qsar studies of sulfonamide carbonic anhydrase inhibitors

... functional and histological studies suggested the existence of several carbonic anhydrase isoforms in the trophosome tissue [16,17], indicating the possible existence of various CA isoforms in groups other ... number of transcripts instead of having a strong transcription promoter The fact that several genes can be the source of several isoforms in the branchial plume could increase global carbonic anhydrase ... was composed of lL of Moloney murine leukemia virus reverse transcriptase buffer; 0.5 lL of BSA (10 mgÆmL)1), lL of total RNA (1.24 lgÆlL)1), 2.5 lL of dNTP (4 mm total), 1.5 lL of Random Primer...

Ngày tải lên: 18/02/2014, 16:20

... results of RT-PCR, so we considered that the resistance may be related to a number of other differential genes associated with a variety of cellular functions, such as those encoding carbonic anhydrase ... the expression of MT2A was upregulated in Tca8113 ⁄ PYM cells MT2A, as the main isoform of MTs, may closely mediate the resistance of Tca8113 ⁄ PYM cells to PYM BMP2 is a member of the transforming ... because of the methylation of the promoter, and restoration of DKK1 expression can induce apoptosis and suppress colony formation [42] As a suppressor of cancer, the downregulated expression of DKK1...

Ngày tải lên: 06/03/2014, 22:21

... Characterization of CA XIII, a novel member of the carbonic anhydrase isozyme family J Biol Chem 279, 2719–2727 Carter ND, Lonnerholm G, Meyerson BJ & Wistrand PJ ¨ (2001) Androgen-linked control of carbonic ... expression of cytosolic carbonic anhydrase in human hepatocellular carcinoma Life Sci 73, 2211–2223 Kuo WH, Yang SF, Hsieh YS, Tsai CS, Hwang WL & Chu SC (2005) Differential expression of carbonic anhydrase ... (Fig 3A) Surprisingly, the viability of 5.61 cells was significantly less than Rat1 cells at each concentration of H2O2 (Fig 3A) The viability of the entire panel of cell populations was examined...

Ngày tải lên: 29/03/2014, 08:20

... (B) Examination of CA12 mRNA quantity by real-time PCR The quantity of CA12 gene was expressed as a ratio of mean quantity of CA12 to b-actin CA12 expression was similar to that of WD tumors, whereas ... Expression of the hypoxia-inducible and tumor-associated carbonic anhydrases in ductal carcinoma in situ of the breast Am J Pathol 2001, 158(3):1011-1019 Wilson GD, Dische S, Saunders MI: Studies ... of the ovary, the nonpigmented epithelium of ciliary processes, the distal convoluted tubule of the kidney, and the choroid plexus of the brain All of these tissues have highly specialized functions,...

Ngày tải lên: 09/08/2014, 09:20

... was about 11% of those of 49-week-old female WL-chickens, about 25% of those of 52-week-old male WL-chickens and 14 times of the levels of CA-II in erythrocytes of Beagles The levels of CA-II in ... 12.2 mg/g of Hb, and it was 59 times of the levels of CA-II in erythrocytes of Beagles The mean level of CA-II in hemolysate of 53-week-old female Araucana-chickens was 23.4 ± 1.78 mg/g of Hb It ... 1.78 mg/g of Hb These levels of CA-II were about 11% of those of 49-week-old female WL-chickens and about 25% of those of 52-week-old male WL-chickens There was a significant difference of CA-II...

Ngày tải lên: 12/08/2014, 18:22

... four inhibitors were selected to help clarify and elucidate the binding mode of this class of inhibitors Of particular interest was the disposition of the biphenyl groups in the S’ subsites of ... potent inhibitors of cysteine proteases Nitrile inhibitors with 1cyanopyrrolidinyl ring were shown to be potent inhibitors of the degradation of denaturated collagen by cathepsin K and of bone ... plasma and most of them are inhibitors of thrombin Others are inhibitors of coagulation proteins Factor Xa, Factor XIa or of fibrinolytic proteinases like plasmin The gene knock-out of the serpin...

