Complexities of glucuronidation affecting in vitro in vivo extrapolation.

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：: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：: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：:Etoposide (VP-16), a DNA topoisomerase II poison widely used as an antineoplastic agent is also known to cause leukemia. One of its major metabolic pathways involves O-demethylation to etoposide catechol (etoposide-OH) by cytochrome P450 3A4 (CYP3A4). The catechol metabolite can undergo sequential one- and two-electro...

journal_title：Current drug metabolism

authors： Zheng N,Pang S,Oe T,Felix CA,Wehrli S,Blair IA

更新日期：2006-12-01 00:00:00

abstract：:This review focuses on identification of the important active site residues of CYP2D6 in terms of CYP2D6 polymorphism. A meta-analysis was performed on the reported literature regarding (1) values of the Michaelis-Menten constant (K(m)), maximal velocity (V(max)), and intrinsic clearance (V(max)/K(m)) for 41 metabolic...

journal_title：Current drug metabolism

authors： Niwa T,Murayama N,Yamazaki H

更新日期：2011-06-01 00:00:00

abstract：:Ageing is characterized by a progressive decline in the functional reserve of multiple organs and systems, which can influence drug disposition. In addition, comorbidity and polypharmacy are highly prevalent in the elderly. As ageing is associated with some reduction in first-pass metabolism, bioavailability of a few ...

journal_title：Current drug metabolism

authors： Shi S,Klotz U

更新日期：2011-09-01 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：: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

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：:P-glycoprotein (P-gp) is involved in MDR and in neurodegenerative disorders such as Parkinson disease (PD), Alzheimer disease (AD) and epilepsy. Cytochrome P450 enzymes (CYP450s) catalyze the metabolism of a wide variety of endogenous and exogenous compounds including xenobiotics, drugs, environmental toxins, steroids...

journal_title：Current drug metabolism

authors： Inglese C,Perrone MG,Berardi F,Perrone R,Colabufo NA

更新日期：2011-10-01 00:00:00

abstract：BACKGROUND:Bioequivalence studies are a vital part of drug development. The average bioequivalence approach is the standard method of assessment to conclude whether the generic product is bioequivalent to the innovator product. Of late, debates are on whether the average bioequivalence approach adequately addresses dru...

journal_title：Current drug metabolism

authors： Micheal F,Sayana M,Prasad R,Motilal BM

更新日期：2020-01-01 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：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：BACKGROUND:Mutation in the B RAF at V600E has been well implicated in the carcinogenesis that makes it as an attractive therapeutictarget. In the present study, we sought to identify the basis of V600E mutation at functional and structural grounds. The study also endeavors in identification of small molecule as a poten...

journal_title：Current drug metabolism

authors： Bandaru S,Sumithnath TG,Sharda S,Lakhotia S,Sharma A,Jain A,Hussain T,Nayarisseri A,Singh SK

更新日期：2017-07-21 00:00:00

abstract：:Membrane transporters play an important role in intestinal absorption, distribution and clearance of drugs. Additionally transporters along with enzymes regulate tissue exposures (e.g. liver, kidney and brain), which are important for safety and efficacy considerations. Early identification of transporters involved gu...

journal_title：Current drug metabolism

authors： Taskar KS,Harada I,Alluri RV

更新日期：2021-01-01 00:00:00

abstract：:In the recent decades, the use of herbal products has been rapidly growing in the Western countries. While their use in many cases causes adverse effects, to date, safety issues of herbal products have not been adequately addressed. It is rarely determined whether the non-purported bioactive constituents in the herbs ...

journal_title：Current drug metabolism

authors： Li N,Xia Q,Ruan J,Fu PP,Lin G

更新日期：2011-11-01 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：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：:Understanding the mechanism of action of organophosphates (OP)/nerve agents -- irreversible acetylcholinesterase (AChE, EC 3.1.1.7) inhibition at the cholinergic synapses followed by metabolic dysbalance of the organism -- two therapeutic principles for antidotal treatment are derived. The main drugs are anticholinerg...

journal_title：Current drug metabolism

authors： Bajgar J,Kuca K,Jun D,Bartosova L,Fusek J

更新日期：2007-12-01 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：:Glucuronidation represents a major pathway which enhances the elimination of many lipophilic xenobiotics and endobiotics to more water-soluble compounds. The UDP-glucuronosyltransferase (UGT) family catalyzes the glucuronidation of the glycosyl group of a nucleotide sugar to an acceptor compound (aglycone) at a nucleo...

journal_title：Current drug metabolism

authors： King CD,Rios GR,Green MD,Tephly TR

更新日期：2000-09-01 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：:Decarboxylation, reduction and hydrolysis can yield active metabolites from the parent drug. Major therapeutic indications and metabolic routes of these drugs are reviewed. Changes in the logP values (determined and calculated) from the parent drug to the active metabolite show certain characteristics in comparison to...

journal_title：Current drug metabolism

authors： Hartyánszky I,Kalász H,Adeghate E,Gulyás Z,Hasan MY,Tekes K,Adem A,Sótonyi P

更新日期：2012-07-01 00:00:00

abstract：BACKGROUND:Nanoparticles (NPs) are being used extensively owing to their increased surface area, targeted delivery and enhanced retention. NPs have the potential to be used in many disease conditions. Despite widespread use, their toxicity and clinical safety still remain a major concern. OBJECTIVE:The purpose of this...

journal_title：Current drug metabolism

authors： Malaviya P,Shukal D,Vasavada AR

更新日期：2019-01-01 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: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：OBJECTIVES:Induction or inhibition of cytochrome P450 (CYP) enzyme activities, enzymes that activate or detoxify xenobiotics, is one mechanism by which vegetables may alter cancer risk. As the effect of food on CYP enzyme activities have not been studied in the Jordanian population, we examined the effect of supplement...

journal_title：Current drug metabolism

authors： Hakooz N,Hamdan I

更新日期：2007-01-01 00:00:00

abstract：:This review provides a vista of the current opportunities and remaining challenges in the area of in vitro-in vivo extrapolation, with particular emphasis on drug binding terms in predictive models, which has been the source of much controversy. Although the importance of fu(inc) (fraction unbound in in vitro incubati...

journal_title：Current drug metabolism

authors： Grime K,Riley RJ

更新日期：2006-04-01 00:00:00

abstract：:Graphene possesses a wide range of potential biomedical applications because of the unique physical and chemical properties. However, the side effects of grapheme and its derivatives on a number of biological models even on human body are still not very clear. Therefore, to properly assess the potential risk of graphe...

journal_title：Current drug metabolism

authors： Xu C,Wang J,Xu Y,Shang G,Wang R,Lin Y

更新日期：2013-10-01 00:00:00

abstract：BACKGROUND:In the last few years, the use of modified Carbon Nanomaterials (CNMs) for theranostics (therapeutic and diagnosis) applications is a new and rapidly growing area in pharmacy and medical fields. Owing to this, their specific physicochemical behaviors like high stability, drug loading, surface area to volume ...

journal_title：Current drug metabolism

authors： Gupta N,Rai DB,Jangid AK,Kulhari H

更新日期：2019-01-01 00:00:00