Aortic Binding of AZD5248: Mechanistic Insight and Reactivity Assays To Support Lead Optimzation.

abstract：:Developmental and reproductive toxicity (DART) end points are important hazard end points that need to be addressed in the risk assessment of chemicals to determine whether or not they are the critical effects in the overall risk assessment. These hazard end points are difficult to predict using current in silico tool...

journal_title：Chemical research in toxicology

authors： Wu S,Fisher J,Naciff J,Laufersweiler M,Lester C,Daston G,Blackburn K

更新日期：2013-12-16 00:00:00

abstract：:Quantum dots (QDs) are a novel class of inorganic fluorophores which are gaining widespread recognition as a result of their exceptional photophysical properties and their applications as a biomarker and in molecular biomedical imaging. The aim of this study was to evaluate the in vivo genotoxicity in mice exposed to ...

journal_title：Chemical research in toxicology

authors： Khalil WK,Girgis E,Emam AN,Mohamed MB,Rao KV

更新日期：2011-05-16 00:00:00

abstract：:The monoamine oxidase B (MAO-B) catalyzed oxidation of amines has been proposed to proceed via a polar pathway, an initial single-electron transfer pathway and an initial hydrogen atom transfer pathway. Results from previous studies on selected N-cyclopropyl-4-substituted-1,2,3,6-tetrahydropyridine derivatives have le...

journal_title：Chemical research in toxicology

authors： Nimkar SK,Anderson AH,Rimoldi JM,Stanton M,Castagnoli KP,Mabic S,Wang YX,Castagnoli N Jr

更新日期：1996-09-01 00:00:00

abstract：:Taconite mining involves potential exposure to non-asbestiform amphibole mineral fiber. More recent studies have demonstrated increased mortality from respiratory cancers and heart disease among workers in the taconite industry. This finding is not consistent with recent exposure assessment findings, nor is the toxico...

journal_title：Chemical research in toxicology

authors： Mandel JH,Ramachandran G,Alexander BH

更新日期：2016-02-15 00:00:00

abstract：:Acetaminophen (AP) is a popularly recommended over-the-counter analgesic-antipyretic in clinical use. However, the drug is handicapped by the occurrence of hepatotoxic insult following acute ingestion. Consequently, AP-induced hepatotoxicity is often implicated in accidental or suicidal overdose. In the current study,...

journal_title：Chemical research in toxicology

authors： Sahu A,Das D,Sahu P,Mishra S,Sakthivel A,Gajbhiye A,Agrawal R

更新日期：2020-02-17 00:00:00

abstract：:Contact allergy is caused by a wide range of chemicals after skin contact. Its clinical manifestation, allergic contact dermatitis (ACD), is developed upon repeated contact with the allergen. This perspective focuses on two areas that have yielded new useful information during the last 20 years: (i) structure-activity...

journal_title：Chemical research in toxicology

authors： Karlberg AT,Bergström MA,Börje A,Luthman K,Nilsson JL

更新日期：2008-01-01 00:00:00

abstract：:Four novel cadmium-chelating agents N,N'di(D-glucosyl)alkanediamine-N,N'-bis(carbodithioates) 4a-e were prepared as disodium salts of the general formula (CH2)n[N(CS2Na)CH2(CHOH)4CH2OH]2, where n = 7, 8, 10, and 12. They were synthesized by the reductive coupling of 2 mol of alpha-D-(+)-glucose (1) with 1 mol of the c...

journal_title：Chemical research in toxicology

authors： Singh PK,Jones MM,Kostial K,Blanusa M,Piasek M

更新日期：1996-01-01 00:00:00

abstract：:With CO2 present in excess, ONOO- reacts to form an adduct in solution and in the solid state, most likely ONOOCO2-. In solution, the adduct appears within 2 ms and absorbs at 300 with an extinction coefficient, which is either 50% or 100% (preferred) of that of ONOO-, 1.70 × 103 M-1 cm-1, and at 685 nm with an extinc...

journal_title：Chemical research in toxicology

authors： Serrano-Luginbuehl S,Kissner R,Koppenol WH

更新日期：2018-08-20 00:00:00

abstract：:DNA molecules utilize adenine, thymine, cytosine, and guanine for coding genetic information. In addition to these four canonical nucleobases, DNA molecules also contain a variety of modified nucleobases that can control and regulate gene expression and chromosome structure. Elucidating the functions of DNA modificati...

journal_title：Chemical research in toxicology

authors： Yuan BF

更新日期：2020-03-16 00:00:00

abstract：:Although selective estrogen receptor modulators (SERMs) are useful in the treatment and prevention of breast cancer, the SERM tamoxifen has been associated with an increased risk of endometrial cancer possibly due to metabolism to electrophilic quinoids. Another SERM, arzoxifene is currently in clinical trials for the...

