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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 50 for “"Peptidomimetic"”.
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Experimental and Computational Advancements in Peptidomimetic Ligand Discovery
The usage of peptides as therapeutics is a growing area of interest within the pharmaceutical industry for the facilitation of protein-protein interactions (PPIs). Peptides inhabit a unique therapeutic space because of their high levels of chemical customization balanced with their potential for …
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Improving Cardiac Delivery of Antisense Oligonucleotides with Peptidomimetic Targeting Agents
… (AS-MS), with which we can find short peptide or peptidomimetic targeting agents with nM binding affinity to target proteins. Here, I describe a platform for selecting and procuring cardiac-specific proteins or their extracellular domains (ectodomains), in some cases employing the automated …
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Design, synthesis, and thermodynamic evaluation of peptidomimetic ligands binding to the Src SH2 domain
… both. Binding studies of various pYEEI-derived peptidomimetic ligands to the Src SH2 domain were evaluated to investigate the effects of structural changes on protein-ligand binding energetics. The effect of preorganizing the pYEEI ligand into its binding conformation was analyzed by …
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Novel chemical entities against tropical diseases: Peptidomimetic lipopeptides as new anti-orthoflavivirals and 5,6,7,8-tetrahydroimidazo[1,2-a]pyridine derivatives as new antimalarials
Contains fulltext : 310090.pdf (Publisher’s version ) (Open Access)
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Advancing the field of polypeptoids through the synthesis of novel architectures and thermoresponsive polymers
Peptidomimetic polymers are an emerging class of polymers that are structurally related to polypeptides. Due to their structural similarities, these polymers can be used to study some of the physical aspects of polypeptides (for example, protein folding). They are also increasingly being used in …
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Methodologies For Attaching Polypyridyl Ligands Into Amino Acids And Synthesis And Biological Evaluation Of Novel Light Activated Peptidomimetic Cysteine Protease Inhibitors Caged By Ruii(bpy)2
<p>Two separate subjects are described in this dissertation. The first part describes novel methodologies for attaching polypyridyl ligands into unnatural amino acids. The first chapter describes the different possibilities for attaching metal ligands to peptides and their applications as potential …
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Targeting protein: protein interaction sites for drug development against voltage-gated sodium channels
… a short sequence on FGF14 and designed a peptidomimetic (ZL181) fragment as an effective probe for modulating Nav1.6 channels as measured by luciferase-based assay. This peptidomimetic was further evaluated with purified proteins, in silico docking, and whole-cell patch clamp …
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Design and synthesis of novel non peptidomimtic beta-secretase inhibitors in the treatment of Alzheimer's disease
… substrate-based inhibitors, designed as peptidomimetic inhibitors, and non-peptidomimetic ones. The research on non-peptidomimetic small molecules BACE1 inhibitors remains the most interesting approach, since these compounds hold an improved bioavailability after systemic administration, …
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I. Molecular Probes for the Progesterone Receptor. II. Design and Synthesis of a Rigidly Constrained Peptidomimetic as a Potential Beta-Turn Mimic. III. Isolation and Characterization of Novel Ion Channel Modulators From Commercial Phenol Red Preparations
Chemical probes for steroid receptors have proven useful in providing molecular details about important hormone-receptor interactions. $16\alpha,17\alpha$- ((R)-1$\sp\prime$-(4-Azidophenyl)-ethylidenedioxy) pregn-4-ene-3,20-dione (12) was prepared in high specific activity tritium-labeled form (20 …
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Design, synthesis and mode of action of short biphenyl and anthranilamide cationic peptidomimetics
… focused on the development of short cationic peptidomimetics that employ 3'-amino-[1, 1 '-biphenyl)-3-carboxylic acid and anthranilic acid backbones segregated by hydrophobic and cationic groups. The biphenyl peptidomimetic compounds showed that simple diaminoethanes and their respective …
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Synthesis of Novel Sulfonamide-Based Calpain Inhibitors and Their Potential as Anti-Tumor Agents
… active site of calpain, novel sulfonamide-based peptidomimetic analogues of <strong>1 </strong>were synthesized and assayed for their ability to inhibit µ-calpain utilizing a kinetic fluorescence assay and for their anti-tumor ability by SRB colorimetric assay (Chapter 3). Introduction of the …
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Pin1: WW domain ligands, catalytic inhibitors, and the mechanism
… libraries. By using the ELEBA, a pSer-Pro peptidomimetic library of 315 ligands was screened, identifying three promising ligands cis-D2, O2, and M18. Competitive Kd values for cis-D2, O2, and M18 were determined to be 263 ± 6.4, 206 ± 3.4, and 130 ± 3.0μM, respectively. Furthermore, we …
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Syntheses, bioactivities and conformations of peptidomimetics containing 2,3-methanoamino acids
… -2-oxo-3-oxa-bicyclo (3.1.0) hexane. Peptidomimetics containing some of these 2,3-methanoamino acids mentioned above were synthesized via a solid phase approach. The Met$\sp2$ in neuropeptide Phe-Met-Arg-Phe-NH$\sb2$ (FMRF-NH$\sb2$, one letter code for amino acids) was systematically …
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DESIGN AND SYNTHESIS OF NEW PEPTIDOMIMETICS AS POTENTIAL INHIBITORS OF HIV-1 PROTEASE
… with the design and synthesis of peptides and peptidomimetics as potential inhibitors of HIV-1 protease that can circumvent drug resistance and that can be alternatives to active site PR inhibitors. Two different approaches were applied to reach our target. The first one, described in chapter …
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I. Estrogen receptor-mediated inhibition of inflammatory signaling: Implications for treatment of breast cancer II. Small molecule coactivator-binding inhibitors
… that facilitate transcription. We used a peptidomimetic approach to mimic conserved amino acids on the coactivator proteins. Compounds designed in this way did not inhibit the interaction between the estrogen receptor and a coactivator protein.
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I.~Design, Synthesis, and Evaluation of a Rigidly Constrained Peptidomimetic as a Potential Type I Beta-Turn. II.~Development of Novel Estrogen Receptor Ligands With Unique Endocrine Profiles. III.~Design, Synthesis and Biological Evaluation of Potential Aspartic Protease Inhibitors Based on the Diaziridine and Diazirine Isostere
We have prepared novel aspartic proteases inhibitors based on the diaziridine and diazirine isostere, as potential transition-state mimics of the tetrahedral intermediate found along the reaction pathway for enzyme mediated peptide bond hydrolysis. These isosteres (143 and 144) have been …
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I Progress towards the synthesis of plakortether B through a zinc-mediated homologation II Synthesis of novel hydroxy-cyclopropyl peptides isosteres
… The lactone was seen as a precursor to a peptidomimetic that would contain an embedded hydroxycyclopropyl moiety. The formation of the bicyclic lactones was proposed to involve a cascade of homologation-cyclopropanation-rearrangement-lactonization reactions. Amino acid-derived beta-keto …
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Small molecule inhibition of immunoregulatory protein-protein interactions
… utilized two binding-based approaches, a unique peptidomimetic fragment library and high-throughput small-molecule microarrays to design and discover molecules that target three important immunoregulatory PPIs: the DQ8-insulin complex, the KEAP1-Nrf2 complex, and the IL-4/IL-4R receptor complex. …
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