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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 41 for “"Cyclic Peptide"”.
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Genetic selection of cyclic peptide G-quadruplex ligands
… This thesis commences the exploration of cyclic peptides as alternative chemical scaffolds for de novo G4 ligand generation. Widely used to generate protein binders as drug leads but relatively under-explored for nucleic acid targeting, cyclic peptides lie in the chemical space between …
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Biochemical Characterization of the DUF3328 Protein in the Biosynthesis of Cyclic Peptide Cyclochlorotine
Cyclic peptide natural products are valuable sources for medicine. They exhibit significant biological and chemical diversity. Cyclochlorotine, a fungal cyclic pentapeptide produced by Talaromyces islandicus, possesses unique structural modifications, including dichlorination and hydroxylation, yet …
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Modulation of Antibacterial Activity and Cytotoxicity in Amphipathic Cyclic Peptide [R4W4] Using Histidine Substitution
… an alternative approach utilizing antimicrobial peptides (AMPs) as a means to end this cycle. [R4W4] is among known AMPs that demonstrated antimicrobial activity against methicillin-resistant staphylococcus aureus (MRSA) with a minimum inhibitory concentration (MIC) of 2.67 μg/mL. This peptide …
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Mechanistic Study of Antimicrobial Cyclic Peptide [R4W4] Antibacterial Effectiveness against Methicillin-resistant Staphylococcus aureus (MRSA)
<p>Antimicrobial peptides (AMPs) are being explored as a potential solution to combat antibiotic resistance, as they have shown promise in reducing susceptibility to antibiotics. This study explores if [R<sub>4</sub>W<sub>4</sub>] peptide is bacteriostatic or bactericidal using modified two-fold …
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Design and Evaluation of Cyclic Peptide-Epirubicin Conjugate for Enhanced Anticancer Activity and Reduced Myocardial Toxicity
… and development of resistance, with cyclic peptides containing tryptophan (W) and arginine (R) residues showed comparable or higher activity against cancer cells and reduced the toxicity<strong> </strong>to heart cells when compared to free DOX. [(WR)<sub>4</sub>WK]bA-DOX conjugate …
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Synthesis of composite hydrogels incorporating D,L-cyclic peptide nanotubes as a platform for materials engineering
… (GelMA) hydrogels that incorporate D,L-cyclic peptide nanotubes. These nanotubes are biocompatible, stiff and their physical and chemical properties can be tailored simply by changing the amino acid sequence of the peptide. We show that the nanotubes successfully integrated into the …
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Development of Natural Cyclic Peptide Inhibitors of XRCC4/XLF Interaction for Radio-Sensitization of Breast Tumor Cells
… Therefore, it is proposed that small natural cyclic peptides that bind to the XLF interface of XRCC4 near M61 and F106 can be identified through an mRNA display in vitro selection, and these peptides will inhibit NHEJ and thereby radiosensitize breast tumor cells. We have synthesized five DNA …
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Development of Novel Peptide-Doxorubicin Conjugates for Targeting Triple-Negative Breast Cancer
… the cancer cells, I have synthesized three peptide-drug conjugates (PDCs) to specifically target the TNBC cells. The first PDC contains peptide 18-4 with an additional cysteine in the N-terminal (NH2- CWxEAAYQrFL-CONH2) linked to aldoxorubicin (Aldox), a modified version of a common …
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Computational design of functional cyclic peptides using deep learning
Cyclic peptides have gained significant traction as a therapeutic modality. Given their ease of synthesis, expansive chemical space, and the promising pharmacokinetic properties of existing cyclic peptide drugs, cyclic peptides have been proposed as a mid-point between biologics and small …
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De novo design of passively permeable cyclic peptides and incorporation of noncanonical amino acids to improve predicted binding affinity
Cyclic peptides fill an intermediate niche between traditional small molecule therapeutics and larger biologics. In ideal cases they combine the passive permeability and oral availability of small molecules with the binding specificity of larger biologics. However, achieving both of these features …
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Synthesis and Study of Biomimetic Ion Channels: (1) Toward the Development of a Cyclic Peptide-Based Redox-Gated Channel, and (2) Investigations Into the Effect of Pore Size on the Ion Selectivity of an Aminocyclodextrin Channel
To probe the correlation between pore size and ion selectivity, a channel with an alpha-cyclodextrin macrocycle was synthesized and its transport properties were compared with those of an analogous channel with a larger beta-cyclodextrin pore. The anion transport profile of the alpha-cyclodextrin …
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Myoglobin Microsperes and Metalloporphyrin -Peptide Complexes
… and characterized a new class of heme-peptide complexes using disulfide-linked tweezers and cyclic peptides. The binding affinities, helicities, and mechanism of binding of linear, tweezers, and cyclic peptides to [Fe III(coproporphyrin-I)]+ have been determined. We have incorporated …
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The design and synthesis of fluorescent peptides and disaccharides for tumour imaging.
