Nuclear receptors and endobiotics glucuronidation: the good, the bad, and the UGT.

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：:Drug transporters and drug metabolism enzymes govern drug absorption, distribution, metabolism and elimination. Many literature works presenting important aspects related to stereochemistry of drug metabolism are available. However, there is very little literature on stereoselectivity of chiral drug transport and enan...

journal_title：Drug metabolism reviews

authors： Zhou Q,Yu LS,Zeng S

更新日期：2014-08-01 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：: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：:Numerous experimental and epidemiological studies have demonstrated that polycyclic aromatic hydrocarbons (PAHs), which are major constituents of cigarette tobacco tar, are strongly involved in the pathogenesis of the cardiovascular diseases (CVDs). Knowing that PAH-induced toxicities are mediated by the activation of...

journal_title：Drug metabolism reviews

authors： Korashy HM,El-Kadi AO

更新日期：2006-01-01 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：: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：: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：: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：:The multistep, clonal evolution model of cancer predicts fundamental mechanisms by which chemicals may influence the cancer process. These are illustrated by studies of the mechanisms of induction of carcinogenesis by estrogens and the inhibition of carcinogenesis by caloric restriction. ...

journal_title：Drug metabolism reviews

authors： Barrett JC

更新日期：2000-05-01 00:00:00

abstract：:In this paper, we evaluate methodologies and null mouse models used to study drug transporter function in vitro and in vivo. P-glycoprotein and MRP null mice have been used to examine many aspects of xenobiotic distribution and bioavailability. Their advantage over conventional models is that they allow the exclusion ...

journal_title：Drug metabolism reviews

authors： Stanley LA,Horsburgh BC,Ross J,Scheer N,Wolf CR

更新日期：2009-01-01 00:00:00

abstract：:Bupropion is an atypical antidepressant of the aminoketone group, structurally related to cathinone, associated with a wide interindividual variability. An extensive pharmacokinetic and pharmacodynamic review of bupropion was performed, also focusing on chemical, pharmacological, toxicological, clinical and forensic a...

journal_title：Drug metabolism reviews

authors： Costa R,Oliveira NG,Dinis-Oliveira RJ

更新日期：2019-08-01 00:00:00

abstract：:Like any other drugs, antiallergic medications can be associated with large inter- and intraindividual variability in their disposition. The best-documented examples belong to the H1 antihistamines. Variable drugs are more likely to show unpredictable therapeutic response with both increased risks of side effects and ...

journal_title：Drug metabolism reviews

authors： Nicolas JM,Espie P,Molimard M

更新日期：2009-01-01 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：:Synthetic cannabinoids (SC), originally developed as research tools, are now highly abused novel psychoactive substances. We present a comprehensive systematic review covering in vivo and in vitro animal and human pharmacokinetics and analytical methods for identifying SC and their metabolites in biological matrices. ...

journal_title：Drug metabolism reviews

authors： Castaneto MS,Wohlfarth A,Desrosiers NA,Hartman RL,Gorelick DA,Huestis MA

更新日期：2015-05-01 00:00:00

abstract：:Population pharmacokinetics describe the typical relationships between physiology (both normal and disease altered) and pharmacokinetics, the interindividual variability in these relationships, and their residual intraindividual variability. Knowledge of population kinetics can help one to choose initial drug dosage, ...

journal_title：Drug metabolism reviews

authors： Sheiner LB

更新日期：1984-01-01 00:00:00

abstract：:Ronald Estabrook made his initial impact studying cytochrome P450 by demonstrating the oxidative metabolism function of this unique class of enzymes, which had an unusual spectral peak at 450 nm when reduced and in the presence of carbon monoxide. Utilizing a photochemical action spectrum, he demonstrated that a cytoc...

journal_title：Drug metabolism reviews

authors： Sheets JJ

更新日期：2007-01-01 00:00:00

abstract：:Much is known about the distal DNA damage repair response. In particular, many of the enzymes and auxiliary proteins that participate in DNA repair have been characterized. In addition, knowledge of signaling pathways activated in response to DNA damage is increasing. In contrast, comparatively less is known of DNA da...

