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 28 for “"Peptide inhibitors"”.
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Lariat peptide inhibitors of Abl kinase
A majority of kinase inhibitors predominantly occupy the highly conserved adenine-binding pocket located in the kinase catalytic cleft, and therefore the target selectivity of these molecules is a major concern. In order to design highly specific next-generation drugs, it is essential to exploit …
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Rational design and optimization of anti-Cdc42 peptide inhibitors
… and functional analysis of a series of cyclic peptides, engineered as inhibitors of the Rho-family GTPase, Cdc42. The research presented builds on previous work which selected Cdc42 binding peptides using CIS-display. The structure of the highest affinity matured peptide (P7) in solution was …
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Peptide inhibitors of angiogenesis in endometriosis and the female reproductive system
… lesions, and evaluated a novel anti-angiogenic peptide as a potential therapeutic to manage endometriosis. An atlas on the microscopic anatomy of the pregnant mouse uterus is also presented. Synuclein-γ (SNCG), a protein involved in cellular proliferation, was found to have elevated expression …
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Development of peptide inhibitors as molecular therapeutics against tandem-repeat proteins
… this thesis, I have explored the development of peptide-based inhibitors of PPIs involving two targets, Tankyrase (TNKS) the Anaphase Promoting Complex/Cyclosome (APC/C-Cdc20). TNKS belong to the poly-ADP-ribose polymerases (PARP) family of enzymes that PARylate their substrates, leading to …
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Development of Natural Cyclic Peptide Inhibitors of XRCC4/XLF Interaction for Radio-Sensitization of Breast Tumor Cells
… 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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Exploring multivalency and chemical modifications in the development of anti-PD-L1 peptide inhibitors for cancer immunotherapy
… of target receptors. Over the past decade, peptides have garnered considerable interest as promising alternatives to address the limitations of existing anti-PD-L1 therapies and to overcome some of the drawbacks of mAb-based treatments. Compared to mAbs, peptides have better cell …
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Design of selective peptide inhibitors of anti-apoptotic Bfl-1 using experimental screening, structure-based design, and data-driven modeling
… makes it possible to engineer proteins and peptides with desirable interaction profiles using carefully selected sets of experiments that are customized for each design objective. There is great interest in improving the protein design pipeline to create protein binders more efficiently and …
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Development Of Peptide Inhibitors Targeting Clostridium Difficile Toxins A/b And Characterizing The Regulatory Role Of A Putative Negative Regulator Tcdc In Clostridium Difficile Toxin Gene Expression
… and further characterization of</p> <p>peptide therapeutic that target the major virulence factor TcdA/TcdB. Towards</p> <p>development of mechanistic-based anti-toxin agent, phage display was used to identify</p> <p>peptides that bind to the catalytic domain of C. difficile Toxin A. …
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Developing an a-synuclein in vitro model for therapeutic testing for Parkinson's disease
… Chapter Four: evaluates the impact of the peptide inhibitors (βsyn36D) and (S62) in reducing aggregate rates in fetal human cortical neural cells seeded with α-synuclein PFF. βsyn36D significantly reduces aggregate rates in live imaging, lowers the pathological molecular weight of …
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Requirement of ßDELSEED-Motif of <em>Escherichia coli</em> F<sub>1</sub>F<sub>O</sub> ATP Synthase in Antimicrobial Peptide Binding.
… and hydrolyzing ATP. Lately, α-helical cationic peptides such as melittin and melittin related peptide (MRP) were shown to inhibit <em>E. coli</em> ATP synthase. The proposed but unconfirmed site of inhibition is βDELSEED-motif formed by the residues 380-386, located at the interface of α/β …
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Regulation of specific connexins differentially alters gap junction permeability and endothelial cell function
… and wound healing. Using RNA interference or peptide inhibitors to downregulate specific connexins we examined the role of gap junctions in intercellular diffusion, calcium excitation, and in mediating the expression of vascular regulators transforming growth factor-[Beta][ (TGF-[beta]), …
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Modeling the flexibility of alpha helices in protein interfaces : structure based design and prediction of helix-mediated protein-protein interactions
… analysis is used to design novel nanomolar peptide inhibitors of the apoptosis-related Bcl-2 family member, Bcl-xL, and a modification of Crick Parameterization is used to predict the binding orientation of dimeric coiled coils with greater than 80% accuracy. Finally, this study addresses …
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Towards Inhibition of Oncogenic RhoA Signaling using Stapled Peptides
… in developing traditional small molecule inhibitors to many of the identified oncogenic targets, including the Ras superfamily of small GTPases. Peptide therapeutics are emerging as promising new modalities to more efficiently inhibit these "undruggable" targets. RhoA is a member of the …
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HIV entry : a biophysical and mutational analysis of gp41-mediated membrane fusion and its inhibition
… infection of host cells, and to develop inhibitors of viral entry. Env comprises two non-covalently attached subunits, gpl20 and gp41, that associate as a trimer on the virion surface. Once gp 120 contacts the target cell, gp41 undergoes extensive conformational changes to mediate fusion …
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How short, degenerate motifs across the human proteome recognize the actin remodeling factor ENAH
… this information to design selective and tight peptide inhibitors that could disrupt ENAHmediated interactions in mammalian cells. Collectively, my work highlights the importance of studying SLiMs in their native context, motivating the application of my work to other SLiM-binding domain …
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The mechanisms involved in the responses elicited by intracerebroventricular administration of renin and angiotensin in the conscious cat
Angiotensin II is an octapeptide formed by the action of the enzyme renin on a glycoprotein substrate. It has potent pharmacological effects on the central nervous system causing water drinking and vasopressor responses. Recently enzyme systems capable of the synthesis and destruction of …
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Targeting PfUCHL3 Using Chemically Constrained Peptides
… cell viability, and through the use of the RaPID peptide discovery system (Yamagishi Y et al, 2011), 10 novel, non-natural, cyclic peptides were selected for against PfUCHL3. The peptides all display tight dissociation constants for PfUCHL3 in the low nanomolar range (6-35 nM) and 4 of the 10 …
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Development of Non-Atp Competitive, Plk1-Selective Inhibitors
… REPLACE uses structure activity relationships of peptide inhibitors to generate a pharmaceutically acceptable lead molecule by replacing individual amino acid residues with non-peptide fragments. REPLACE was used to identify fragment mimetics for determinants from the endogenous phosphopeptide …
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Functional Characterization of the HIV-1 NEF Acidic Cluster
… measure; however, new measures, including peptide inhibitors and microbicides, are currently being developed and studied for their efficacy. The potential of finding new targets for controlling or preventing infection relies heavily on developments relating to the basic science of the virus …
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