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 44 for “"cyclic peptides"”.
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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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Chemical and chemoenzymatic syntheses of lantibiotics and other bioactive cyclic peptides
… emerging family of natural products, the lanthipeptides, is defined by the presence of the thioether-containing crosslinks lanthionine and methyllanthionine and includes many members with promising activities against clinically-relevant bacterial pathogens, including drug-resistant strains. …
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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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Tandem mass spectrometry approaches to characterizing challenging biomolecules : stapled and cyclic peptides and variants of lipid A from gram-negative bacteria
… and other complex biomolecules. Specifically, cyclic and stapled peptides have become an intriguing class of biomolecules in drug research afforded to them because of their biological stability and resistance to proteolytic digestions. However, challenges are presented in regards to the …
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Myoglobin Microsperes and Metalloporphyrin -Peptide Complexes
… 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 disulfide bridges between amphiphilic peptides to make …
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Design, synthesis, conformation and biological activities of cyclic alpha-melanotropin and related compounds.
… we were able to design a group of linear and cyclic peptides related to "4-10" fragment analogues of α -MSH. The solid phase synthesis of α -MSH and its related analogues using the p-methyl-benzhydrylamine resin was accomplished. The C-terminal carboxamide and N-terminal acetylamide were …
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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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Part I. The Acyl-Tunichlorins: A New Class of Nickel Chlorins Isolated From the Caribbean Tunicate Trididemnum Solidum. Part II. Cytotoxic Constituents of the Sponges Stylissa Carteri and Petrosia Sp. Part III. Electrospray Tandem Mass Spectrometry Studies
… methods in the structure elucidation of cyclic peptides and depsipeptides. Furthermore a new polyacetylene was identified in the marine sponge Petrosia sp.
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Cyclic and Linear Cell-Penetarating Peptides Composed of Tryptophan (WW) and Arginine (RR) Residues as Molecular Transporters
… of cell impermeable compounds, such as phosphopeptides and siRNA, across the cell membrane remains a challenge. Previous studies in Dr. Parang’s laboratory have shown that cyclic peptides composed of tryptophan (W) and arginine (R) amino acids [WR]<sub>5</sub> have higher cellular uptake than …
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Calpain inhibitor design inspired by the natural inhibitor calpastatin
… inhibitors. I have helped design cyclic peptides to mimic important conserved structural elements of calpastatin and have investigated their inhibition potency against calpain. Cyclic peptides and derivative peptidomimetics were able to inhibit cysteine proteases including calpain. …
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Delivery of sting agonist using lipid nanoparticles and discovery of anti-TIGIT peptides for cancer therapy
… research involves the discovery of anti-TIGIT cyclic peptides using phage biopanning to block the interaction between the receptor TIGIT and its high-affinity ligand, CD155. In clinical studies, inhibiting this pathway within the adaptive immune system has demonstrated the ability to reverse …
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CHARACTERIZATION OF BIOACTIVE PEPTIDES IDENTIFIED FROM GENETICALLY ENCODED LIBRARIES.
… insurgence. In this scenario, antimicrobial peptides (AMPs) can represent a solution as they show specificity, efficacy and rapid degradation, thus avoiding the long-term effects observed for chemical pesticides. During the last years, some AMPs have been successfully commercialized as plant …
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Cyclic and Linear Peptides Containing Tryptophan and Arginine Residues as Cell-Penetrating Peptides and Antifungal Agents
… we synthesized a novel group of linear and cyclic amphiphilic peptides containing different sequences of arginine (R) and tryptophan (W) residues. The peptides included a class of cyclic peptides, [R3W3]2, [R3WRW]2, [RWW]4, [WRR]4, [RWRW3]2, and the corresponding linear peptides, (R3WRW)2, …
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Zeolites to peptides: Statistical mechanics methods for structure solution and property evaluation
… study structure and properties of zeolites and peptides. A Monte Carlo method is applied to solve structure of a newly synthesized zeolite. Understanding the structure of a zeolite could lead to optimization of chemical processes it is involved in. Dielectric constant and elastic modulus are …
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Analyzing Functional Interactions of Designed Peptides by NMR Spectroscopy
… report the analysis of two groups of synthetic peptides designed for two applications – broad bactericidal action and inhibition of protein-protein interactions in human cells. Novel amphiphilic peptides designed for antibacterial application incorporated arginine as cationic amino acids and …
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New paradigm for drug design: Design and synthesis of novel biologically active peptides that are agonists at opioid receptors and antagonists at cholecystokinin receptors
… such as cholecystokinin (CCK) in which both the peptides and their receptors are increased in pain states. To effectively treat diseases involving "systems changes" a new paradigm for the design of compounds was proposed. In this new approach single peptide or peptidomimetic molecules are …
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The preparation of racemic and optically active beta-amino-acids and their utilisation in peptide formation.
… reports the successful preparation of linear and cyclic peptides of racemic and optically active B-aminobutyric acid. B-Amino acid cyclisation studies by Barker 84 had led to the conclusion that oxazinones could only be obtained from saturated B-benzamido—acids containing quaternary B-cabon atoms, …
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Novel Bifunctional Ligands For Neuropathic Pain: Design and Synthesis of Overlapping Pharmacophores of Opioid and Melanocortin Ligands
… the treatment of pain, a series of linear and cyclic peptides based on the overlapping pharmacophores of endogenous melanocyte stimulating hormone and opioid ligands are designed through computational aided molecular modeling and synthesized. Throughout the studies the opioid pharmacophore is …
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Biochemical and computational studies towards selective inhibition of the immunoproteasome
… (S1-4) allows structure-based drug design. The cyclic peptides argyrin A and F exhibit potent, reversible CP inhibition with mechanisms distinct to existing therapeutics. In this project, argyrin B inhibition and binding interactions between the CP and IP are investigated, using purified enzyme …
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