Chapter 1: Peptide targeting of integrin αvβ3 Integrins are cellular surface receptor proteins involved in numerous cellular signalling and adhesion processes. The integrin αvβ3 subtype is up-regulated around sites of malignancy especially solid tumour masses. This is due to its expression on the …
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Supramolecular Functional Materials Based on Cucurbit[8]uril-Enhanced π–π Interactions
… the cucurbit[n]uril (CB[n]) family of macrocyclic hosts has attracted considerable attention over the last decade. Advantages of CB[n]-based systems include compatibility with a wide guest scope of molecules, a high binding affinity that spans a wide range (10³ – 10¹⁵ M⁻¹), proven …
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Liposome drug delivery systems for anticancer agents
… formulation of an amphiphilic anticancer peptide using the ANTS/DPX leakage assay. The effects of lipid composition on the liposomes' resistance to an amphiphilic cyclic peptide c[KS.S.S.KWL W] were studied by the ANTS/DPX leakage assay. One or more unsaturated acyl chains in the …
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Amphiphilic Cyclic Cell-Penetrating Peptides Containing Tryptophan and Arginine as Anticancer Agents and Drug Delivery System
<p>Amphiphilic cyclic cell-penetrating peptides composed of an increasing number of alternative tryptophan (W) and arginine (R) were synthesized and evaluated as a molecular transporter and for their ability to deliver doxorubicin (Dox) and large molecular weight molecules, such as siRNA and …
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Design and Synthesis of Hyaluronan:RHAMM Interaction Inhibitors
… for treating cancer but truncation of RHAMM into peptides mimicking only the HA binding domains is predicted to lose their natural α-helical structure. The goal of this project is to explore the effects cyclizing each binding domain has on helicity and its biological effect. Eighteen peptides were …
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Chemoenzymatic synthesis of an analogue of the potent antifungal mycosubtilin
… activity. Structurally, mycosubtilin is a macrocycliclipoheptapeptide of sequence Asn-Tyr-Asn-Gln-Pro-Ser-Asn, with the N-terminal Asn joined by a β-amino fatty acid. Besides the antifungal and antibiotic activities,these molecules are also hemolytic in nature. Hence, the purpose of this study …
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Damaged Collagen Detection and A Novel Approach to 1,3-Dipolar Cycloaddition Reactivity: Research at the Interface of Chemistry and Biology
Part I Chapter 1. Collagen Mimetic Peptides as a Selective Binder for Damaged Collagen. “Collagen diseases” were first introduced by Klemperer and coworkers in the 1950s. This type of disease can cause fibrinoid degeneration or changes in the collagen fibers that denature the collagen triple helix. …
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Amphiphilic Cell-Penetrating Hybrid Cyclic-Linear Peptides as a Drug Delivery System
<p>A number of cyclic peptides containing a positively charged ring composed of arginine residues attached to hydrophobic tail made of tryptophan residues through a lysine linker namely [R<sub>5</sub>K]W<sub>5</sub>, [R<sub>6</sub>K]W<sub>5</sub>, [R<sub>5</sub>K]W<sub>6</sub>, …
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