journal_title：Chemical research in toxicology

authors： Liu H,Liu J,van Breemen RB,Thatcher GR,Bolton JL

更新日期：2005-02-01 00:00:00

abstract：:The binding conformations of single anti- and syn-BPDE-N2-dG adducts in oligonucleotides of varying base composition have been studied by induced circular dichroism (ICD) and light absorption spectroscopy. The sign of the ICD in single-stranded oligonucleotide adducts correlates with the absolute configuration of the ...

journal_title：Chemical research in toxicology

authors： Pradhan P,Jernström B,Seidel A,Nordén B,Gräslund A

更新日期：1999-05-01 00:00:00

abstract：:To obtain definitive information about the mechanisms of urinary calculus formation and the structural characteristics of the calculi induced by biphenyl administration in rats, with a focus on the sex dependency, the constituents of the urinary calculi were analyzed by HPLC, inductively coupled plasma spectroscopy (I...

journal_title：Chemical research in toxicology

authors： Ohnishi M,Yajima H,Yamamoto S,Matsushima T,Ishii T

更新日期：2000-08-01 00:00:00

abstract：:A methodology called quantitative component analysis of mixtures (QCAM) was used to analyze an existing set of product formulation data to determine if the irritating ingredients in the mixtures could be identified. Eye irritation scores, based on a rat model, for 18 mixtures having a composite total of 37 components,...

journal_title：Chemical research in toxicology

authors： Patel HC,Duca JS,Hopfinger AJ,Glendening CD,Thompson ED

更新日期：1999-11-01 00:00:00

abstract：:Exposure to arsenic affects large human populations worldwide and has been associated with a long list of human diseases, including skin, bladder, lung, and liver cancers, diabetes, and cardiovascular disorders. In addition, there are large individual differences in susceptibility to arsenic-induced diseases, which ar...

journal_title：Chemical research in toxicology

authors： Lu K,Cable PH,Abo RP,Ru H,Graffam ME,Schlieper KA,Parry NM,Levine S,Bodnar WM,Wishnok JS,Styblo M,Swenberg JA,Fox JG,Tannenbaum SR

更新日期：2013-12-16 00:00:00

abstract：:The effect of trans-1,2-dichloroethylene (DCE), an inhibitor of cytochrome P450 (P450) 2E1, on the catalytic activities and total content of hepatic P450 was determined in vivo and in vitro. Hepatic microsomes were prepared from groups of rats prior to dosing and at 2, 5, 12, and 24 h postdosing, and total P450 conten...

journal_title：Chemical research in toxicology

authors： Mathews JM,Etheridge AS,Raymer JH,Black SR,Pulliam DW Jr,Bucher JR

更新日期：1998-07-01 00:00:00

abstract：:All pesticides must go through a rigorous risk assessment process in order to show that they are safe for use.With respect to dermal risk assessment for re-entry workers, the absorption value applied to predict systemic dose from this external exposure is obtained by testing liquid forms of the pesticide in vivo and/o...

journal_title：Chemical research in toxicology

authors： Clarke JF,Cordery SF,Morgan NA,Knowles PK,Guy RH

更新日期：2015-02-16 00:00:00

abstract：:Formyl chloride has been indirectly implicated as an intermediate in the oxidation of CH(2)Cl(2) and proposed to be a product of the oxidation of some other compounds. Formyl chloride was synthesized and added to aqueous solutions, with CO formed as a product. The presence of glutathione (GSH) did not reduce the yield...

journal_title：Chemical research in toxicology

authors： Watanabe K,Guengerich FP

更新日期：2006-08-01 00:00:00

abstract：:Magnesium is directly involved in the control of cell growth and survival, but its role in cancer biology and therapy is multifaceted; in particular, it is highly controversial whether magnesium levels can affect therapy outcomes. Here we investigated whether magnesium availability can modulate cellular responses to t...

journal_title：Chemical research in toxicology

authors： Trapani V,Luongo F,Arduini D,Wolf FI

更新日期：2016-03-21 00:00:00

abstract：:Aminoglutethimide (AMG) is an aromatic amine aromatase inhibitor associated with a high incidence of idiosyncratic blood dyscrasias, especially agranulocytosis. Animal models of idiosyncratic drug reactions (IDRs) represent essential tools to study these reactions; however, there is currently no valid model of idiosyn...

journal_title：Chemical research in toxicology

authors： Ng W,Uetrecht J

更新日期：2013-08-19 00:00:00

abstract：:Mouse models are powerful tools to study the developmental neurotoxicity of polychlorinated biphenyls (PCBs); however, studies of the oxidation of chiral PCB congeners to potentially neurotoxic hydroxylated metabolites (OH-PCBs) in mice have not been reported. Here, we investigate the atropselective oxidation of chira...

