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Plasmodium falciparum alanine M1-aminopeptidase (PfA-M1) is a validated target for anti-malarial drug development. Presence of
significant similarity between PfA-M1 and human M1-aminopeptidases, particularly within regions of enzyme active site leads to
problem of non-specificity and off-target binding for known aminopeptidase inhibitors. Molecular docking based in silico screening
approach for off-target binding has high potential but requires 3D-structure of all human M1-aminopeptidaes. Therefore, in the
present study 3D structural models of seven human M1-aminopeptidases were developed. The robustness of docking parameters
and quality of predicted human M1-aminopeptidases structural models was evaluated by stereochemical analysis and docking of
their respective known inhibitors. The docking scores were in agreement with the inhibitory concentrations elucidated in enzyme
assays of respective inhibitor enzyme combinations (r2≈0.70). Further docking analysis of fifteen potential PfA-M1 inhibitors
(virtual screening identified) showed that three compounds had less docking affinity for human M1-aminopeptidases as compared
to PfA-M1. These three identified potential lead compounds can be validated with enzyme assays and used as a scaffold for
designing of new compounds with increased specificity towards PfA-M1. 相似文献
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Plasmonics - In this paper, a detailed numerical investigation has been carried out to find the effect of stress on the optical performances of hybrid plasmonic waveguides (HPWs) operating at 1550... 相似文献
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Plasmonics - In this paper, design and performance estimation of a hybrid plasmonic-based optical filter operating at 1550 nm in the presence of stress is presented. The proposed integrated Bragg... 相似文献
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Sneha Vangaveti Prasenjit Das Vijay L. Kumar 《Journal of biochemical and molecular toxicology》2021,35(1)
The use of cyclosporine A (CsA) as an immunosuppressive agent is often limited owing to its hepatotoxic and nephrotoxic properties. The present study was designed to evaluate the protective effect of metformin and silymarin in a rat model of CsA induced hepatorenal toxicity. The study included seven groups of Wistar albino rats (n = 6 per group): normal control, experimental control (CsA alone, 25 mg/kg), CsA + metformin (50 and 500 mg/kg), CsA + silymarin (50 and 200 mg/kg) and CsA + vitamin E (100 mg/kg). All the drugs were given daily for a period of 21 days by oral gavage and their effect was evaluated on serum levels of organ function markers (serum glutamate pyruvate transaminase, serum glutamate oxaloacetate transaminase, bilirubin, urea/blood urea nitrogen, creatinine), markers of oxidative stress (thiobarbituric acid reactive substances, glutathione, superoxide dismutase), inflammation (nitrite, myeloperoxidase, tumour necrosis factor‐alpha, prostaglandin E2), apoptosis (terminal deoxynucleotidyl transferase dUTP nick end labelling positivity) in addition to tissue histology, cyclooxygenase (COX)‐2 and inducible nitric oxide synthase (iNOS) immunoreactivity. Administration of metformin and silymarin along with CsA ameliorated functional damage to liver and kidneys in a dose‐dependent manner. Significant and comparable improvement in the tissue levels of oxidative stress, inflammation, apoptotic markers was also observed following treatment with both the test drugs. Normalization of histology scores, as well as COX‐2 and iNOS immunoreactivity scores, further strengthened these findings. The hepatoprotective and nephroprotective effects of metformin and silymarin were comparable and matched with that of reference drug, vitamin E. The findings of the present study suggest that both metformin and silymarin have a potential for clinical use in patients receiving long‐term CsA treatment to maintain their liver and kidney functions. 相似文献
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Maisam Makarem Nagarajan Kannan Long V. Nguyen David J. H. F. Knapp Sneha Balani Michael D. Prater John Stingl Afshin Raouf Oksana Nemirovsky Peter Eirew Connie J. Eaves 《PLoS biology》2013,11(8)
Many normal adult tissues contain rare stem cells with extensive self-maintaining regenerative potential. During development, the stem cells of the hematopoietic and neural systems undergo intrinsically specified changes in their self-renewal potential. In the mouse, mammary stem cells with transplantable regenerative activity are first detectable a few days before birth. They share some phenotypic properties with their adult counterparts but are enriched in a subpopulation that displays a distinct gene expression profile. Here we show that fetal mammary epithelial cells have a greater direct and inducible growth potential than their adult counterparts. The latter feature is revealed in a novel culture system that enables large numbers of in vitro clonogenic progenitors as well as mammary stem cells with serially transplantable activity to be produced within 7 days from single fetal or adult input cells. We further show that these responses are highly dependent on novel factors produced by fibroblasts. These findings provide new avenues for elucidating mechanisms that regulate normal mammary epithelial stem cell properties at the single-cell level, how these change during development, and how their perturbation may contribute to transformation. 相似文献
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Sachin Honnenahalli Rajegowda Sneha Rani Athahalli Honnagirigowda 《Cell biochemistry and function》2023,41(1):33-44
Cassia siamea is a nonedible legume belonging to Fabaceae. The seed of C. siamea contains ~16% of protein. The study reports the biochemical characterization of purified novel serine protease inhibitor from seeds of C. siamea, aimed with assessing the anti-inflammatory activity. The seed extract was subjected to ammonium sulfate precipitation followed by fast protein liquid chromatography (FPLC)-anion exchange chromatography and affinity-chromatography to obtain a relative pure protease inhibitor. Thirty-fivefold purification with the specific activity of 250 U/mg of trypsin inhibitory unit was obtained. The characterization of protease inhibitor for optimum temperature, pH, and metal ions were measured using N-α-benzoyl-DL-arginine-p-nitroanilide (BAPNA) assay and casein zymogram. The C. siamea trypsin inhibitor (CsTI) has a relative molecular mass of 25.540 kDa. Purified CsTI and Dolichos biflorus were tested for anti-inflammatory efficacy against A549 and RAW264.7 cell lines. The inhibitory activity of both purified inhibitors are comparable and are potent toward anti-inflammatory activity. The purified inhibitor shows to be a promising candidate as anti-inflammatory agent by targeting the serine proteases. 相似文献