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Dissertations / Theses on the topic 'HIV fusion inhibitor'

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1

Quinn, Killian. "The development of a new fusion inhibitor for the treatment of HIV." Thesis, Imperial College London, 2017. http://hdl.handle.net/10044/1/50677.

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Since the introduction of combination antiretroviral therapy (ART), there has been a dramatic improvement in the prognosis of people living with HIV. Indeed, data from numerous cohorts now show that for people commenced on ART at high CD4 counts and who are retained in care, life expectancy is similar to matched HIV-negative people. Consequently, the number of years an individual diagnosed with HIV can expect to be treated with ART is set to increase markedly. With the emergence of an older population, polypharmacy and drug-drug interactions are now more prominent clinical problems in the mana
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2

Fallarino, Lorena. "Anti HIV-1 gene therapy approach combining multiple siRNAs with the membrane-anchored fusion inhibitor C-peptide maC46." Doctoral thesis, Università degli studi di Padova, 2018. http://hdl.handle.net/11577/3426674.

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The development of highly active anti-retroviral therapy (HAART) has considerably improved life expectancy of HIV-1 positive patients by transforming this infection, which once was lethal, into a manageable chronic illness. Although a significant suppression of viral replication under undetectable level is guaranteed following a constant therapeutic adherence, this therapy fails to completely eliminate the infection due to the persistence of HIV-1 into reservoirs, which represent therefore the main obstacle to a definite cure. Furthermore, a lifelong adherence to treatment is associated with d
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3

Martins, do Canto António Manuel teixeira. "Estudo teórico da estrutura e dinâmica de péptidos inibidores da fusão do HIV em água e membranas biológicas." Doctoral thesis, Instituto de Formação Avançada, Universidade de Évora, 2013. http://hdl.handle.net/10174/10012.

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A acção dos péptidos inibidores de fusão (FI) do HIV, T-20 e T-1249, foi analisada nesta tese por uma abordagem in silico através da técnica de dinâmica molecular (MD). Foi estudada tanto a estrutura como a dinâmica destes FI em três situações diferentes: em solução (com o intuito de tentar mimetizar a situação do péptido no plasma sanguíneo) e a interagir com modelos de membranas de 1-palmitoil-2-oleil-fosfatidilcolina (POPC) (na fase líquido desordenado - Ld) e membranas de POPC / colesterol (1:1) (POPC / Chol) (na fase líquido ordenado – Lo). Com isto tentámos perceber se haveria diferenças
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4

Silva, Fabio Eduardo Santos da. "Avaliação da resistência genotípica ao Enfuvirtida em pacientes submetidos ao HAART. Fenotipagem virtual das cepas de HIV1 isoladas de trinta e dois pacientes que apresentaram resistência aos antirretrovirais." Universidade de São Paulo, 2009. http://www.teses.usp.br/teses/disponiveis/9/9136/tde-19112009-132144/.

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Introdução: estudos com Enfuvirtida (ENF) mostraram que mutações na HR1 da gp41 levam à resistência primária de cepas em pacientes sem tratamento prévio com inibidores de fusão (Derdeyn et al., 2000; Rimsky et. al., 1998; Sista et. al., 2002). Outros, que o uso contínuo de HAART leva à falha virológica (Shafer et. al., 1998; Shafer & Vuitton, 1999). Para a melhor escolha terapêutica recomenda-se usar a Genotipagem do HIV1 (Ministério da Saúde, 2008b; Perez-Elias et. al., 2003; Shafer et. al., 2001). Objetivos: avaliar o perfil de resistência do HIV1 ao ENF pelo sequenciamento da HR1 da gp41 em
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5

Chinnadurai, Raghavan. "HIV-1 resistance to fusion inhibitors." [S.l. : s.n.], 2007. http://nbn-resolving.de/urn:nbn:de:bsz:289-vts-58600.

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6

Cherry, Elana. "Trans-dominant negative inhibition of human immunodeficiency virus type 1 replication by expression of protease-reverse transcriptase fusion proteins." Thesis, National Library of Canada = Bibliothèque nationale du Canada, 1999. http://www.collectionscanada.ca/obj/s4/f2/dsk1/tape7/PQDD_0019/NQ50069.pdf.

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7

Suntoke, Tara R. "HIV entry : a biophysical and mutational analysis of gp41-mediated membrane fusion and its inhibition." Thesis, Massachusetts Institute of Technology, 2005. http://hdl.handle.net/1721.1/31181.

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Thesis (Ph. D.)--Massachusetts Institute of Technology, Dept. of Biology, 2005.<br>Includes bibliographical references.<br>The experiments described in this thesis were designed to elucidate the manner in which the HIV-1 envelope protein (Env) initiates 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 of viral and cellular membranes. First, a short hydrophob
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8

Huhmann, Susanne [Verfasser]. "Stabilization of peptides by site-specific incorporation of fluorinated amino acids: Model studies and the development of fluorinated, peptide-based HIV-1 fusion inhibitors / Susanne Huhmann." Berlin : Freie Universität Berlin, 2019. http://d-nb.info/1176632922/34.

