Computational predictions of the site of metabolism of cytochrome P450 2D6 substrates: comparative analysis, molecular docking, bioactivation and toxicological implications.

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：: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：: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：: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：:The Pharmacogenetics and Pharmacogenomics Knowledge Base (PharmGKB: http://www.pharmgkb.org) is devoted to disseminating primary data and knowledge in pharmacogenetics and pharmacogenomics. We are annotating the genes that are most important for drug response and present this information in the form of Very Important ...

journal_title：Drug metabolism reviews

authors： Sangkuhl K,Berlin DS,Altman RB,Klein TE

更新日期：2008-01-01 00:00:00

abstract：:S-carboxymethyl-L-cysteine, the side-chain carboxymethyl derivative of the sulfur-containing amino acid, cysteine, has been known and available for almost 80 years. During this time, it has been put to a variety of uses, but it is within the field of respiratory medicine that, presently, it has found a clinical niche....

journal_title：Drug metabolism reviews

authors： Mitchell SC,Steventon GB

更新日期：2012-05-01 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：: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：: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：: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：: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：: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：: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：: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：: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：: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：: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：: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：:An association between marijuana use and schizophrenia has been noted for decades, and the recent emergence of high-efficacy synthetic cannabinoids (SCBs) as drugs of abuse has lead to a growing number of clinical reports of persistent psychotic effects in users of these substances. The mechanisms underlying SCB-elici...

journal_title：Drug metabolism reviews

authors： Fantegrossi WE,Wilson CD,Berquist MD

更新日期：2018-02-01 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：: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：: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：: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：: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：: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：:Hyperbilirubinemia may accompany harmful effects such as jaundice, brain dysfunction, and pharmacokinetic alterations of drugs. Clinical drugs are the important causes of hyperbilirubinemia, especially for patients with certain pathologic conditions or with genetic variations. This article reviews hyperbilirubinemic p...

journal_title：Drug metabolism reviews

authors： Ah YM,Kim YM,Kim MJ,Choi YH,Park KH,Son IJ,Kim SG

更新日期：2008-01-01 00:00:00

abstract：:The high rate of attrition during drug development and its associated high research and development (R&D) cost have put pressure on pharmaceutical companies to ensure that candidate drugs going to clinical testing have the appropriate quality such that the biological hypothesis could be evaluated. To help achieve this...

journal_title：Drug metabolism reviews

authors： Ballard P,Brassil P,Bui KH,Dolgos H,Petersson C,Tunek A,Webborn PJ

更新日期：2012-08-01 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：: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：:Traditional Chinese medicine (TCM) has a long history of medical use in China and is still used worldwide. Unexpected herb-drug interactions (HDIs) may lead to adverse drug reactions or loss of therapeutic efficacy of the victim drug. Here, based on searches of Medline, EBSCO, Science Direct and Web of Science using v...

journal_title：Drug metabolism reviews

authors： Ma BL,Ma YM

更新日期：2016-01-01 00:00:00