Metabolism of bioconjugate therapeutics: why, when, and how?

abstract：:The multiple functions of NAD(P)H:quinone oxidoreductase 1 (NQO1, DT-diaphorase) in the cell are reviewed. NQO1 has long been viewed as a chemoprotective enzyme involved in cellular defense against the electrophilic and oxidizing metabolites of xenobiotic quinones. It also participates in reduction of endogenous quino...

journal_title：Drug metabolism reviews

authors： Ross D

更新日期：2004-10-01 00:00:00

abstract：:The present paper has discussed available test systems for determination of the response of G-6-PD-deficient human erythrocytes to environmental agents. The limitations and advantages of each model have been examined, and the results of research using each model have been presented. The future development of suitable ...

journal_title：Drug metabolism reviews

authors： Horton HM,Calabrese EJ

更新日期：1986-01-01 00:00:00

abstract：:1. The metabolic activity of the gastrointestinal microflora can be modified by numerous factors derived from the host, the host's environment, and the flora itself. 2. Marked differences exist in microbial composition and metabolism of the gut floras of different species of animal, and in the degree of colonization o...

journal_title：Drug metabolism reviews

authors： Rowland IR

更新日期：1988-01-01 00:00:00

abstract：:This article reviews the regulatory, social, policy, and other issues that will shape the development of pharmacogenomics applications. We identify and analyze 19 key public policy issues, ranging from the economic incentives for linked diagnostic-drug development, to the regulation of tests and drugs, and to privacy ...

journal_title：Drug metabolism reviews

authors： Garrison LP Jr,Carlson RJ,Carlson JJ,Kuszler PC,Meckley LM,Veenstra DL

更新日期：2008-01-01 00:00:00

abstract：:The physiological and biochemical measurements that can be performed noninvasively in humans with modern imaging techniques offer great promise for defining the precise state of a patient's disease and its response to therapy. In general, there are two critical points in drug development when PET measurements are like...

journal_title：Drug metabolism reviews

authors： Fischman AJ,Alpert NM,Babich JW,Rubin RH

更新日期：1997-11-01 00:00:00

abstract：:Indirect evidence for the participation of cytochrome P450 (P450) in the microsomal N-oxygenation of primary and N-substituted amine functions is presented by studies employing diagnostic modifiers of the hemoprotein system as well as immunochemical approaches. Experiments with recombinant hemoproteins or isozymes pur...

journal_title：Drug metabolism reviews

authors： Hlavica P

更新日期：2002-08-01 00:00:00

abstract：:The reabsorptive and excretory capacity of the kidney has an important influence on the systemic concentration of drugs. Multidrug resistance proteins (MRP/ABCC) expressed in the kidney play a critical role in the tubular efflux of a wide variety of drugs and toxicants, and, in particular, of their negatively charged ...

journal_title：Drug metabolism reviews

authors： van de Water FM,Masereeuw R,Russel FG

更新日期：2005-01-01 00:00:00

abstract：:Pregnane X receptor (PXR) and constitutive active/androstane receptor (CAR), members of the nuclear receptor superfamily, are two major xeno-sensing transcription factors. They can be activated by a broad range of lipophilic xenobiotics including therapeutics drugs. In addition to xenobiotics, endogenous compounds suc...

journal_title：Drug metabolism reviews

authors： Kodama S,Negishi M

更新日期：2013-11-01 00:00:00

abstract：:The CYP4 family of cytochrome P450 enzymes and the mammalian peroxidases covalently bind their heme groups. In the CYP4 enzymes this involves one, and in the peroxidases two, covalent ester links between heme methys and carboxylic acid side-chains. In addition, in myeloperoxidase, a methionine forms a sulfonium link t...

journal_title：Drug metabolism reviews

authors： Ortiz de Montellano PR

更新日期：2008-01-01 00:00:00

abstract：:Monkeys, especially macaques, including cynomolgus (Macaca fascicularis) and rhesus monkeys (Macaca mulatta), are frequently used in drug metabolism studies due to their evolutionary closeness to humans. Recently, numerous cytochrome P450 (P450 or CYP) cDNAs have been identified and characterized in cynomolgus and rhe...

journal_title：Drug metabolism reviews

authors： Uno Y,Iwasaki K,Yamazaki H,Nelson DR

更新日期：2011-08-01 00:00:00

abstract：:Most foreign compounds, including nonnutrients in foods and vapors in air, undergo extensive metabolism before they are eliminated from the body. Included in this paper are discussions of the urinary clearance of various kinds of foreign compounds, the nonspecific enzymes that catalyze the formation of many metabolite...

