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 13 of 13 for “"protease inhibition"”.
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Biological activity of Sinularia notanda
… The crude extract was also tested for HIV-1 protease inhibition using a direct enzyme assay, and antioxidant activity determined using 1,1-diphenyl-2picrylhydrazyl (DPPH). Bioassay guided fractionation, column chromatography and thin layer chromatography were used to identify active fractions …
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Thioamides And Proteolysis: Examining The Effects And Applications Of A Single-Atom Substitution
… applications in studying proteolysis, monitoring protease activity and in selective protease inhibition. To date, we have used model substrates to investigate the positional effects that these thioamide substitutions have on proteolysis rates, as well to examnine the ability of thioamides to …
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Insights Into the Dynamic Structure and Inhibitory Mechanism of Plasminogen Activator Inhibitor Type 1
… reducing the rate of full loop insertion during protease inhibition. We provide evidence strongly suggesting that these hindrances to RCL flexibility and mobility affect the mechanism by which PAI-1 inactivates t-PA at several steps, perturbing the initial non-covalent binding, slowing the …
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Bioactivity evaluation and structural modification of Bowman-Birk type protease inhibitory peptides from amphibian skin secretions
… analogue, QUB-1879 showed better bioactivity on protease inhibition and anti-proliferation. In addition, negligible LDH releasing was observed when treated by QUB-1879. In Chapter 5, the trypsin inhibitory loop was linked to Tat49-57 to improve the biological activities and bioavailability. …
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Investigating the role of rhomboid proteases in the development of Dictyostelium discoideum
… previously by collaborators for serine protease inhibition and urokinase-type plasminogen activator (uPA) inhibition, both in vitro and in vivo. In those biochemical assays, three compounds, BC11, SR3 and BC57 displayed micromolar inhibition of uPA with an excellent selectivity profile …
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Migration of tumor cells and leukocytes in extracellular matrix : proteolytic and nonproteolytic strategies for overcoming tissue barriers
… computer-assisted cell tracking. Expression of proteases, including several MMPs, ADAMs, serine proteases and cathepsins, was shown by flow cytometry, Western blot, zymography, and RT-PCR. Protease activity by migrating HT-1080 fibrosarcoma cells resulting in collagenolysis in situ and …
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Identification and rational design of Bowman-Birk type protease inhibitory peptides derived from Ranidae frogs
… analogue QUB1820 also promoted chymotrypsin inhibition more than the parent. In chapter 4, QUB1906 and designed analogue, QUB1853, displayed trypsin inhibitory activity and antimicrobial activity. Meanwhile, QUB1873, the designed chymotrypsin inhibitor with anti-proliferative effect on a …
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Improving the skin barrier function in atopic dermatitis
… Our study also found disproportionately raised protease inhibitory activities amongst the AD participants. This inappropriately raised protease inhibition may interfere with profilaggrin proteolysis, leading to the development of AD in some wild-type patients. Having demonstrated that deficiency …
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Characterization of Pleiotropic Activities of alpha1-Antitrypsin
… emphysema, includes the excess of uninhibited proteases released from inflammatory cells. alpha1-antitrypsin (AAT), an acute phase protein, is the prototypic member of the serpin super family and a major inhibitor of serine proteases such as neutrophil elastase. The clinical importance of AAT …
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Systematic Survey of the Plasmodium falciparum Hemoglobin Catabolic Pathway in Intact Cells Using the Digestomics Approach
… including aspartic, cysteine, metalloproteases and aminopeptidases. Importantly, this model is largely based on in vitro experiments using purified Plasmodium and recombinant proteases, and the molecular underpinnings of this catabolic process in intact cells remain poorly understood. …
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Cathepsin S as a mediator of acute lung inflammation
… outcomes.<br/><br/>Proteolytic enzymes, or proteases, are known to play important roles in the maintenance of pulmonary homeostasis. However, during disease, proteolytic activity can become dysregulated and cause damage to the lung, contributing to the pathology of conditions like cystic …
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Probing the chemical biology involved in the haem detoxification pathway of the human malaria parasite, plasmodium falciparum
… (2) uptake of RBC cytosol into the DV, (3) protease enzyme concentration within the DV, (4) basal levels of haemoglobin, haem and haemozoin and (5) the cellular effects of perturbing the pathway with inhibitors. As such, this thesis addresses the gap in the required experimental data …
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Methodologies For Attaching Polypyridyl Ligands Into Amino Acids And Synthesis And Biological Evaluation Of Novel Light Activated Peptidomimetic Cysteine Protease Inhibitors Caged By Ruii(bpy)2
… the synthesis of the first caged cysteine protease inhibitor. After an introductory survey of different Ru and Pt complexes used as potential therapeutic cancer agents, cysteine protease inhibitors are described. The syntheses of RuII(bpy)2 complexes caging cathepsin inhibitors are revealed …