Search results for "Heterocyclic compound"
showing 10 items of 382 documents
Inflammation in the Human Periodontium Induces Downregulation of the α1- and β1-Subunits of the sGC in Cementoclasts
2021
Nitric oxide (NO) binds to soluble guanylyl cyclase (sGC), activates it in a reduced oxidized heme iron state, and generates cyclic Guanosine Monophosphate (cGMP), which results in vasodilatation and inhibition of osteoclast activity. In inflammation, sGC is oxidized and becomes insensitive to NO. NO- and heme-independent activation of sGC requires protein expression of the &alpha
Über den Chemismus von Zustandsänderungen des Aktomyosins
1950
(1) By means of a simple method the conditions were investigated for contraction and relaxation of actomyosin (AM) under the influence of potassium, magnesium, and calcium ions, of adenosintriphosphate (ATP) or muscle-adenylic-acid and phosphocreatin.
2,3,7,8-Tetrachlorodibenzo-p-dioxin-Dependent Release from Contact Inhibition in WB-F344 Cells: Involvement of Cyclin A
2002
2,3,7,8-Tetrachlorodibenzo-p-dioxin (TCDD) is the most potent tumor promoter ever tested in rodents. Although it is known that most of TCDD actions are mediated by binding to the aryl hydrocarbon receptor (AhR), the mechanisms leading to tumor promotion still remain to be elucidated. Loss of contact inhibition is one characteristic hallmark in tumorigenesis. In rat liver epithelial WB-F344 cells, TCDD induces a release from contact inhibition, which is manifested by a twofold increase in cell number when TCDD (1 nM for 48 h) is added to confluent cells in the presence of serum, but not when given to exponentially growing or subconfluent, serum-deprived WB-F344 cells. Loss of G1 arrest was a…
Optimization of anti-proliferative activity using a screening approach with a series of bis-heterocyclic G-quadruplex ligands
2013
Abstract Using a phenotypic screening and SAR optimization approach, a phenyl-bis-oxazole derivative has been identified with anti-proliferative activity, optimized with the use of a panel of cancer cell lines. The lead compound was synthesized by means of a short and effective two-step synthesis using Pd-catalyzed direct arylation. The compound stabilizes several quadruplex DNA sequences including a human telomeric DNA and one from the promoter of the HSP90 gene, although the structure–activity relationships of the series are not obviously related to the quadruplex binding.
NODAPA-OH and NODAPA-(NCS)n: Synthesis, 68Ga-radiolabelling and in vitro characterisation of novel versatile bifunctional chelators for molecular ima…
2008
This report concerns synthesis, (68)Ga-radiolabelling and stability data of 1,4,7-triazacyclononane-1,4-diacetic acid-7-p-isothio-cyanatophenyl-acetic acid (NODAPA-NCS), 1,4,7-triazacyclononane-1-acetic acid-4,7-di-p-isothiocyanatophenyl-acetic acid (NODAPA-(NCS)(2)) and 1,4,7-triazacyclononane-1,4-diacetic acid-7-p-hydroxyphenyl-acetic acid (NODAPA-OH), versatile bifunctional chelators with potential for molecular imaging. Protein binding and exemplified conjugation are also reported.
Epoxidation of benzo[a]pyrene-7,8-dihydrodiol by human CYP1A1 in reconstituted membranes. Effects of charge and nonbilayer phase propensity of the me…
2002
Human cytochrome P4501A1 (CYP1A1) is one of the key enzymes in the bioactivation of environmental pollutants such as benzo[a]pyrene (B[a]P) and other polycyclic aromatic hydrocarbons. To evaluate the effect of membrane properties and distinct phospholipids on the activity of human CYP1A1 purified insect cell-expressed human CYP1A1 and of human NADPH-P450 reductase were reconstituted into phospholipid vesicle membranes. Conversion rates of up to 36 pmol x min(-1) x pmol(-1) CYP1A1 of the enantiomeric promutagens (-)- and (+)-trans-7,8-dihydroxy-7,8-dihydro-B[a]P (7,8-diol) to the genotoxic diolepoxides were achieved. The highest rates were obtained when negatively charged lipids such as phos…
A quantitative method of photoadsorption determination for irradiated catalyst in liquid–solid system
2009
WOS: 000266963000002
Chloroplast DNA evidence for introgression and long distance dispersal in the desert annualSenecio flavus (Asteraceae)
1995
Phylogenetic analysis of chloroplast DNA (cpDNA) restriction site variation supports a close genetic relationship between the Southwest AsianSenecio flavus subsp.breviflorus and the North AmericanS. mohavensis. The intercontinental disjunct distribution of these two desert annuals may have originated via long distance dispersal. The chloroplast genomes of the Southern and North AfricanS. flavus subsp.flavus and subsp.breviflorus differ by at least ten restriction sites, while at most two restriction sites differentiate the cpDNA genomes of subsp.breviflorus and the outgroupS. squalidus. This suggests that the cpDNA genome ofS. flavus subsp.breviflorus may have resulted from introgression an…
Gas—liquid chromatographic analyses
1989
Abstract The retention (I), dispersion (IM) and selectivity (I*) indices of sixteen polychlorinated dibenzo-p-dioxins and fourteen polychlorinated dibenzofurans were determined on a low-polarity HP-5 capillary column using a gas chromatograph connected with an ion-selective detector. IM and I* values were also calculated for all 73 dibenzo-p-dioxins from the di- to the octachloro isomer and for all possible 135 chlorinated dibenzofurans based on the predicted retention index data reported earlier. The effect of the position of chlorination is shown and the results are compared with those for several series of chlorinated aromatics.
Stereoselective Metabolic Activation of Dibenzo[a,l]Pyrene in the Human Mammary Carcinoma Cell Line MCF-7 Results in Formation of (-)-antiand (+)-syn…
1996
Abstract Dibenzo[a,l]pyrene (DB[a,l]P) is an important polycyclic aromatic hydrocarbon because of possible human exposure and its exceptionally high carcinogenicity in rodents. We examined the metabolism of DB[a,l]P and the formation of DB[a,l]P-DNA adducts in the human mammary carcinoma cell line (MCF-7). Analysis of the DNA adducts by 33P-postlabeling, immobilized boronate chromatography, HPLC and TLC demonstrated that DB[a,l]P is stereoselectively metabolized to specific optical isomers of DB[a,l]P-11,12-diol-13,14-epoxide (DB[a,l]PDE). The major anti-DB[a,l]PDE adduct formed in DB[a,l]P-treated MCF-7 cells resulted from reaction of (-)-anti-DB[a,l]PDE with DNA whereas the two major syn-…