journal_title：Chemical research in toxicology

authors： Wu X,Duffel M,Lehmler HJ

更新日期：2013-11-18 00:00:00

abstract：:Organic electrophiles have been recognized as important components of the exposome that can be characterized as cumulative totality of exposure in the organism in response to environmental perturbation. For such compounds, chemical reactivity may contribute significantly to the toxicological profile through covalent a...

journal_title：Chemical research in toxicology

authors： Böhme A,Laqua A,Schüürmann G

更新日期：2016-06-20 00:00:00

abstract：:Structure-function relationships for the inhibition of human cytochrome P450s (P450s) 1A1, 1A2, 1B1, 2C9, and 3A4 by 33 flavonoid derivatives were studied. Thirty-two of the 33 flavonoids tested produced reverse type I binding spectra with P450 1B1, and the potencies of binding were correlated with the abilities to in...

journal_title：Chemical research in toxicology

authors： Shimada T,Tanaka K,Takenaka S,Murayama N,Martin MV,Foroozesh MK,Yamazaki H,Guengerich FP,Komori M

更新日期：2010-12-20 00:00:00

abstract：:Five major products (adducts A(1a), A(1b), A(2), A(3,) and B) from the reaction of guanosine (Guo) with 4-oxo-2(E)-nonenal (ONE) were detected by liquid chromatography-mass spectrometry (LC-MS). Tandem MS (MS/MS) analysis of these compounds suggested that modifications to the nucleoside had been introduced. Adducts A(...

journal_title：Chemical research in toxicology

authors： Zhu P,Lee SH,Wehrli S,Blair IA

更新日期：2006-06-01 00:00:00

abstract：:Cholyl adenylate is a putative intermediate for biosynthesis of cholic acid-coenzyme A (CoA) thioester conjugates by acyl-CoA synthetase. Early studies showed the conjugated acid anhydride moiety of cholyl adenylate to be reactive, attacking proteins to form protein-cholic acid adducts. In the present study, to clarif...

journal_title：Chemical research in toxicology

authors： Takamura-Enya T,Mano N,Kawahara N,Goto J,Wakabayashi K

更新日期：2005-11-01 00:00:00

abstract：:Estrogen exposure through early menarche, late menopause, and hormone replacement therapy increases the risk factor for hormone-dependent cancers. Although the molecular mechanisms are not completely established, DNA damage by quinone electrophilic reactive intermediates, derived from estrogen oxidative metabolism, is...

journal_title：Chemical research in toxicology

authors： Chandrasena RE,Edirisinghe PD,Bolton JL,Thatcher GR

更新日期：2008-07-01 00:00:00

abstract：:Furanoid 8-epidiosbulbin E acetate (EEA) is one of the most abundant diterpenoid lactones in herbal medicine Dioscorea bulbifera L. (DB). Our early work proved that EEA could be metabolized to EEA-derived cis-enedial (EDE), a reactive intermediate, which is required for the hepatotoxicity observed in experimental anim...

journal_title：Chemical research in toxicology

authors： Zhou S,Zhang N,Hu Z,Lin D,Li W,Peng Y,Zheng J

更新日期：2020-07-20 00:00:00

abstract：:To reveal the roles of Y family DNA polymerases in the mutagenesis induced by oxidatively damaged DNA precursors, 2-hydroxy-dATP (2-OH-dATP) and 8-hydroxy-dGTP (8-OH-dGTP) were introduced into Escherichia coli strains deficient in the Y family polymerases, DNA polymerase IV (pol IV, encoded by the dinB gene) and DNA p...

journal_title：Chemical research in toxicology

authors： Satou K,Yamada M,Nohmi T,Harashima H,Kamiya H

更新日期：2005-08-01 00:00:00

abstract：:Understanding the molecular basis of inorganic chemical toxicity has lagged behind the proliferation of detailed mechanisms that explain the biochemical toxicology of many organic xenobiotics. In this perspective, general barriers to explicating the bioinorganic chemistry of toxic metals are considered, followed by a ...

journal_title：Chemical research in toxicology

authors： Petering DH

更新日期：2017-01-17 00:00:00

abstract：:Many cyanobacterial species are able to produce cyanotoxins as secondary metabolites. Among them, microcystins (MC) are a group of around 80 congeners of toxic cyclic heptapeptides. MC-LR is the most studied MC congener, in view of its high acute hepatotoxicity and tumor promoting activity. Humans may be exposed to cy...

journal_title：Chemical research in toxicology

authors： Buratti FM,Scardala S,Funari E,Testai E

更新日期：2011-06-20 00:00:00

abstract：:Inorganic arsenic is a strong carcinogen, possibly by interaction with the telomere length. The aim of the study was to evaluate how chronic arsenic exposure from drinking water as well as the arsenic metabolism efficiency affect the individual telomere length and the expression of telomere-related genes. Two hundred ...

journal_title：Chemical research in toxicology

authors： Li H,Engström K,Vahter M,Broberg K

更新日期：2012-11-19 00:00:00