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 11 of 11 for “"peptide stapling"”.
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CYCLIZATION-BASED SITE-SELECTIVE N-TERMINAL CYSTEINE CONJUGATION, PEPTIDE STAPLING AND HISTONE DEACETYLASE (HDAC) PROBING
… modify N-terminal cysteines of unprotected peptides or proteins in a single step. We showed that α-fluoroketone molecules afford the cyclization reaction with the beta amino thiol group of N-terminal cysteine. Both chemo and stereo-selectivity of this reaction have been studied using 2D NMR …
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Azobenzenes for the development of therapeutics
… 1 explores 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 …
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Design and synthesis of molecular tools for the ubiquitin proteasome system
… α-helix 9 of E2-25K. Creating a short helical peptide analogous 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 …
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Strain-promoted Stapled Peptides for Inhibiting Protein-protein Interactions
… for 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 …
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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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Proteolysis targeting chimeras for the directed ubiquitination of the androgen receptor
… of prostate cancer. First, in this work stapled peptide PROTACs recruiting E3 ligase MDM2 for AR degradation were investigated. MDM2 has been underexploited as an E3 ligase for PROTACs, despite a beneficial ability to modulate the p53 protein, a vital tumour suppressor, in additional to inducing …
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TARGETING THE NRF2/KEAP1 INTERACTION
… This work describes a cell penetrating, TAT-Nrf2 peptide which targets the Nrf2/Keap1 interaction in vitro. Induction of downstream genes is both sequence and dose dependent. In an established model of bacterial sepsis, the peptide reduces pro-inflammatory mediators. Investigation of both cell …
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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
Peptides are useful modulators of protein-protein interactions (PPIs) and cellular membranes, both of which are traditionally challenging to target using small molecules. Often therapeutic peptides suffer from issues including poor proteolytic stability. Two-component peptide stapling can improve …
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Bioactive Peptides as Antibacterial Agents and Visual Transduction
Bioactive peptides (BPs) are specific protein fragments which positively impact bodily functions and primary health conditions. BPs are formed from amino acids linked by amide bonds and classified by their mode of action in health-related applications. The amino acid composition and their secondary …
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Approaches Towards the Inhibition of Anti-Apoptotic Proteins
… a combination of rational-based approach and peptide stapling, twenty-two conformationally-constrained peptides were generated to target the protein-protein interaction (PPI) of CK2 and affect its function. The lead peptide, P7-F1C5, presented a novel, highly-functionalised constraint that …
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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
Peptides are recognised for their ability to disrupt protein-protein interactions (PPIs), which have traditionally been considered ‘undruggable’ with small molecules. However, due to issues such as a susceptibility to degradation by proteases, the use of peptide therapeutics in the clinic has been …