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9

Baron, Alice. "Synthèse et Etude d'Analogues Peptidiques en tant qu'Inhibiteurs de Fusion du VIH." Thesis, Montpellier 2, 2010. http://www.theses.fr/2010MON20209/document.

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Depuis la découverte du Virus de l'Immunodéficience Humaine (VIH) au début des années 80, la recherche de nouvelles molécules anti-VIH demeure un challenge important pour la communauté scientifique. Les effets secondaires liés à l'usage d'inhibiteurs de la réplication virale, la découverte des récepteurs et la compréhension du mécanisme d'entrée du virus dans la cellule hôte ont encouragé la recherche sur de nouveaux inhibiteurs ciblant l'entrée virale. A ce jour, l'Enfuvirtide est le seul inhibiteur d'entrée approuvé en tant qu'inhibiteur de fusion. Bien que ce composé soit un antiviral puiss
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10

Chinnadurai, Raghavan [Verfasser]. "HIV-1 resistance to fusion inhibitors / presented by Raghavan Chinnadurai." 2006. http://d-nb.info/995860548/34.

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11

Borrego, Pedro José Vieira Borga Martins 1980. "Probing entry inhibitors' activity on HIV and development of new fusion inhibitors : integrating evolutionary biology with virology." Doctoral thesis, 2011. http://hdl.handle.net/10451/4598.

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Tese de doutoramento, Farmácia (Microbiologia), Universidade de Lisboa, Faculdade de Farmácia, 2011<br>The general aims of this thesis were: 1) to examine the C2, V3 and C3 envelope regions ofHIV-1 and HIV-2 at the molecular, evolutionary and structural levels; 2) to compare HIV-1and HIV-2 susceptibility to entry inhibitors and assess their potential value in HIV-2therapy; 3) to produce a new fusion inhibitor peptide using evolutionary biology basedstrategies.In the first study (Chapter 2), HIV-1 and HIV-2 were compared at the molecular,evolutionary and structural levels in the C2, V3 and C3 e
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12

Augusto, Marcelo Alexandre da Costa Tavares. "Interactions of HIV fusion inhibitors with biomembranes model systems and human blood cells." Master's thesis, 2013. http://hdl.handle.net/10451/9564.

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Tese de mestrado em Bioquímica, apresentada à Universidade de Lisboa, através da Faculdade de Ciências, 2013<br>O Síndrome da Imunodeficiência Adquirida (SIDA) é uma das doenças infecciosas mais sérias que tem afetado a humanidade, cujo agente causador é o vírus da imunodeficiência humana (HIV). Em geral, o sistema imunitário fica enfraquecido, levando a um aumento da suscetibilidade dos pacientes a infeções de baixa gravidade na ausência da imunossupressão, bem como tumores que normalmente não afetam indivíduos saudáveis. Existem dois tipos de HIV, sendo o vírus do tipo 1 (HIV-1) o mais vir
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13

Santos, Ana Catarina Cunha 1986. "Antibody engineering for HIV therapeutics : from fusion inhibition to delivery of genetic regulators." Doctoral thesis, 2017. http://hdl.handle.net/10451/29865.

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Tese de doutoramento, Farmácia (Biotecnologia Farmacêutica), Universidade de Lisboa, Faculdade de Farmácia, 2017<br>Despite latest advances on antiretroviral therapeutics, HIV infection continues to be a chronic condition with serious complications and burden costs of treatment. The rapidly emergence of resistant strains constitutes a major contributor for failure of standard therapy. Accordingly, there is a continuous need for design of innovative HIV inhibitors against conserved and important targets on virus replication cycle. On the other hand, the exploration of novel classes of HIV inhib
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14

Kagiampakis, Ioannis. "Improving the Anti-HIV Potency of Different Compounds through Synergy and Covalent Linkage: Dimerization Studies of CXCL8." Thesis, 2010. http://hdl.handle.net/1969.1/ETD-TAMU-2010-08-8512.

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In the first part of my dissertation we focused on the development of covalently linking compounds that bind gp120 with those that bind gp41 in order to block HIV fusion. We used griffithsin or CD4M33, that both bind to gp120, covalently linked with C-peptide C37 of gp41. The results show the linked compound Griff37 is several-fold more potent than griffithsin alone in both fusion and viral assay, making Griff37 an attractive candidate for further development as a microbicide against HIV. In the second part of my dissertation we investigate the effect of combining HIV fusion inhibitors having
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15

Franquelim, Henri Girão 1984. "The role of lipid membranes in the mechanism of action of sifuvirtide and other HIV-1 fusion inhibitors." Doctoral thesis, 2012. http://hdl.handle.net/10451/7113.

