In vitro cytochrome P450 inhibition and induction.

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：: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：:Arachidonic acid (AA) is metabolized by enzymes of the cytochrome P450 (CYP) 4A and CYP4F subfamilies to 20- hydroxyeicosatetraeonic acid (20-HETE), which plays an important role in the cardiovascular system. In the current work, we reviewed the formation of 20-HETE in different species by different CYPs; 20-HETE meta...

journal_title：Current drug metabolism

authors： Elshenawy OH,Anwar-Mohamed A,El-Kadi AO

更新日期：2013-07-01 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：:Advances in high-throughput technologies to measure genome-scale changes of genes, proteins, and other biomolecular components ('omics') in complex biological systems have dramatically revolutionized biomedical research. However, the benefits of utilizing omics information in drug development have not yet been fully r...

journal_title：Current drug metabolism

authors： Fang H,Wang K,Zhang J

更新日期：2008-12-01 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:Malignant tumors are the leading cause of death in humans. Due to the tedious efforts and investigations made in the field of marine drug discovery, there is now a scientific bridge between marine and pharmaceutical sciences. However, currently only few marine drugs have been lined towards anticancer directi...

journal_title：Current drug metabolism

authors： Shakeel E,Arora D,Jamal QMS,Akhtar S,Khan MKA,Kamal MA,Siddiqui MH,Lohani M,Arif JM

更新日期：2018-01-01 00:00:00

abstract：BACKGROUND:Despite recent therapeutic advances, osteoarthritis continues to be a challenging health problem, especially in the elderly population. Opioids, which are potent analgesics, have shown an extraordinary ability to reduce intense pain in many osteoarthritic clinical trials; however, there is an increased need ...

journal_title：Current drug metabolism

authors： Alhaj-Suliman SO,Milavetz G,Salem AK

更新日期：2020-01-01 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：AIMS:Because of the high affinity of these animal neurotoxin proteins for some special target site, they were usually used as pharmacological tools and therapeutic agents in medicine to gain deep insights into the function of the nervous system. BACKGROUND AND OBJECTIVE:The animal neurotoxin proteins are one of the mo...

journal_title：Current drug metabolism

authors： Yu Y,Wang S,Wang Y,Cao Y,Yu C,Pan Y,Su D,Lu Q,Zuo Y,Yang L

更新日期：2020-01-01 00:00:00

abstract：:The aim of the present study was to develop and improve methods for phenotyping of CYP2E1, an important enzyme in the biotransformation of many industrial chemicals, therapeutic drugs and endogenous substances. The possibility to measure CYP2E1 activity in lymphocytes by using p-nitrophenol as a substrate and CYP2E1 p...

journal_title：Current drug metabolism

authors： Ernstgård L,Johanson G,Karlsson AS,Warholm M

更新日期：2007-06-01 00:00:00

abstract：BACKGROUND:Methotrexate (MTX) is a folate analogue with high therapeutic efficiency in the treatment of cancers and autoimmune diseases. The efficacy and toxicity of MTX may be altered by genetic polymorphisms in genes involved in MTX metabolic pathway. Personalized pharmacotherapy based on gene polymorphisms enables a...

journal_title：Current drug metabolism

authors： Cao M,Guo M,Wu DQ,Meng L

更新日期：2018-01-01 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：:Oral administration remains the most preferred route for the treatment of many diseases due to its convenience and adaptability. However, the presystemic metabolism may be an important barrier that prevents lipophilic drugs from achieving their pharmacological effects following oral delivery. Nano-based drug delivery ...

journal_title：Current drug metabolism

authors： Zhang Z,Gao F,Jiang S,Ma L,Li Y

更新日期：2012-10-01 00:00:00

abstract：:Glucuronidation is responsible for the clearance of a diverse range of drug and chemicals whose topology confers properties that complicate in vitro-in vivo clearance correlations as compared to those possible for oxidative metabolism. The active site of the UGTs faces the inside of the luminal space of the endoplasmi...

journal_title：Current drug metabolism

authors： Lin JH,Wong BK

更新日期：2002-12-01 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：: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：: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: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：:Cytochrome P450s (P450 or CYPs) comprise a superfamily of enzymes that catalyze the oxidation of a wide variety of xenobiotic chemicals. Although most of P450 inhibitors decrease the metabolic activities mediated by the corresponding P450 forms, unexpected phenomena, which are called as activation or heterotropic coop...

journal_title：Current drug metabolism

authors： Niwa T,Murayama N,Yamazaki H

更新日期：2008-06-01 00:00:00

abstract：:Human genome sequencing highlights the involvement of genetic variation towards differential risk of human diseases, presence of different phenotypes, and response to pharmacological elements. This brings the field of personalized medicine to forefront in the era of modern health care. Numerous recent approaches have ...

journal_title：Current drug metabolism

authors： Prakash S,Agrawal S

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: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 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：:The nature and level of systemic exposure to the active herbal constituents will profoundly affect their effects at action sites, which is fundamental in understanding their roles in the overall beneficial effects of a herbal medicine. The objective of this study is to gain a full picture of the systemic exposure to v...

journal_title：Current drug metabolism

authors： Li L,Zhao Y,Du F,Yang J,Xu F,Niu W,Ren Y,Li C

更新日期：2012-06-01 00:00:00

abstract：BACKGROUND:Hepatocellular carcinoma (HCC) is among the world's most common cancers. For over ten years, the only medical treatment for it has been the multikinase inhibitor Sorafenib. Currently, however, other first or second-line therapeutic options have also shown efficacy against HCC, such as multikinase inhibitors ...

journal_title：Current drug metabolism

authors： Galati G,Massimo Vainieri AF,Maria Fulgenzi CA,Di Donato S,Silletta M,Gallo P,Onorato A,Vespasiani-Gentilucci U,Picardi A

更新日期：2020-01-01 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：: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：: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：BACKGROUND:The prolonged circulation time of nanoparticles in the blood is a prerequisite to realize a controlled and targeted (passive or active targeting) release of the encapsulated gene/drug at the desired site of action. The most popular method to mask or camouflage nanoparticles is the adsorbed, grafted or conjug...

journal_title：Current drug metabolism

authors： Hu J,Sheng Y,Shi J,Yu B,Yu Z,Liao G

更新日期：2018-01-01 00:00:00