HIV-1 reverse transcriptase inhibitors: current issues and future perspectives.

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：: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：:The assessment of in vitro inhibition and induction of the cytochrome P450 enzymes of the liver is a critical part of the drug discovery and development process in order to ensure that two or more drugs can be safely coadministered without alterations in exposure. Early assessment of potential candidates using high th...

journal_title：Current drug metabolism

authors： Walsky RL,Boldt SE

更新日期：2008-11-01 00:00:00

abstract：: ...

journal_title：Current drug metabolism

authors： Wei JF

更新日期：2018-01-01 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：:This paper reviews the empirical methods of quantitative microdialysis that have been used to interpret the results obtained from pharmacokinetic studies. The concept of extraction efficiency or recovery and the properties of recovery in vivo (variation with flow rate, time dependency and influence of the mode of admi...

journal_title：Current drug metabolism

authors： Cano-Cebrián MJ,Zornoza T,Polache A,Granero L

更新日期：2005-04-01 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：:The pharmacological effects of a drug are highly dependent on the absorption, metabolism, elimination, and distribution of the drug. In the past few years it has become apparent that transport proteins play a major role in regulating the distribution, elimination and metabolism of some drugs. As a consequence of our n...

journal_title：Current drug metabolism

authors： Hochman JH,Yamazaki M,Ohe T,Lin JH

更新日期：2002-06-01 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：: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：: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：: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：:Personalized medicine has gained significant attention over the last decade as technologies for understanding biological differences between individuals have advanced dramatically. There are many potential benefits of personalized medicine including minimizing risk of drug toxicity, increasing benefit from drugs used,...

journal_title：Current drug metabolism

authors： Sorich MJ,McKinnon RA

更新日期：2012-09-01 00:00:00

abstract：:Phenolic compounds are commonly found in natural sources like plant-based foods and beverages. These compounds have received much attention due to their unique biological properties. Polyphenols possess a significant binding affinity for serum albumins which are known to be principal extracellular proteins with a high...

journal_title：Current drug metabolism

authors： Jaldappagari S,Balakrishnan S,Hegde AH,Teradal NL,Narayan PS

更新日期：2013-05-01 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：:The combined treatment with anticonvulsant and antidepressant drugs is reported in both neurologic and psychiatric practice; it is, therefore, evident that the issue of managing such type of polytherapy is frequently encountered by clinicians. To review current literature on pharmacokinetic interactions between antico...

journal_title：Current drug metabolism

authors： Mula M

更新日期：2008-10-01 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

abstract：:The binding of drugs with serum proteins can affect the activity, distribution, rate of excretion, and toxicity of pharmaceutical agents in the body. One tool that can be used to quickly analyze and characterize these interactions is high-performance affinity chromatography (HPAC). This review shows how HPAC can be us...

journal_title：Current drug metabolism

authors： Hage DS,Anguizola J,Barnaby O,Jackson A,Yoo MJ,Papastavros E,Pfaunmiller E,Sobansky M,Tong Z

更新日期：2011-05-01 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：BACKGROUND:Neuropsychiatric diseases primarily characterized by dementia stand third in the global list of diseases causing disability. The poor water solubility, erratic oral absorption, low bioavailability, poor intestinal absorption, and the impeding action of the blood-brain barrier (BBB) are the major factors limi...

journal_title：Current drug metabolism

authors： Rehman S,Nabi B,Pottoo FH,Baboota S,Ali J

更新日期：2020-01-01 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：: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：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：: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：OBJECTIVE:Tyrosine kinase inhibitors (TKIs) are widely used drugs which have high availability in reducing the activity of BCR-ABL1 tyrosine kinase, therefore they play an indispensable role in the treatment of Chronic myeloid leukemia (CML). Imatinib, dasatinib and nilotinib have been proved to have absolute bioavaila...

journal_title：Current drug metabolism

authors： Wang R,Zhong C,Zhang C,Hua M,Ma D

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：BACKGROUND:Interleukin-28B (IL28B) locus on a human chromosomal region mapped to 19q13 execute immune defense against viruses. During Hepatitis C Virus (HCV) infection the IL28B has a promising role in deciding the consequence of infection for spontaneous clearance of viruses or causing chronic liver infection. Treatme...

journal_title：Current drug metabolism

authors： Asthana M,Sahu SK,Kumar A,Mohanty S,Chakrabarti S,Das P,Chattopadhya NR,Chatterjee K,Singh SP,Rajasubramaniam S,Choudhuri T

更新日期：2018-01-01 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：: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：: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