Magister Scientiae - MSc (Pharmaceutical Chemistry)

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https://hdl.handle.net/10566/14970

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Browsing by Author "Egieyeh, Samuel"

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    Homology modelling and characterization of three-dimensional (3d) protein structures of selected variants of cyp3a4
    (University of the Western Cape, 2022) Omotoso, Christianah Taye; Egieyeh, Samuel
    The efficacy and toxicity of several drugs and prodrugs are influenced by the interindividual genetic variations in drug-metabolising enzymes. Cytochrome P450 enzymes constitute the major metabolising enzymes in humans. Cytochrome 3A4 (CYP3A4) is the highest abundantly expressed human cytochrome P450 enzyme metabolising about 40% of marketed drugs. Several studies have shown the significant effects of CYP3A4 single nucleotide variability on its enzymatic activity and the pharmacokinetic parameters of metabolized drugs. However, there is a paucity of information on the molecular characteristics (including threedimensional protein structures, physicochemical properties, and molecular dynamics characteristics) of single nucleotide variants of CYP3A4 enzymes that may be correlated with the reported variability of their enzymatic activities.
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    Selection, synthesis and evaluation of novel drug-like compounds from a library of virtual compounds designed from natural products with antiplasmodial activities
    (University of the Western Cape, 2020) Pokomi, Rostand Fankam; Joubert, Jacques; Malan, Sarel; Egieyeh, Samuel
    Malaria is an infectious disease which continues to kill more than one million people every year and the African continent accounts for most of the malaria death worldwide. New classes of medicine to combat malaria are urgently needed due to the surge in resistance of the Plasmodium falciparum (the parasite that causes malaria in humans) to existing antimalarial drugs. One approach to circumvent the problem of P. falciparum resistance to antimalarial drugs could be the discovery of novel compounds with unique scaffolds and possibly new mechanisms of action. Natural products (NP) provide a wide diversity of compounds with unique scaffolds, as such, a library of virtual compounds (VC) designed from natural products with antiplasmodial activities (NAA) can be a worthy starting point.