Ngày tải lên: 14/09/2015, 14:09

... other studies [4-6] because of activity against key pathogens Consideration of the influence of appropriateness of empiric therapy against subsequently identified pathogens was beyond the scope of ... Discussion The results of this pooled analysis of two phase III studies indicated that initial use of doripenem in patients with VAP was associated with shorter durations of mechanical ventilation ... cost of hospitalization as demonstrated in a recent economic analysis of studies and [29] Using discrete event simulation, Kongnakorn and colleagues [29] estimated that use of doripenem instead of...

Ngày tải lên: 25/10/2012, 10:02

... underlying state of CNS dis-inhibition involved in the pathophysiology of the condition [93] Genetic linkage studies involving families with a history of alcoholism show involvement of chromosomes ... stimulus variation types Despite a relatively recent growth of interest in N2b characterization, a number of studies have probed the effect of stimulus and experimental condition variations on this ... notable that the detection of a frontal N2 is associated only with instances of a NOGO response Thus, the P300 appears to be inhibited by the appearance of the N2b in tasks of motor activity suppression...

Ngày tải lên: 02/11/2012, 11:08

... productivity and quality of the developed software The outcome of several of these improvement initiatives was summed up in an article in Communications of the ACM [10] Claims of order of magnitude improvements ... Problems with software development Software development can often be challenging There are many examples of software projects that have failed The much-cited Standish report on software projects ... we ask: Does the introduction of a knowledge management system: Improve the quality of software? Lower the cost of developing software? Improve the work situation of employees in an organisation?...

Ngày tải lên: 16/01/2014, 16:33

... Inexcitability Stimulus Rate of depolarization Suppression of AP generation Prolongation of refractory period = duration of inexcitability A Effects of antiarrhythmics of the Na+-channel blocking ... neurotransmitters The plasmalemma also harbors the sites of action of cardiac glycosides (the Na/K-ATPases, p 130), of Ca2+ antagonists (Ca2+ channels, p 122), and of agents that block Na+ channels (local anesthetics; ... degree of shortening, i.e., the force of contraction Sources of Ca2+ are: a) extracellular Ca2+ entering the cell through voltage-gated Ca2+ channels; b) Ca2+ stored in membranous sacs of the...

Ngày tải lên: 26/01/2014, 19:20

... rupture of veil, showing tendency to double annulus on the stem Portions of the veil also dripping from margin of pileus (Natural size.)] =The Color of the Gills.= The color of the gills of the ... Toxicology of Mushrooms, and Characters of Mushrooms, to which their names are appended, and also to Dr Chas Peck, of Albany, N Y., and Dr G Bresadola, of Austria-Hungary, to whom some of the specimens ... propagation of mushrooms The spawn is nothing more than the vegetative portion of the plant It is made up of countless numbers of delicate, tiny, white, jointed threads, the _mycelium_ =Mycelium of a...

Ngày tải lên: 13/02/2014, 12:20

... 2011 FEBS 545 N-acylsulfonamide-linked dinucleoside inhibitors of RNase A N Thiyagarajan et al Fig Superposition (stereo representation) of N-acylsulfonamide (gray) and N-acylsulfonamide (maroon) ... large N-Acylsulfonamide-linked dinucleosides as inhibitors of RNase A Given the efcacy of the sulfonimidyl group as a phosphoryl group surrogate, we sought to determine the advantage of adding ... Chemical structures of N-acylsulfonamide-linked nucleosides 47 Fig Isotherms for the binding of N-acylsulfonamide-linked dinucleosides to RNase A Data were tted to Eqn (1) (A) N-acylsulfonamide 7,...

Ngày tải lên: 14/02/2014, 22:20

... metabolic consequences of having HPRT deficiency are an overproduction of uric acid and elevated levels of PRPP [3] Patients having mutations resulting in partial HPRT deficiency often suffer from gouty ... analysis of a wide range of species indicates that HPRT have eleven completely conserved amino acids, whereas PRTFDC1 genes not show full conservation of these eleven residues [10,11] Because one of ... distances of approximately 2.4 A The phosphate of the GMP is hydrogen bonded to main chain and side chain atoms of amino acids 145–149 (Fig 1C) A second Ca2+ ion is coordinated by the side chain of...

