Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 20 of 53 for “"ENZYME INHIBITION"”.
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Investigating domain-selective angiotensin converting enzyme inhibition and oxidative inactivation
Angiotensin converting enzyme (ACE) is a zinc metalloprotease comprised of two highly homologous, catalytically active domains (90% active site identity and 60% sequence similarity). The C-domain is responsible for blood pressure regulation via angiotensin I cleavage while the N-domain inactivates …
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Anti-Diabetic and Anti-Obesity Activities of Cocoa (Theobroma cacao) via Physiological Enzyme Inhibition
… and anti-obesity bioactivities, such as inhibition of certain enzymes in the body. Polyphenol profiles, protein-binding abilities, presence of compounds termed oxidative polymers, and abilities to inhibit α-glucosidase, pancreatic α-amylase, lipase, and dipeptidyl peptidase-IV (DPP4) in …
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In vitro evaluation of the enzyme inhibition and membrane permeation properties of benzophenones extracted from honeybush
… fat uptake can be controlled by honeybush tea is enzyme inhibition in the gastrointestinal tract. The aim of this study was to determine the enzyme inhibition (i.e. lipase and α-glucosidase) effect of crude honeybush extracts, benzophenone rich fractions and xanthone rich fractions from Cyclopia …
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The study and optimization of the Enzyme Inhibition Bioassay 96 for the detection of organophosphate and carbamate compounds
… of pollutants present in the environment. The Enzyme Inhibition Bioassay 96 (EIB 96) is one such field-screening tool; The EIB 96 is an assay that can detect the presence of organophosphate and carbamate compounds, providing scientists with valuable information to focus their future sampling …
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Characterization of Leucyl -Trna Synthetase From Saccharomyces Cerevisiae and Escherichia Coli in Aminoacylation, Amino Acid Editing and Enzyme Inhibition
… drugs. Leucyl-adenylate analogs were tested for inhibition activity against LeuRS from different sources. These analogs efficiently inhibited the E. coli and Saccharomyces cerevisiae mitochondrial LeuRS enzymes with low nanomolar K I's, but had no inhibitory effects on the eukaryotic S. …
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Effect of Selective and Nonselective Cyclooxygenase Enzyme Inhibition on Arterial Blood Pressure and Cerebral Blood Flow with Exposure to Intermittent Hypoxia in Humans
Background: Intermittent hypoxia (IH) simulating obstructive sleep apnea raises blood pressure (BP) and impairs cerebral blood flow response. The pathophysiology of intermittent hypoxia-mediated increase in BP involves multiple mechanisms but the role of cyclooxygenase (COX) catalyzed vasoactive …
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Orally Induced Tolerance to Streptococcus Mutans and Glucosyltransferase in Neonatal Mice
… the antibody response to vaccine and BSA, and an enzyme inhibition assay was employed to measure GTase antibody titer. Daily feeding during the first eight days of life resulted in a lower antibody response to the antigens upon subsequent challenge.
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Fate and Effect of Peracetic Acid Solutions on Biological Wastewater Treatment Systems
… was dose-dependent, with significant inhibition at PAA 40 mg/L; fast recovery was observed after direct PAA solution addition ended. Microbial acclimation to PAA did not take place under aerobic conditions, but a low degree of acclimation was observed under anoxic conditions over a …
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The use of purified enzymes for the early assessment of toxicity
… in vitro tests, the potential of three purified enzymes: α-chymotrypsin, acid phosphatase, and carbonic anhydrase for use in the early assessment of toxicants at environmentally significant levels. Activities of α-chymotrypsin and acid phosphatase were measured spectrophotometrically, while …
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Biochemical Evaluation of Lignin-like Molecules
… unsulfated and size fractionated LMWLs. Detailed enzyme inhibition studies with sulfated and unsulfated LMWLs of ferulic and caffeic acid oligomers revealed that sulfation was not absolutely critical for dual inhibition property and smaller oligomers can yield a potent anticoagulant. …
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Kinetics of Acid Inactivation of Soybean Lipoxygenase and Its Effects on the Functional Properties of Soy Protein
… whole soybeans in water acidified with HCl. The enzyme was found to be completely and irreversibly inactivated at pH 3.0 and below. From a study of enzyme kinetics of lipoxygenase extracted from the acidified soy slurries, significant changes were observed with the values of the Michaelis …
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Evaluation of cocoa (Theobroma cacao) bean processing strategies to enhance alpha-glucosidase inhibitory activity of dietary cocoa
… CPEs dose-dependently inhibited α-glucosidase enzyme activity, with cool fermented/cool roasted cocoa powder exhibiting the best inhibition (IC50 of 62.2 µg/mL). Increasing flavanol mDP was correlated with decreasing IC50 values, suggesting that the complex flavanols produced during processing …
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Targeting isoprenoid biosynthesis for drug discovery
… and bisamine) that inhibit UPPS, an essential enzyme involved in cell wall biosynthesis. The inhibitors bind to one or more of the four inhibitor-binding sites with the most active leads binding to site-4, not the substrate-binding sites. The most potent leads are active against Staphylococcus …
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NMR, Crystallographic and Computational Investigations of Peptides, Proteins and Bisphosphonates: New Paradigms for Rational Drug Design
… (3) developing mathematical models based on enzyme-inhibition data and molecular descriptors to predict potency/activity of compounds in cell-based assays."
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Design, Synthesis, and Evaluation of Small Molecules in the Discovery of Novel Antimicrobial Agents
… head groups, were discovered demonstrating good enzyme inhibition and good antimicrobial activity against clinically relevant bacteria. Finally, Chapter 4 provides an overall discussion of the work detailed in this dissertation and future directions that will continue the advancement of these …
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Organismi acquatici e ambiente: meccanismi biochimici di interazione, risposta e adattamento
… responses to contaminants of membrane-bound enzyme activities involved in key biochemical mechanisms, namely cell ionic regulation and mitochondrial energy production. In vitro and in vitro approaches have been pursued. In vitro assays were carried out by adding the contaminants (NH4Cl and …
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Enzyme microspheres for biosensing and cell signaling perturbation
… To bypass these problems, we developed enzyme based sensor arrays that rapidly and simultaneously analyze multiple analytes in solutions without separation. In our approach, porous agarose beads, with enzymes for L-lactate immobilized on them, were localized to wells etched into a …
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Translational high-dimesional drug interaction discovery and validation using health record databases and pharmacokinetics models
… from publicly available in vitro selective CYP enzyme inhibition studies. The fm was then estimated from the curated data. Then, proposed a random control selection approach for nested case-control design for electronical health records (HER) and electronical medical records (EMR) databases. By …
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Controlling the Stability of Colloidal Drug Aggregates for Chemotherapeutic Delivery
… results in screening assays. In biochemical enzyme inhibition assays colloids non-specifically adsorb proteins leading to partial unfolding and enzyme inactivation. In cell-based cytotoxicity assays colloids are unable to cross cell membranes leading to the drug being unable to bind to its …
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Synthesis And Biological Evaluation Of Nitrile-Based Inhibitors Of Cysteine Proteases Caged With Ruthenium Complexes
… and stability data were studied. Cathepsin enzyme activity inhibition in 2D and 3D assays were established. This work showcased the applicability of ruthenium complexes in photocaging cathepsin inhibitors for gaining spatiotemporal control over enzyme inhibition. Later we reported that …
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