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.
Results
Showing 1 to 15 of 15 for “"Entry inhibitors"”.
-
Development of Small Molecules as Broad-spectrum Filoviral Entry Inhibitors
… is used to mediate several steps in filoviral entry. In the effort to develop broad-spectrum antifilovirals, a series of N-substituted pyrrole-based heterocycles and elacestrant derivatives were developed to target GP and effectively inhibit diverse filoviral entry in a pseudovirus assay. …
-
Mechanistic Studies of Small Molecule Entry Inhibitors of Influenza A Viruses
… Hence, it is crucial to develop anti-influenza inhibitors that exhibit strong effectiveness against novel viral targets. Considering the criticality of the IAV surface glycoprotein hemagglutinin (HA) for IAV receptor binding and fusion, the focus of this thesis was the following: 1) …
-
Characterisation of llama antibody fragments able to act as HIV-1 entry inhibitors
Human immunodeficiency virus type 1 (HIV-1) entry into cells is mediated by the functional envelope spike, which consists of trimers of gp120 bound to gp41. Most variants of HIV-1 enter cells through attachment of the envelope spike to the main cellular receptor CD4, allowing interaction with a …
-
DESIGN, SYNTHESIS, AND OPTIMIZATION OF SMALL-MOLECULE CD4 MIMETICS AS HIV-1 ENTRY INHIBITORS AND SYNTHETIC EFFORTS TOWARD THE TOTAL SYNTHESIS OF NAHUOIC ACID Cii
… represent a promising strategy that blocks viral entry by binding to the conserved Phe43 cavity of gp120, thereby competing with native CD4 for Env engagement. Beyond direct entry inhibition, CD4mcs induce conformational rearrangements that expose normally occluded epitopes on gp120, sensitizing …
-
A Novel Gene Therapy Approach Based on Secreted Antiviral Proteins for the Control of HIV Replication
HIV entry into target cells requires the interaction of the HIV envelope glycoprotein (Env) with a primary receptor (CD4) and a co-receptor (most commonly CCR5 or CXCR4). Protein-based HIV entry inhibitors are highly effective in protecting cells from infection. However, their clinical application …
-
Mechanisms of CCR5 Agonist/Antagonist Inhibition of HIV-1 Entry and In Vitro Selection of Virus Resistant to Maraviroc
Entry inhibitors represent a new class of antiretrovirals for the treatment of HIV-1 infection. These inhibitors target interactions of the viral envelope glycoprotein with host cell receptors as well as fusion of the viral and host cell membranes. Extensive development of inhibitors that target …
-
The Design And Synthesis Of Inhibitors Of Hiv-1 Viral Entry And Photoaffinity Labeled Probes For Structural Elucidation Of The Hiv-1 Env
… family of small molecule “Dual-Action Virucidal Entry Inhibitors” (DAVEIs). These compounds, comprised of a small molecule warhead tethered to a segment of the gp41 MPER denoted Trp3, have achieved irreversible lytic inactivation of HIV-1 virions. Finally, small molecules appended with …
-
Synthesis of Macrocyclic Polyamines and their Cu, Fe, Mn and Zn Complexes Targeting HIV (AIDS).
… (CADA) and bicyclam AMD3100 act as entry inhibitors against HIV by different mechanisms. The manganese complex of pyridine-fused macrocyclic polyamine (M40401) has been found to reduce HIV-1 induced apoptosis of astroglial cells. Based on these findings, seventeen new compounds were …
-
Structure-based Design of Small Molecule Inhibitors of HIV-1 Entry
… and replication. One of the targets of HIV entry inhibitors is the interaction between CD4 and gp120. A large percentage of CD4-gp120 contacts revolved around a cavity in gp120 in which the PHE43 residue of CD4 caps. We were able to design and synthesize a progression of small molecule …
-
Male genital tract versus blood HIV-1 compartmentalization and selection: the first step of the transmission bottleneck?
… tested the sensitivity of variants to a range of entry and other inhibitors in order to explore possible changes in function that may arise when viral variants grow in the shifted selective milieu of the genital tract. We further hypothesized that this change of selective milieu as HIV-1 moves …
-
The pharmacologenetics of lopinavir in a cohort of black African HIV/AIDS patients
… and non-nucleoside reverse transcriptase inhibitors (NRTIs/NNRTIs); fusion/entry inhibitors; integrase inhibitors; and protease inhibitors (PIs). In South Africa PIs, specifically lopinavir (LPV) boosted with another PI, ritonavir (RTV) are used in second-line ARV regimens along with a …
-
Characterisation of HIV-1 Envelope features of breakthrough infections from the CAPRISA 004 Microbicide Trial
… assays were performed using the following inhibitors: tenofovir, maraviroc, T20, PSC-RANTES and anti-CD4 antibody clone SK3. In addition, envs for 19 participants were cloned and used to generate pseudoviruses which were evaluated for entry efficiency. Viral isolates were identical or very …
-
Single Molecule Ligand Binding Studies on CCR5 by Fluorescence Cross-Correlation Spectroscopy
… only Food and Drug Administration (FDA) approved entry inhibitor for HIV-1 but resistance to maraviroc has been reported indicating the need for novel entry inhibitors. Recently, four peptides derived from RANTES (Regulated on Activation, Normal T cell Expressed and Secreted), the endogenous …
-
Characterisation of functional properties of Envelopes of highly neutralisation resistant HIV-1 isolates
… between neutralisation resistance and entry efficiency. Very highly neutralisation resistant viruses appear under-represented in the population. We hypothesised that this may be at least partially explained by decreased entry efficiency as changes to Envelope (Env) during escape could …
-
The HIV-1 entry inhibition capabilities of Isoflavones
… HIV life cycle but with little research in HIV entry inhibition. In this study, the anti-HIV activity of the isoflavones was quantified through the generation of IC50 values using a luciferase reporter assay. Evidence for potential entry-inhibiting activity was generated through time-of-addition …