The impact of in vitro binding on in vitro-in vivo extrapolations, projections of metabolic clearance and clinical drug-drug interactions.

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：BACKGROUND:Thiopurine antimetabolites are important agents for the treatment of severe diseases, such as acute lymphoblastic leukemia and inflammatory bowel disease. Their pharmacological actions depend on biotransformation into active thioguanine-nucleotides; intracellular metabolism is mediated by enzymes of the salv...

journal_title：Current drug metabolism

authors： Pelin M,De Iudicibus S,Londero M,Spizzo R,Dei Rossi S,Martelossi S,Ventura A,Decorti G,Stocco G

更新日期：2016-01-01 00:00:00

abstract：:Brain, the centre of the nervous system and an integral part the body, is protected by two anatomical and physiological barriers- Blood-Brain Barrier (BBB) and Blood-Cerebrospinal Fluid Barrier (BCSFB). Blood-Brain Barrier is a very complex and highly organized multicellular structure that shields the brain from harmf...

journal_title：Current drug metabolism

authors： Sarkar A,Fatima I,Jamal QMS,Sayeed U,Khan MKA,Akhtar S,Kamal MA,Farooqui A,Siddiqui MH

更新日期：2017-01-01 00:00:00

abstract：BACKGROUND:It is well known that ethanol can cause significant morbidity and mortality, and much of the related toxic effects can be explained by its metabolic profile. OBJECTIVE:This work performs a complete review of the metabolism of ethanol focusing on both major and minor metabolites. METHOD:An exhaustive litera...

journal_title：Current drug metabolism

authors： Dinis-Oliveira RJ

更新日期：2016-01-01 00:00:00

abstract：:The occurrence of idiosyncratic adverse drug reactions during late clinical trials or after a drug has been released can lead to a severe restriction in its use and even in its withdrawal. Metabolic activation of relatively inert functional groups to reactive electrophilic intermediates is considered to be an obligato...

journal_title：Current drug metabolism

authors： Kalgutkar AS,Gardner I,Obach RS,Shaffer CL,Callegari E,Henne KR,Mutlib AE,Dalvie DK,Lee JS,Nakai Y,O'Donnell JP,Boer J,Harriman SP

更新日期：2005-06-01 00:00:00

abstract：BACKGROUND:The use of psychoactive substances is one of the most dangerous social problems worldwide. Nicotine dependence results from the interaction between neurobiological, environmental and genetic factors. Serotonin is a neurotransmitter that has a wide range of central nervous system activities. The serotonin tra...

journal_title：Current drug metabolism

authors： Kandemis E,Tuncel G,Asut O,Temel SG,Ergoren MC

更新日期：2020-01-01 00:00:00

abstract：:Toxicogenomics is defined as an integration of genomics (transcriptomics, proteomics and metabolomics) and toxicology. It is a scientific field that studies how the genome is involved in responses to environmental stressors and toxicants. It combines studies of mRNA expression, cell and tissue-wide protein expression ...

journal_title：Current drug metabolism

authors： Gomase VS,Tagore S

更新日期：2008-03-01 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：:Arylamine N-acetyltransferases (NAT) are xenobiotic-metabolizing enzymes responsible for the acetylation of many aromatic arylamine and heterocyclic amines, thereby playing an important role in both detoxification and activation of numerous drugs and carcinogens. Two closely related isoforms (NAT1 and NAT2) have been ...

journal_title：Current drug metabolism

authors： Rodrigues-Lima F,Dairou J,Dupret JM

更新日期：2008-07-01 00:00:00

abstract：:A amyloid-β (Aβ) plaque formation in the brain is known to be the root cause of Alzheimer's disease (AD), which affects the behavior, memory, and cognitive ability in humans. The brain starts undergoing changes several years before the actual appearance of the symptoms. Nanotechnology could prove to be an alternative ...

journal_title：Current drug metabolism

authors： Chauhan PS,Yadav D,Koul B,Mohanta YK,Jin JO

更新日期：2020-01-01 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：: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：: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：:The M2 proton channel is translated by the M gene segment of influenza viruses, and has been adopted as an attractive target for influenza A viruses, on which a series of adamantane-based drugs act. However, recently epidemic influenza viruses have had strong resistant effects against the adamantane-based drugs. In th...

journal_title：Current drug metabolism

authors： Yu Y,Li X,Hao P,Wang JF,Chou KC

更新日期：2014-01-01 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 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：:The pressing need for targeting, detecting, monitoring, and treating diseased cells concomitantly gives rise to multi-functional nanomedicines, especially those that can combine diagnostic and therapeutic abilities, which are referred to as nanotheranostics. Recently, nanotheranostics are of significant clinical inter...

journal_title：Current drug metabolism

authors： Han N,Yang YY,Wang S,Zheng S,Fan W

更新日期：2013-07-01 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

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：:There are several clinically useful endoperoxides, mainly artemisinin derivatives available in market for the treatment of malaria. These are highly potent drugs, with fastest parasite reduction ratio, broadest parasite stage specificity and effectiveness against all species of plasmodium in human. Endoperoxides are c...

journal_title：Current drug metabolism

authors： Gautam A,Ahmed T,Batra V,Paliwal J

更新日期：2009-03-01 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：:Modern biologics are biotechnology-derived pharmaceuticals. They are mostly used for diagnosis, prevention and treatment of serious and chronic diseases. Today, therapeutic biologics range from traditional biologics like blood and blood components, fractionated blood products, and antitoxins to modern biologics such a...

journal_title：Current drug metabolism

authors： Baumann A

更新日期：2006-01-01 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：: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：BACKGROUND:Drug-metabolizing enzymes and transporters play key roles in drug disposition and drug interactions. The alterations of their expression will influence drug pharmacokinetics and pharmacodynamics. However, the changes in the expression of enzymes and transporters in the disease state are still unclear. OBJEC...

journal_title：Current drug metabolism

authors： Dong Y,Gong L,Lu X,Ye M,Lin Y,Xie S,Zhang J,Zhou F,Tang L,Zou W,Liu M

更新日期：2020-01-01 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：: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：:This review provides an overview of the in vitro methods currently used in studies of intestinal drug metabolism and active efflux with a special emphasis on the efflux- metabolism interplay. These methods include e.g. expressed enzymes or efflux transporters, fractionated intestinal cells, cell lines, primary cells, ...

journal_title：Current drug metabolism

authors： Siissalo S,Heikkinen AT

更新日期：2013-01-01 00:00:00

abstract：:When used at a high dose, many anticancer drugs produce undesirable side effects including hepatotoxicity. Transdermal delivery bypasses first-pass metabolism, allowing the use of a lower dose of drug while decreasing systemic toxicity. In this review, we summarize various advanced technologies for improving anticance...

journal_title：Current drug metabolism

authors： Fang JY,Liu PF,Huang CM

更新日期：2008-09-01 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