排序方式: 共有105条查询结果,搜索用时 15 毫秒
61.
Bayram T Arslan O Ugras HI Cakir U Ozensoy O 《Journal of enzyme inhibition and medicinal chemistry》2007,22(6):739-744
The enzyme carbonic anhydrase (E.C. 4.2.1.1) has a stimulatory effect on glaucoma, an eye disease that has a risk to dogs, which are models for the human eye disease, that is similar to that in humans. In this study, some sulfonamide derivatives, 2-(3-cyclohexene-1-carbamido)-1,3,4-thiadiazole-5-sulfonamide (CCTS), 4-(3-cyclohexene-1-carbamido) methyl-benzenesulfonamide (CCBS), 2-(9-octadecenoylamido)-1,3,4-thiadiazole-5-sulfonamide (ODTS), 2-(4,7,10-trioxa-tetradecanoylamido)-1,3,4-thiadiazole-5-sulfonamide (TDTS), and 2-(8-methoxycoumarine-3-carbamido)-1,3,4-thiadiazole-5-sulfonamide (MCTS), as well as some anionic compounds (perchlorate and chloride) and existing medicines (dorzolamide-HCl, gentamicine sulphate, tropicamide, and procaine-HCl) were assayed for their inhibition of dog carbonic anhydrase (dCA), which was purified from erythrocytes on an affinity gel of L-tyrosine-sulfonamide-Sepharose 4B. ODTS showed the highest potency amongst the synthetic compounds with IC50 value 1.18 x 10(-5) M. Amongst the medicines tested, only dorzolamide showed inhibition with IC50 value 5.05 x 10(-4) M. Procaine and tropicamide actually showed an activatory effect, whereas gentamicine sulfate had no significant effect. The inhibitory effects of anionic compounds such as perchlorate and chloride were also investigated; whereas perchlorate showed inhibition, chloride did not. 相似文献
62.
Sercan O Hämmerling GJ Arnold B Schüler T 《Journal of immunology (Baltimore, Md. : 1950)》2006,176(2):735-739
IFN-gamma has a dual function in the regulation of T cell homeostasis. It promotes the expansion of effector T cells and simultaneously programs their contraction. The cellular mechanisms leading to this functional dichotomy of IFN-gamma have not been identified to date. In this study we show: 1) that expansion of wild-type CD8+ T cells is defective in IFN-gamma-deficient mice but increased in IFN-gammaR-deficient mice; and 2) that contraction of the effector CD8+ T cell pool is impaired in both mouse strains. Furthermore, we show that CD11b+ cells responding to IFN-gamma are sufficient to limit CD8+ T cell expansion and promote contraction. The data presented here reveal that IFN-gamma directly promotes CD8+ T cell expansion and simultaneously induces suppressive functions in CD11b+ cells that counter-regulate CD8+ T cell expansion, promote contraction, and limit memory formation. Thus, innate immune cells contribute to the IFN-gamma-dependent regulation of Ag-specific CD8+ T cell homeostasis. 相似文献
63.
The aminoglycoside-3'-phosphotransferase IIIa [APH(3')-IIIa] phosphorylates aminoglycoside antibiotics and renders them ineffective against bacteria. APH(3')-IIIa is the most promiscuous aminoglycoside phosphotransferase enzyme, and it modifies more than 10 different aminoglycoside antibiotics. A wealth of information exists about the enzyme; however, thermodynamic properties of enzyme-aminoglycoside complexes are still not known. This study describes the determination of the thermodynamic parameters of the binary enzyme-aminoglycoside and the ternary enzyme-metal-ATP-aminoglycoside complexes of structurally related aminoglycosides using isothermal titration calorimetry. Formation of the binary enzyme-aminoglycoside complexes is enthalpically driven and exhibits a strongly disfavored entropic contribution. Formation of the ternary enzyme-metal-ATP-aminoglycoside complexes yields much smaller negative DeltaH values and more favorable entropic contributions. The presence of metal-ATP generally increases the affinity of aminoglycosides to the enzyme. This is consistent with the kinetic mechanism of the enzyme in which ordered binding of substrates occurs. However, the observed DeltaH values neither correlate with kinetic parameters k(cat), K(m), and k(cat)/K(m) nor correlate with the molecular size of the substrates. Comparison of the thermodynamic properties of the complexes formed by structurally similar aminoglycosides indicated that the 2'- and the 6'-amino groups of the substrates are involved in binding to the enzyme. Thermodynamic properties of the complexes formed by aminoglycosides differing only at the 3'-hydroxyl group suggested that the absence of this group does not alter the thermodynamic parameters of the ternary APH(3')-IIIa-metal-ATP-aminoglycoside complex. Our results also indicate that protonation of ligand and protein ionizable groups is coupled to the complex formation between aminoglycosides and APH(3')-IIIa. Comparison of DeltaH values for different aminoglycoside-enzyme complexes indicates that enzyme and substrates undergo significant conformational changes in complex formation. 相似文献
64.