journal_title：Drug metabolism reviews

authors： Gillette JR

更新日期：1979-01-01 00:00:00

abstract：:Xenobiotic metabolism, a ubiquitous natural response to foreign compounds, elicits initiating signals for many pathophysiological events. Currently, most widely used techniques for identifying xenobiotic metabolites and metabolic pathways are empirical and largely based on in vitro incubation assays and in vivo radiot...

journal_title：Drug metabolism reviews

authors： Chen C,Gonzalez FJ,Idle JR

更新日期：2007-01-01 00:00:00

abstract：:Flavin-containing monooxygenases (FMOs) are important oxidative drug metabolizing enzymes. FMO3 is the primary human adult liver FMO enzyme, but is developmentally regulated. FMO3 promoter characterization using in vitro DNA binding assays with HepG2 cell and fetal and adult liver nuclear protein, as well as FMO3/repo...

journal_title：Drug metabolism reviews

authors： Klick DE,Hines RN

更新日期：2007-01-01 00:00:00

abstract：:When target organ toxicity arises in animal models during routine drug safety evaluation, it raises several key questions: Is this target organ toxicity related to the pharmacology? What is the mode of action (MOA)? Is the target organ toxicity relevant to humans? Pathology or prior knowledge of the compound class may...

journal_title：Drug metabolism reviews

authors： Roberts R,Cain K,Coyle B,Freathy C,Leonard JF,Gautier JC

更新日期：2003-11-01 00:00:00

abstract：:At present, the methods and enzymology of the UDP-glucuronosyltransferases (UGTs) lag behind that of the cytochromes P450 (CYPs). About 15 human UGTs have been identified, and knowledge about their regulation, substrate selectivity, and tissue distribution has progressed recently. Alamethicin has been characterized as...

journal_title：Drug metabolism reviews

authors： Fisher MB,Paine MF,Strelevitz TJ,Wrighton SA

更新日期：2001-08-01 00:00:00

abstract：:Gold Nanostars (GNS) have attracted tremendous attention toward themselves owing to their multi-branched structure and unique properties. These state of the art metallic nanoparticles possess intrinsic features like remarkable optical properties and exceptional physiochemical activities. These star-shaped gold nanopar...

journal_title：Drug metabolism reviews

authors： Mousavi SM,Zarei M,Hashemi SA,Ramakrishna S,Chiang WH,Lai CW,Gholami A

更新日期：2020-05-01 00:00:00

abstract：:Mineral fibers, including asbestos, are ubiquitous contaminants of the environment. Asbestos fibers are generally present at levels below 1 fiber/L in air though 10 fibers/L may be found in cities; these levels do not appear to be high enough to present a hazard to health. These fibers come mostly from the use of fibr...

journal_title：Drug metabolism reviews

authors： Hoskins JA,Brown RC

更新日期：1994-01-01 00:00:00

abstract：:The cytochrome P450 (P450) field came out of interest in the metabolism of drugs, carcinogens, and steroids, which remain major focal points. Over the years we have come to understand the P450 system components, the multiplicity of P450s, and many aspects of the regulation of the genes and also the catalytic mechanism...

journal_title：Drug metabolism reviews

authors： Guengerich FP

更新日期：2004-05-01 00:00:00

abstract：:N-acetyltransferase 1 (NAT1), a polymorphic Phase II enzyme, plays an essential role in metabolizing heterocyclic and aromatic amines, which are implicated in urinary bladder cancer (BCa). This systematic review investigates a possible association between the different NAT1 genetic polymorphisms and BCa risk. Medline,...

journal_title：Drug metabolism reviews

authors： Dhaini HR,El Hafi B,Khamis AM

更新日期：2018-05-01 00:00:00

abstract：:Voriconazole, a second-generation triazole frequently used for the prophylaxis and treatment of invasive fungal infections, undergoes complex metabolism mainly involving various (polymorphic) cytochrome P450 enzymes in humans. Although high inter- and intraindividual variability in voriconazole pharmacokinetics have b...

journal_title：Drug metabolism reviews

authors： Schulz J,Kluwe F,Mikus G,Michelet R,Kloft C

更新日期：2019-08-01 00:00:00

abstract：:Acetaminophen (APAP, paracetamol, N-acetyl-p-aminophenol) is a widely used analgesic that is safe at therapeutic doses but is a major cause of acute liver failure (ALF) following overdose. APAP-induced hepatotoxicity is related to the formation of an electrophilic reactive metabolite, N-acetyl-p-benzoquinone imine (NA...

