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.
Results
Showing 1 to 20 of 33 for “"High potency"”.
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Institutions and Drug Markets
… which are capable of yielding continuous, high-potency crops. Methamphetamine producers also adopt small-scale, decentralized strategies, but commodity control increases their exposure and leads to greater overall transaction costs during the manufacturing process.
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Using Chemically Modified Oligonucleotides to Modulate Gene Expression, Treat Genetic Diseases, and Probe Novel Mechanisms of RNA Interference
… To combine the simplicity of ASO and high selectivity of dsRNA, we tested chemically modified, single-stranded small-interfering RNA (ss-siRNA) of sequences targeting CAG repeats in collaboration with ISIS Pharmaceutical, and showed them to have high potency (IC50 ~2 nM) and …
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Aglycon Modifications of Ipomoeassin F: Synthetic Route Development and Analog Synthesis to Enable Further SAR Studies
… of resin glycosides were discovered to have a high potency against numerous cancer cell line, with ipomoeassin F being the most potent among the family of natural products. Interestingly, one of the few differences between ipomoeassin F and the other compounds is the length of the fatty-acid …
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Synthesis of Saponin Immunoadjuvants
… of, and access to, novel adjuvants with high potency and attenuated toxicity. The QS-21 fraction of Quillaja saponaria extracts comprises an isomeric mixture of complex triterpene saponins and is currently the most promising immunopotentiator in several antitumor and infectious disease …
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Synthesis and SAR study of Meperidine Analogues as Selective Serotonin Reuptake Inhibitors (SSRIs)
… and 3,4-dichloro benzyl analogues and exhibited high potency for serotonin transporters and high selectivity over the dopamine transporter (DAT) and the norepinephrine transporter (NET). Also the N-demethylated analogues improve the binding affinity and selectivity for serotonin transporter. The …
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The Discovery and Development of Thienopyrimidines as Inhibitors of Helicobacter pylori
… for the treatment of H. pylori infections, a high-throughput screen was performed to identify selective compounds against H. pylori. This screen revealed two selective and structurally related thienopyrimidines. Structure-activity relationship of the thienopyrimidines against H. pylori was …
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Biochemical characterization of enzymes involved in the biosynthesis of the thiopeptide thiomuracin
… have outstanding biological profile, including high potency against a variety of antibiotic resistant pathogenic strains. Their new modes of action have attracted many efforts to develop chemical syntheses, and to study their biological function and biosynthetic origin. However, the complex …
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Identifying and Inhibiting Cholesterol-Protein Interactions for Therapeutic Development
… target diseased cells with abnormally high levels of inner plasma membrane cholesterol, allowing for high potency and safety in in vitro and in vivo drug testing. As a whole, this dissertation aims to demonstrate that cholesterol-protein interaction inhibitors represent a viable new …
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Water-Soluble Deep-Cavity Cavitands: Synthesis, Molecular Recognition, and Interactions with Phospholipid Membranes
… anions inside the hydrophobic pocket with much higher association constants. Moreover, external binding of several anions to the cavitand pendant feet was observed.</p> <p>Looking towards biological applications, we desired to learn how these molecules interact with phospholipid membranes. Six …
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Opioid Prescribing Among Hospitalized Patients in Tertiary Care Hospitals: A Retrospective Cohort Study
… if hospital prescribers are contributing to this high prescription rate. The purpose of this project was to describe opioid prescribing in two tertiary care hospitals in Canada. Methods This retrospective cohort study linked data from electronic discharge abstracts and inpatient prescription …
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Cannabinoids and Psychosis – Cause and Treatment
… suggested that the absence of CBD in modern, 'high-potency' forms of cannabis (sinsemilla or 'skunk') underlies the risk of such preparations for mental health. However, the evidence for this is sparse. <em>Characterising the effect of CBD on THC-elicited responses was the second major theme in …
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Synthesis of FtsZ inhibitors : potential antibiotic agents
… The cell division protein FtsZ, which is a highly conserved, essential and druggable protein, could be utilised as a target in this fight against antibiotic resistance. This thesis aimed to develop a set of novel antibacterial compounds that inhibit the function of FtsZ. The previous …
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Development of Novel Nicotinic Receptor Mediated Therapeutic Agents: Synthesis and Biological Evaluation of Novel Epibatidine Analogs and the First Total Synthesis of Anabasamine and Related Analogs
… nicotinic acetylcholine receptor ligands with high potency and selectivity. In addition, a series of rigid acetylcholine analogs were synthesized from cocaine to study the conformation of acetylcholine, the endogenous neurotransmitter at the nicotinic acetylcholine receptor. A stereoselective …
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Design and development of novel antagonists targeting Cdc20, a central regulator of the Anaphase-Promoting Complex/Cyclosome, for the treatment of cancer
… the advancement of lead compounds that exhibit high potency in halting cell proliferation in Triple Negative Breast Cancer (TNBC) cells at low concentrations. Subsequently, one lead compound was selected for preclinical development studies involving deeper functional assays analysis and …
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Tamoxifen metabolites can target both aromatase and estrogen receptors
… 70 nM and 20 nM, respectively. Nor and Hdn have high binding affinity for ER-α and ER-β, with EC50 values less than 35 nM. Nor and Hdn can inhibit breast cancer cell proliferation with high potency, with IG50s of 25 nM and 9 nM, respectively. Nor and Hdn can suppress progesterone receptor (PGR) …
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Enhanced heterogeneous nucleation on oxides in Al alloys by intensive melt shearing
… refined as-cast microstructure is generally highly desirable for either subsequent processing ability or mechanical properties of the finished components. In this thesis, the grain refined microstructures in Al alloys have been achieved by intensive melt shearing using the melt conditioning …
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Sites of interaction between calcitonin-family peptides and their receptors
… of RAMP3 has been demonstrated to be crucial for high affinity binding and high potency response of AM at the AM₂ receptor. In addition, a naturally occurring variant of the human CTR lacking the N-terminal 47 amino acids has been characterised in this thesis. For the first time, it has been shown …
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Interrogation and engineering of RAD51:BRC repeat interactions
… biophysical methods, I investigated a novel, high-affinity chimeric repeat BRC8-2 composed of FxxA and LFDE modules from different natural repeats. I determined the X-ray crystallographic structure of its complex, which allowed me to uncover the determinants of high affinity binding. I applied …
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One-Carbon Bridge Stapling for use in Peptide-Drug Conjugates
… and have many advantageous properties, such as high potency and selectivity. Yet one fundamental shortcoming of therapeutic peptides is their poor stability. Two-component peptide stapling (2C-PS) is an incredibly valuable tool used to increase a peptide’s stability and provide a point for …
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