journal_title：Drug metabolism reviews

authors： Monks TJ,Xie R,Tikoo K,Lau SS

更新日期：2006-01-01 00:00:00

abstract：:In summary, the concerns that environmental and other agents are causing adverse effects on reproductive function in humans are real, although the risk is not necessarily well characterized. The range of concerns for the types of effect that agents might have on reproduction span the full range of reproductive events....

journal_title：Drug metabolism reviews

authors： Schwetz BA

更新日期：1996-02-01 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 aim of this study was to evaluate diazepam and oxazepam as cytochrome P450 inducers at doses previously shown to cause liver tumors in mice but not rats. In rats, diazepam and oxazepam induced CYP2B, and were as effective as phenobarbital despite lacking phenobarbital's tumor-promoting effect in rats. In mice, dia...

journal_title：Drug metabolism reviews

authors： Parkinson A,Leonard N,Draper A,Ogilvie BW

更新日期：2006-01-01 00:00:00

abstract：:Aryl and heterocyclic amines are of particular interest because of their carcinogenicity. The N-hydroxy derivatives are formed by oxidation, usually by the cytochrome P450 (P450) enzymes and most often by P450 family 1. The mechanism of oxidation appears to resemble that of other P450 reactions. The N-hydroxy products...

journal_title：Drug metabolism reviews

authors： Guengerich FP

更新日期：2002-08-01 00:00:00

abstract：:Human tumors arise from multiple genetic changes that gradually transform growth-limited cells into highly invasive cells that are unresponsive to growth controls. The genetic evolution of normal cells into cancer cells is largely determined by the fidelity of DNA replication, repair, and division. Cell-cycle arrest i...

journal_title：Drug metabolism reviews

authors： Flatt PM,Pietenpol JA

更新日期：2000-08-01 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：:Cyclindole was extensively metabolized and eliminated primarily via the kidneys from most laboratory animals and man. Only in the dog was cyclindole a major urinary component. Cyclindole was metabolized by N-demethylation and/or hydroxylation. In studies utilizing radiolabeled drug, the primary urinary component was p...

journal_title：Drug metabolism reviews

authors： Edelson J,Benziger DP

更新日期：1980-01-01 00:00:00

abstract：:Psilocybin and psilocin are controlled substances in many countries. These are the two main hallucinogenic compounds of the "magic mushrooms" and both act as agonists or partial agonists at 5-hydroxytryptamine (5-HT)2A subtype receptors. During the last few years, psilocybin and psilocin have gained therapeutic releva...

journal_title：Drug metabolism reviews

authors： Dinis-Oliveira RJ

更新日期：2017-02-01 00:00:00

abstract：:The rat P450IIA subfamily was characterized at the protein, cDNA, and gene level. The purified IIA1 and IIA2 P-450s displayed distinct positional specificities toward hydroxylation of the prototype substrate testosterone. The IIA1 and IIA2 genes were also regulated differently during development; IIA1 was expressed wi...

journal_title：Drug metabolism reviews

authors： Gonzalez FJ,Matsunaga T,Nagata K

更新日期：1989-01-01 00:00:00

abstract：:Bioconjugation of therapeutic agents has been used as a selective drug delivery platform for many therapeutic areas. Bioconjugates are prepared by the covalent linkage of active compounds (small or large molecule) to a carrier molecule (lipids, proteins, peptides, carbohydrates, and polymers) through a chemical linker...

journal_title：Drug metabolism reviews

authors： Liu H,Bolleddula J,Nichols A,Tang L,Zhao Z,Prakash C

更新日期：2020-02-01 00:00:00

abstract：:The lung, which is in intimate contact with the external environment, is exposed to a number of toxicants both by virtue of its large surface area and because it receives 100% of the cardiac output. Lung diseases are a major disease entity in the U.S. population ranking third in terms of morbidity and mortality. Despi...

journal_title：Drug metabolism reviews

authors： Buckpitt A,Boland B,Isbell M,Morin D,Shultz M,Baldwin R,Chan K,Karlsson A,Lin C,Taff A,West J,Fanucchi M,Van Winkle L,Plopper C

更新日期：2002-11-01 00:00:00