Ngày tải lên: 15/02/2014, 01:20

... result of NADH oxidation was measured One unit of enzyme activity was defined as the reduction of lmolÆmin)1 of NADH (corresponding to the carboxylation of lmolÆmin)1 of acetyl-CoA) Quantification of ... extinction coefficient of 6200 m)1Æcm)1 One unit of enzyme activity was defined as the oxidation of lmolÆmin)1 of NADH POR enzyme assays The oxidative decarboxylation activity of POR was assayed at ... atmosphere The reduction of metronidazole was calculated using an extinction coefficient of 9300 m)1Æcm)1 One unit of enzyme activity was defined as the reduction of lmolÆmin)1 of metronidazole (corresponding...

Ngày tải lên: 16/02/2014, 09:20

... effects of one of the substrates, i.e pantoate [8,9] One of the interesting features of the plant PSs is the presence of a conserved 24 residue insertion in the sequence [9] This sequence of amino ... we report the results of the structural studies of the pantoate-bound form of the N-terminal domain of E coli PS (nPS) The structure and substrate-binding interactions of E coli nPS have been ... The overlay of selected regions of H–15N correlation spectra, highlighting cumulative changes in chemical shifts of specific residues of nPS as a function of substrate(s) The resonances of free nPS...

Ngày tải lên: 16/02/2014, 09:20

... H and Mizumoto, Y (2006) Estimation of Intake Level of Di (2-ethylhecyl) phthalate (DEHP) of Japanese pregnant woman based on measurement of concentrations of three urinary metabolites Jpn J Hyg., ... concentration of some organic compounds is regulated The WHO has proposed guideline value of organic compounds,67) as has The Ministry of Health, Labor and Welfare in Japan.68) The effect of volatile ... systematic review of provocation studies, J Allergy Clin Immunol., 118, 1257–1264 Hojo, S., Sakabe, K., Ishikawa, S., Miyata, M and Kumano, H (2009) Evaluation of subjective symptoms of Japanese patients...

Ngày tải lên: 17/02/2014, 22:20

... cleavage of procaspase-8 and procaspase-10, and subsequent downstream activation of the extrinsic and intrinsic pathways of apoptosis [4] Despite the considerable interest raised by the potential of ... induce expression of DR5 in glioma cells To elucidate the underlying molecular mechanisms of the observed synergistic effects of PIs, we focused on the transcriptional activation of pro-apoptotic ... functioning of the ubiquitin–proteasome pathway is essential for the degradation of the majority of intracellular proteins and is implicated in many cellular processes, including regulation of apoptosis...

Ngày tải lên: 18/02/2014, 17:20

... deuteration of C2¢ of the epimerase product The lack of deuteration of the C2¢ of DHMP is not due to the lack of deuterons, because it has been shown previously that the 6-hydroxymethyl group of the ... is presumably related to the sizes of the Fig Stopped-flow analysis of the binding of HPO to SaDHNA The concentration of SaDHNA was lM, and the concentrations of HPO were 10, 20, 30, and 40 lM ... association rate constant of HPO (0.55 lm)1Æs)1) was very similar to that of HP (0.65 lm)1Æs)1), but the dissociation rate constant of HPO (0.062 s)1) was about a quarter of that of HP (0.26 s)1), suggesting...

Ngày tải lên: 19/02/2014, 00:20

... levels of phosphorylation expressed in relation to percentage dThd phosphorylation of the wild-type Relative phosphorylation expressed as a relation of the percentage of dThd phosphorylation of the ... phosphorylation of dGuo was reduced markedly Structure of Dm-dNK-E52D in complex with dTTP The structure of one of the mutants, E52D, was solved ˚ using X-ray crystallography at a resolution of 2.5 A ... illustrating the binding of the feedback inhibitor dTTP and the position of Mg2+ in the active site Mg ion that coordinates the phosphates of dTTP (Fig 3) Discussion Mutation of residues in the active...

Ngày tải lên: 19/02/2014, 02:20

... enzyme must sacrifice some of its stability It has previously been suggested that the lower thermal stability of cold-adapted enzymes is simply a consequence of the lack of selective pressure for ... function of the nuclease NucM of Erwinia chrysanthemi FEMS Microbiol Lett 112, 99–103 18 Moulard M, Condemine G & Robert-Baudouy J (1993) Characterization of the nucM gene coding for a nuclease of ... shows that the rate of irreversible unfolding for VsEndA is higher than for VcEndA, with a half-life of % 13 and 33 min, respectively Substrate specificity analysis An analysis of the substrate specificity...

Ngày tải lên: 19/02/2014, 05:20