivo study results are widely em...

journal_title：Current drug metabolism

authors： Suma RN,Mohanan PV

更新日期：2015-01-01 00:00:00

abstract：:Evaluation and optimization of drug metabolism and pharmacokinetic data plays an important role in drug discovery and development and several reliable in vitro ADME models are available. Recently higher throughput in vitro ADME screening facilities have been established in order to be able to evaluate an appreciable f...

journal_title：Current drug metabolism

authors： Hop CE,Cole MJ,Davidson RE,Duignan DB,Federico J,Janiszewski JS,Jenkins K,Krueger S,Lebowitz R,Liston TE,Mitchell W,Snyder M,Steyn SJ,Soglia JR,Taylor C,Troutman MD,Umland J,West M,Whalen KM,Zelesky V,Zhao SX

更新日期：2008-11-01 00:00:00

abstract：:Knowledge regarding cytochrome P450 (P450) is crucial to the fields of drug therapy and drug development, as well as in our understanding of the mechanisms underlying the metabolic activation of potentially toxic and carcinogenic compounds. Escherichia coli is the most extensively utilized host in the production of re...

journal_title：Current drug metabolism

authors： Yun CH,Yim SK,Kim DH,Ahn T

更新日期：2006-05-01 00:00:00

abstract：:Transporters for organic anions and organic cations in kidney, liver, intestine, brain, and placenta play essential roles in drug disposition. The cloning and characterization of these transporters have significantly advanced our understanding of the molecular and cellular mechanisms of the drug disposition process. T...

journal_title：Current drug metabolism

authors： You G

更新日期：2004-02-01 00:00:00

abstract：:In recent years several arylpiperazine derivatives have reached the stage of clinical application, mainly for the treatment of depression, psychosis or anxiety. Examples are the pyrimidinylpiperazine buspirone, the chlorophenylpiperazine derivatives nefazodone and trazodone, the dichlorophenylpiperazine aripiprazole a...

journal_title：Current drug metabolism

authors： Caccia S

更新日期：2007-08-01 00:00:00

abstract：:Hepatotoxicity related to antidepressive pharmacotherapy is a major safety concern, particularly considering that severe forms of hepatic failure with fatal outcome have been reported. Severe hepatotoxic adverse drug reactions were also reported for agomelatine (AGM), an antidepressive agent, which was approved for th...

journal_title：Current drug metabolism

authors： Gahr M,Kratzer W,Fuchs M,Connemann BJ

更新日期：2014-01-01 00:00:00

abstract：:With the advances in recombinant DNA biotechnology, molecular biology and immunology, the number of biotech drugs, including peptides, proteins and monoclonal antibodies, available for clinical use has dramatically increased in recent years. Although pharmacokinetic principles are equally applicable to the large molec...

journal_title：Current drug metabolism

authors： Lin JH

更新日期：2009-09-01 00:00:00

abstract：:Maternal antenatal therapy with glucocorticoids (GC) is routinely used to prevent lung immaturity. The potential harmful effects on other organs, including in particular the central nervous system (CNS), are still controversial. In the present review we aimed to investigate: i) the beneficial and detrimental effects o...

journal_title：Current drug metabolism

authors： Gazzolo D,Serpero LD,Frigiola A,Abella R,Dro Giamberti A,Li Volti G,Michetti F

更新日期：2013-02-01 00:00:00

abstract：:This paper reviews the metabolism of new designer drugs of abuse that have emerged on the black market during the last years and is an update of a review published in 2005. The presented review contains data concerning the so-called 2C compounds (phenethylamine type) such as 4-bromo-2,5-dimethoxy-beta-phenethylamine (...

journal_title：Current drug metabolism

authors： Meyer MR,Maurer HH

更新日期：2010-06-01 00:00:00

abstract：:Cytochromes P450 of the liver are involved in maintenance of lipid homeostasis (cholesterol, vitamin D, oxysterol and bile acid metabolism) and in detoxification processes of endogenous compounds (i. e. bile acids) and xenochemicals (drugs). This review describes the roles of various CYPs in production of cholesterol ...

journal_title：Current drug metabolism

authors： Hafner M,Rezen T,Rozman D

更新日期：2011-02-01 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：:Recently, it was found that mutations in the binding cavity of drug-metabolizing Cytochrome P450 BM3 mutants can result in major changes in regioselectivity in testosterone (TES) hydroxylation. In the current work, we report the intrinsic reactivity of TES' C-H bonds and our attempts to rationalize experimentally obse...

journal_title：Current drug metabolism

authors： de Beer SB,van Bergen LA,Keijzer K,Rea V,Venkataraman H,Guerra CF,Bickelhaupt FM,Vermeulen NP,Commandeur JN,Geerke DP

更新日期：2012-02-01 00:00:00

abstract：:Gender differences in drug concentrations, drug response and toxicity have been attributed to various distinct yet interrelated physiological and molecular mechanisms. Drug transporters and metabolising enzymes play an important role in the xenobiotic cascade and are important regulators of drug disposition at the mol...

journal_title：Current drug metabolism

authors： Bebawy M,Chetty M

更新日期：2009-05-01 00:00:00

abstract：:Pharmacokinetic studies conducted in patients with CRF demonstrate that the nonrenal clearance of multiple drugs is reduced. Although the mechanism by which this occurs is unclear, several studies have shown that CRF affects the metabolism of drugs by inhibiting key enzymatic systems in the liver, intestine and kidney...

journal_title：Current drug metabolism

authors： Pichette V,Leblond FA

更新日期：2003-04-01 00:00:00

abstract：:Fluoropyrimidines and oxaliplatin continued to be the mainstay of therapeutic regimens in the treatment of colorectal cancer (CRC). For this reason, pharmacokinetic and metabolism of these drugs were analyzed and the identification of accurate and validated predictive, prognostic and toxicity markers became necessary ...

journal_title：Current drug metabolism

authors： Gnoni A,Russo A,Silvestris N,Maiello E,Vacca A,Marech I,Numico G,Paradiso A,Lorusso V,Azzariti A

更新日期：2011-12-01 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：:Currently the major research highlights of bioengineering and medical technology are directed towards development of improved diagnostic techniques to screen complex diseases. Screening requirements are to identify the cause of illnesses, monitor improvement or progression of the state of diseases such as cancer, card...

journal_title：Current drug metabolism

authors： Savaliya R,Shah D,Singh R,Kumar A,Shanker R,Dhawan A,Singh S

更新日期：2015-01-01 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：:Superparamagnetic iron oxide nanoparticles (SPIONs) have attracted a lot of interest due to their widespread diagnostic and therapeutic applications in neuro-oncology. Functinalization of the particles surface with targeting molecules that recognize tumor receptors might be exploited for the specific brain tumor targe...

journal_title：Current drug metabolism

authors： Shevtsov MA

更新日期：2016-06-15 00:00:00

abstract：:Several epidemiological studies throughout the years have suggested that polyphenols from fruits and vegetables promote health and reduce the risk of certain chronic and neurodegenerative diseases. Yet, it has been proved to be extremely difficult to quantitatively establish the benefit afforded by polyphenols, princi...

journal_title：Current drug metabolism

authors： Rubió L,Macià A,Motilva MJ

更新日期：2014-01-01 00:00:00