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Tese de doutoramento, Ciências Biomédicas (Bioquímica Médica), Universidade de Lisboa, Faculdade de Medicina, 2012<br>The HIV‐1 fusion process, mediated by the viral gp120‐gp41 complex, occurs in extreme confinement between the viral and cellular membranes. The efficacy of HIV‐1 fusion inhibitors (FIs) may, therefore, be related to their ability to interact with membranes. Lipid membranes can serve as catalysts in the mode of action of this class of inhibitors, by providing a local increased concentration of the drugs near the fusion site. Peptide‐based FIs derived from the gp41 C‐termina
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16

"Search of inhibitors that target HIV pre-mRNA splicing to overcome drug resistance." 2012. http://library.cuhk.edu.hk/record=b5549184.

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引發獲得性免疫缺陷綜合癥(AIDS)的人類免疫缺陷病毒(HIV)是一種逆轉錄病毒。過去的十餘年間,高效抗逆轉錄病毒治療療法(HARRT),在抗病毒感染方面取得了很大的成功。高效抗逆轉錄病毒治療療法是一種將多種抗逆轉錄病毒藥物複合的藥物聯用療法。然而,因為病毒的逆轉錄過程極易突變,導致HIV已經可以對大多數使用的抑製藥物產生抗藥性。因此,有越來越多的需要去尋找新型的抗病毒複製機理,例如將人體細胞蛋白作為載體,來達到克服病毒抗藥性的目的。<br>HIV-1的複製離不開宿主細胞的剪接因子,例如SR蛋白。選擇性剪接因子ASF/SF2,一個典型的調控pre-RNA剪接的SR蛋白,在HIV-1的pre-mRNA剪接和複製中起到了很重要的調控作用。ASF/SF2和其他SR蛋白一樣,都被丝氨酸/苏氨酸蛋白激酶(SRPK)磷酸化,磷酸化位點位於C端的丝氨酸/苏氨酸結構域(RS domain)。SRPK通過磷酸化來調節ASF/SF2在細胞中的分佈。對於SRPK 和ASF/SF2複合物的結構學和功能學研究指出,ASF/SF2的docking motif和SRPK1的遠離活性位點的docking groove存在很強的相互作用。而這種相互作用是調節磷酸化過程關鍵。所以,在我們的研究過程中,我們希望通過阻斷2個蛋白的相互作用來干擾ASF/SF2的磷酸化,進而抑制其在HIV-1 pre-mRNA剪接過程中的活
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17

Mulampaka, Shiva Naresh. "Theoretical Studies of the Mechanisms of the Entry of Virus into Cells." Thesis, 2014. http://etd.iisc.ac.in/handle/2005/3082.

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Viruses cause human diseases by entering in to human cells. Many drugs have been developed that act at various stages of viral infection, but they fail due to their toxic side effects and high mutation rates of viruses. Recently, a new class of drugs called entry inhibitors has been developed which acts on the early stages of viral infection. These drugs have been developed by studying the entry process of viruses in to host cells. The success of these drugs, however, is still limited and research is being done to quantify the optimum dosage of these drugs and find new drugs targets. We develo
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18

Mulampaka, Shiva Naresh. "Theoretical Studies of the Mechanisms of the Entry of Virus into Cells." Thesis, 2014. http://hdl.handle.net/2005/3082.

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Viruses cause human diseases by entering in to human cells. Many drugs have been developed that act at various stages of viral infection, but they fail due to their toxic side effects and high mutation rates of viruses. Recently, a new class of drugs called entry inhibitors has been developed which acts on the early stages of viral infection. These drugs have been developed by studying the entry process of viruses in to host cells. The success of these drugs, however, is still limited and research is being done to quantify the optimum dosage of these drugs and find new drugs targets. We develo
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19

Zhao, Bo. "Structural and Functional Studies of the Receptor-binding and Glycosaminogly-canbinding Mechanisms of a Viral Chemokine Analog vMIP-II and Rational Design of Chemokine-based Highly Potent HIV-1 Entry Inhibitors." Thesis, 2011. http://hdl.handle.net/1969.1/ETD-TAMU-2011-05-9230.

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Chemokines are small immune system proteins mediating leukocyte migration and activation, and are important in many aspects of health and diseases. Some chemokines also have the ability to block HIV-1 infection by binding to the HIV-1 co-receptors CCR5 (CC chemokine receptor 5) and CXCR4 (CXC chemokine receptor 4). The first part of this work is to determine the mechanism of action of a human herpesvirus-8 encoded viral chemokine analog vMIP-II (viral macrophage inflammatory protein-II) by characterizing its interactions with endothelial surface glycosaminoglycans (GAGs) and cell surface rec
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