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 25 for “"Stapling"”.
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Stapling and Unstapling Peptides and Proteins With S-Tetrazine
… to macrocyclic conformations (i.e. stapling). Importantly, the incorporated s-tetrazine chromophore will undergo photodisassociation upon absorp-tion of a photon permitting the release of the restricted conformations (i.e. unstapling). In chapter one, we aimed to study a fundamental …
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One-Carbon Bridge Stapling for use in Peptide-Drug Conjugates
One-Carbon Bridge Stapling for use in Peptide-Drug Conjugates Bethany M. Cooper Therapeutic peptides lie in between small molecules and therapeutic proteins in terms of their molecular weight and have many advantageous properties, such as high potency and selectivity. Yet one fundamental …
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Peptide/Protein Stapling and Unstapling: Introduction and Photorelease of Isobutylene Graft
… crosslinking, also termed “stapling”, is an important technology in the development of bioactive peptide-based therapeutics. Among all of the tools, S-alkylation is one of the most flexible approaches, as a wide range of bis-thiol-reactive linkers are commercially available. …
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A Survey of Stapling Methods to Increase the Affinity, Activity and Stability of Ghrelin Analogues
… activity. We present an analysis of different stapling methods at positions 12 and 16 of ghrelin(1-20) analogues with the goal of increasing proteolytic stability and to retain or improve affinity and activity towards GHSR. Ghrelin(1-20) analogues were modified with a wide range of chemical …
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CYCLIZATION-BASED SITE-SELECTIVE N-TERMINAL CYSTEINE CONJUGATION, PEPTIDE STAPLING AND HISTONE DEACETYLASE (HDAC) PROBING
… pathways. Taken together, our FTDR-based stapling approach may provide a novel class of cell-permeable peptides that might open a new window to probe intracellular targets. This dissertation reports another cyclization reaction between hydrazine and carbamate, synthesized from 7-hdyroxy …
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Interrogation and engineering of RAD51:BRC repeat interactions
… inhibitors of RAD51. A method for cysteine stapling of recombinantly produced peptides was optimised to yield the correct product of high purity. The optimised stapling methodology provides a promising general approach for recombinant production and evaluation of cysteine-stapled peptides. …
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Azobenzenes for the development of therapeutics
… the utilisation of azobenzenes for peptide stapling, that has gained notable interest for therapeutic applications. However, many reported methodologies rely on the use of tissue-damaging UV light. Recent approaches that minimise the dependence on UV light have been successful at adjusting …
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Strain-promoted Stapled Peptides for Inhibiting Protein-protein Interactions
… targeting PPIs. One such methodology is peptide stapling, which involves constraining a short peptide into its native alpha-helical form by forming a covalent link between two of its amino acid side-chains. The Sondheimer dialkyne reagent has previously been used in strain-promoted double-click …
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DEVELOPMENT OF MOLECULAR PROBES ACTING ON aSYN/TUBULIN AND TAU/TUBULIN INTERACTION
… disordered protein, and in our case stapling strategies were completely successful. We, therefore, explored a less common stapling approach, by also designing a novel linker to afford the stapling. Unfortunately, our linker was not stable in standard SPPS conditions. Finally, Two …
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Design and synthesis of molecular tools for the ubiquitin proteasome system
… to α-9 of E2-25K with the technique of peptide stapling could potentially block the action of Ubb+1 and provide a tool to investigate the role of the UPS in AD.Following synthesis of the requisite alkenyl amino acids for peptide stapling, an initial palette of nine peptides, containing the …
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Property determinants of dextran:polyethylene glycol adhesive sealants
… use of closure techniques, such as suturing or stapling of disjoined tissues. Risk factors associated with these techniques are largely attributed to the discrete nature of the mechanical forces arising in the tissues. Adhesive sealants can mitigate risk by imparting a continuous stress …
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The development of stapled peptides as chemical tools to investigate activin A signalling and as antibacterial agents targeting MsbA-mediated efflux
… in the clinic has been limited. Peptide stapling, whereby a peptide is constrained into its binding conformation, presents a means by which some of the weaknesses of peptide therapeutics may be overcome. This thesis describes two projects in which stapled peptides were developed to …
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The introduction of a new manufacturing facility for plastic injection moulding at Acco-Rexel Ltd', Llangeinor, South Wales
… to manufacture components for its high volume stapling machine products. Injection moulding in itself is not new, but modern manufacturing methods such as Just-In-Time(small batch manufacturing) are still being developed for new & existing processes. The need to improve processes within a …
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Virginia Woolf: The Bookbinder and the Bibliophile
… to have engaged herself for many hours folding, stapling, sewing and gluing the publications which she and her husband Leonard had tried printing (at least to start) with the small platen press they had set up in their home. What is even less acknowledged is that Virginia Woolf maintained a …
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Hand-assisted laparoscopic ovariohysterectomy in the mare
… achieved using a combination of a laparoscopic stapling instrument, an ultrasonically activated instrument and endoscopic clips. The genital tract was exteriorized through the laparotomy, and the body of the uterus transected and sutured in conventional pattern. Horses were evaluated through …
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The effect of handle characteristics of a hammer stapler on biomechanical and physiological response
… inclines. Each experimental trial consisted of stapling roofing underlayment onto the simulated roof at a frequency of 1 staple per second for a two-minute duration. At a significance level of 5%, Tool #3 produced lower discomfort ratings in fingers and hand and higher favorable ratings for …
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Proteolysis targeting chimeras for the directed ubiquitination of the androgen receptor
… degradation. Using a two-component peptide stapling strategy, stapled peptide PROTACs were developed for AR degradation via recruitment of MDM2. Stapled peptides are commonly used to target challenging protein-protein interactions, such as MDM2-p53. Peptides are capable of emulating elements …
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TARGETING THE NRF2/KEAP1 INTERACTION
… both head-to-tail cyclisation and peptide stapling were examined in order to restore potency in cell based assays. Finally, an alternative method for identification of Nrf2/Keap1 disruptors was explored. In silico docking calculations were used to identify potential novel PPI disruptors …
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The development of functionalised stapled peptides as chemical tools to modulate biological processes in platelets and as novel antimicrobial therapeutics targeting Pseudomonas aeruginosa
… proteolytic stability. Two-component peptide stapling can improve stability and enable facile peptide functionalisation. This thesis describes the development of functionalised stapled peptides for two biological applications. 1. The development of stapled peptides as chemical tools to …
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Determining ideal staple size for small intestinal surgery in cats
Background: The use of stapling equipment for intestinal surgery in cats is rarely reported, and appropriate staple sizes for cat intestine are unknown. Objective: To determine staple cartridge sizes for thoracoabdominal (TA) and endoscopic gastrointestinal anastomosis (EndoGIA) that will …
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