Browsing by Author "Fielding, Burtram"

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    Human coronavirus OC43 3CL protease and the potential of ML188 as a broad-spectrum lead compound: Homology modelling and molecular dynamic studies
    (Springer Nature, 2015) Berry, Michael; Fielding, Burtram; Gamieldien, Junaid
    The coronavirus 3 chymotrypsin-like protease (3CLpro) is a validated target in the design of potential anticoronavirus inhibitors. The high degree of homology within the protease’s active site and substrate conservation supports the identification of broad spectrum lead compounds. A previous study identified the compound ML188, also termed 16R, as an inhibitor of the Severe Acute Respiratory Syndrome coronavirus (SARS-CoV) 3CLpro. This study will detail the generation of a homology model of the 3CLpro of the human coronavirus OC43 and determine the potential of 16R to form a broad-spectrum lead compound. MODELLER was used to generate a suitable three-dimensional model of the OC43 3CLpro and the Prime module of Schrӧdinger predicted the binding conformation and free energy of binding of 16R within the 3CLpro active site. Molecular dynamics further confirmed ligand stability and hydrogen bonding networks.
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    Medicinal uses of Galenia africana: A study of the antimicrobial, antifungal and anticancer properties
    (University of the Western Cape, 2018) Nguni, Tiza; Fielding, Burtram
    Medicinal uses of Galenia africana: A study of the antimicrobial, antifungal and anticancer properties Over the years, microorganisms have become resistant to commonly used antimicrobial agents leading to multidrug resistance. This is believed to occur even with new classes of therapeutic agents thus creating a challenge on the global healthcare system. The study of medicinal plants allows for their possible use as alternative therapeutic agents. Galenia africana (G. africana) is a South African medicinal plant with numerous health benefits. The purpose of this study was to evaluate the potential antimicrobial, antifungal and anticancer properties of the ethanolic extract of G. africana. Prior to evaluating these properties, in vitro and in vivo acute toxicity studies were conducted to assess the toxicity profile of G. africana.
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    Transient transgene expression of human coronavirus nl63 orf3 protein
    (University of the Western Cape, 2020) Liedeman, Kerwin; Fielding, Burtram
    Insect-derived baculoviruses have been used extensively as a safe and versatile research model for transgenic protein expression. Preclinical studies have revealed the promising potential of Baculoviruses as a delivery vector for a variety of therapeutic applications, including vaccination, tissue engineering and cancer treatments. Coronaviruses are enveloped viruses containing linear, non-segmented ribonucleic acid. Human coronavirus NL63 was first discovered in the Netherlands in January 2004, where a 7-month-old girl presented with an acute respiratory tract infection that was later established to predominantly infect infants, the elderly and immunocompromised individuals. In addition to the known non-structural and structural proteins of coronaviruses, an accessory protein known as open reading frame 3 which is conserved in the Coronaviridae family has not been extensively researched. Open reading frame 3 encodes a putative membrane-bound protein. This study cloned the open reading frame 3 viral gene of 741 base pairs into the baculovirus expression construct via competent bacterial cell lines. Open reading frame 3-Baculovirus particles were generated in Spodoptera frugiperda insect cells. Recombinant cells containing the viral protein gene were used to infect healthy Spodoptera frugiperda 9 cells at varying ratios of multiplicity of infection over a fixed time-course. The open reading frame 3 viral protein was not detected by quantification methods at a molecular weight of 26 kilo Dalton, due to polyclonal antibody degradation.
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    Transient transgene expression of human Coronavirus nl63 orf3 protein in a baculovirus system
    (University of Western Cape, 2020) Liedeman, Kerwin; Fielding, Burtram
    Insect-derived baculoviruses have been used extensively as a safe and versatile research model for transgenic protein expression. Preclinical studies have revealed the promising potential of Baculoviruses as a delivery vector for a variety of therapeutic applications, including vaccination, tissue engineering and cancer treatments. Coronaviruses are enveloped viruses containing linear, non-segmented ribonucleic acid. Human coronavirus NL63 was first discovered in the Netherlands in January 2004, where a 7-month-old girl presented with an acute respiratory tract infection that was later established to predominantly infect infants, the elderly and immunocompromised individuals.