65.
Semra Isik Feray Kockar Meltem Aydin Oktay Arslan Ozen Ozensoy Guler Alessio Innocenti Andrea Scozzafava Claudiu T. Supuran 《Bioorganic & medicinal chemistry letters》2009,19(6):1662-1665
The protein encoded by the Nce103 gene of Saccharomyces cerevisiae, a β-carbonic anhydrase (CA, EC 4.2.1.1) designated as scCA, was investigated for its activation with amines and amino acids. scCA was poorly activated by amino acids such as l-/d-His, Phe, DOPA, Trp (KAs of 82–90 μM) and more effectively activated by amines such as histamine, dopamine, serotonin, pyridyl-alkylamines, aminoethyl-piperazine/morpholine (KAs of 10.2–21.3 μM). The best activator was l-adrenaline, with an activation constant of 0.95 μM. This study may help to better understand the catalytic/activation mechanisms of the β-CAs and eventually to design modulators of CA activity for similar enzymes present in pathogenic fungi, such as Candida albicans and Cryptococcus neoformans. 相似文献
66.
Mustafa Ozen 《American journal of human genetics》2004,74(1):192-193
67.
Takamiya M Ozen A Rasmussen M Alter T Gilbert T Ussery DW Knøchel S 《Standards in genomic sciences》2011,4(2):113-122
Campylobacter is one of the leading causes of food-borne gastroenteritis and has a high prevalence in poultry. Campylobacter jejuni subsp. jejuni 327 is a subspecies of the genus Campylobacter of the family Campylobacteraceae in the phylum Proteobacteria. The microaerophilic, spiral shaped, catalase positive bacterium obtains energy from the metabolism of amino acids and Krebs cycle intermediates. Strain 327 was isolated from a turkey slaughter production line and is considered environmentally sensitive to food processing (cold, heat, drying) and storage conditions. The 327 whole genome shotgun sequence of 1,618,613 bp long consists of 1,740 protein-coding genes, 46 tRNA genes and 3 rRNA operons. A protein based BLAST analysis places the turkey isolate 327 close to the human clinical strain 81116 (NCTC 11828). 相似文献
68.
Ozen OZENSOY Oktay ARSLAN Feray KOCKAR 《Journal of enzyme inhibition and medicinal chemistry》2013,28(4):579-585
Hypoxia is a common characteristic of locally advanced solid tumors that has been associated with diminished therapeutic response and malignant progression. Human carbonic anhydrase (hCA) hCA IX and XII isozymes are tumor associated isoforms which contribute to acidification of the tumor environment by catalyzing the hydration of carbon dioxide to bicarbonate and protons.In the present study our goal was to investigate the inhibition effects of 15 different antibiotics belonging to the following classes: Lactams, cephalosporins, macrolides etc., on the tumor associated carbonic anhydrase isozymes hCA-IX, hCA-XII and cytosolic carbonic anhydrase hCA-I and hCA-II. 相似文献
69.
M. A. Aladag Y. Turkoz H. Parlakpinar H. Ozen M. Egri S. C. Unal 《Neurochemical research》2009,34(11):1935-1944
In the present study, we investigated the in vivo effects of melatonin on SAH-induced cerebral vasospasm and oxidative stress,
resulting from SAH in an experimental rat model. Twenty-eight rats (225–250 g) were divided into four groups equally: group
1; control, group 2; SAH, group 3; SAH plus placebo, and group 4; SAH plus melatonin. We used double haemorrhage method for
SAH groups. Beginning 6 h after SAH, 20 mg/kg melatonin or equal volume of 0.9% saline was administered intraperitoneally
twice daily for 5 days to groups 3 and 4, respectively. Melatonin or 0.9% saline injections were continued up to fifth day
after SAH and rats were sacrificed at the end of this period. Brain sections at the level of the pons were examined by light
microscopy. The lumen diameter and the vessel wall thickness of basilar artery were measured using a micrometer. The serum
levels of cerebral vasodilator nitric oxide (NO), the brain levels of an intrinsic antioxidant superoxide dismutase (SOD)
and a NO regulator arginase activities were measured. The brain levels of inducible nitric oxide (iNOS) and nitrotyrosine,
a nitrosative stress parameter immunohistochemiacally determined. In conclusion, melatonin administration ameliorated cerebral
vasospasm by increasing serum NO level and decreasing the brain the levels of arginase and oxidative stress. It is therefore
possible that increased brain arginase activity after SAH may also have a significant role in the pathogenesis of vasospasm
by limiting the availability of arginine for NO production. 相似文献