journal_title：Drug metabolism reviews

authors： Coen M

更新日期：2015-02-01 00:00:00

abstract：:Human cytochrome P450 (CYP) 3A subfamily members (mainly CYP3A4 and CYP3A5) mediate the metabolism of approximately half all marketed drugs and thus play a critical role in the drug metabolism. A huge number of studies on CYP3A-mediated drug metabolism in humans have demonstrated that CYP3A activity exhibits marked et...

journal_title：Drug metabolism reviews

authors： Liu YT,Hao HP,Liu CX,Wang GJ,Xie HG

更新日期：2007-01-01 00:00:00

abstract：:Historically, failure rates in drug development are high; increased sophistication and investment throughout the process has shifted the reasons for attrition, but the overall success rates have remained stubbornly and consistently low. Only 8% of new entities entering clinical testing gain regulatory approval, indica...

journal_title：Drug metabolism reviews

authors： Maharao N,Antontsev V,Wright M,Varshney J

更新日期：2020-05-01 00:00:00

abstract：:The cannabinoid receptor 1 (CB1) is a G protein-coupled receptor (GPCR) that is located primarily in the central nervous system. CB1 is a therapeutic target which may impact pathways to mediate pain, neurodegenerative disorders, hunger, and drug-seeking behavior. Despite these benefits, development of orthosteric ther...

journal_title：Drug metabolism reviews

authors： Dopart R,Lu D,Lichtman AH,Kendall DA

更新日期：2018-02-01 00:00:00

abstract：:Human CYP1A2 is one of the major CYPs in human liver and metabolizes a number of clinical drugs (e.g., clozapine, tacrine, tizanidine, and theophylline; n > 110), a number of procarcinogens (e.g., benzo[a]pyrene and aromatic amines), and several important endogenous compounds (e.g., steroids). CYP1A2 is subject to rev...

journal_title：Drug metabolism reviews

authors： Zhou SF,Wang B,Yang LP,Liu JP

更新日期：2010-05-01 00:00:00

abstract：:For patients undergoing cardiopulmonary bypass (CPB) during cardiac surgery, there are well-documented changes in the pharmacokinetics (PK) of commonly administered drugs. Although multiple factors potentially underpin these changes, there has been scant research attention on the impact of CPB to alter the activities ...

journal_title：Drug metabolism reviews

authors： Adiraju SKS,Shekar K,Fraser JF,Smith MT,Ghassabian S

更新日期：2018-05-01 00:00:00

abstract：:Nano-hydroxyapatite (nano-HA) is a material with multiple uses due to its biocompatibility and its resemblance to the nonorganic bone structure. It is used in various dental domains such as implantology, surgery, periodontology, esthetics and prevention. The aim of this study is to provide a wide understanding of nano...

journal_title：Drug metabolism reviews

authors： Bordea IR,Candrea S,Alexescu GT,Bran S,Băciuț M,Băciuț G,Lucaciu O,Dinu CM,Todea DA

更新日期：2020-05-01 00:00:00

abstract：:The recent progresses in molecular biology and pharmacology approaches allowed the characterization of a series of nuclear receptors (NRs) as efficient regulators of uridine diphosphate glucuronosyltransferase (UGT) genes activity. These regulatory processes ensure an optimized UGT expression in response to specific e...

journal_title：Drug metabolism reviews

authors： Bigo C,Caron S,Dallaire-Théroux A,Barbier O

更新日期：2013-02-01 00:00:00

abstract：:Global statistical data shed light on an alarming trend that every year thousands of people die due to adverse drug reactions as each individual responds in a different way to the same drug. Pharmacogenomics has come up as a promising field in drug development and clinical medication in the past few decades. It has em...

journal_title：Drug metabolism reviews

authors： Chaudhary R,Singh B,Kumar M,Gakhar SK,Saini AK,Parmar VS,Chhillar AK

更新日期：2015-08-01 00:00:00

abstract：:Chemicals that cause toxicity though a direct mechanism, such as acetaminophen, covalently bind to a select group of proteins prior to the development of toxicity, and these proteins may be important in the initiation of the events that lead to the hepatotoxicity. Disruption of the cell is measured by release of intra...

journal_title：Drug metabolism reviews

authors： Pumford NR,Halmes NC,Hinson JA

更新日期：1997-02-01 00:00:00