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Show simple item record Makungo, T Tsekoa, Tsepo L Theron, Anjo Mancama, Dalubuhle T Van Ree, T 2020-02-07T06:04:11Z 2020-02-07T06:04:11Z 2019-04
dc.identifier.citation Makungo, T., Tsekoa, T.L., Theron, A., Mancama, D.T., Van Ree, T. 2019. Characterization, modelling and docking studies of Plasmodium falciparum kinase PfCDPK4. South African Journal for Science and Technology, v38(1), 15pp. en_US
dc.identifier.issn 2222-4173
dc.identifier.issn 0254-3486
dc.description Copyright: © 2019. Authors. Licensee: Die Suid-Afrikaanse Akademie vir Wetenskap en Kuns. This work is licensed under the Creative Commons Attibution License. en_US
dc.description.abstract Characterization, modelling and docking studies of Plasmodium falciparum kinase PfCDPK4: The increasing incidence of Plasmodium strains that are resistant to current frontline antimalarial drugs has become one of the greatest challenges of controlling malaria incidence and mortality. There is, therefore, an urgent need to develop novel targets and antimalarial drugs that are effective against drug-resistant malarial parasites. At the same time the need to develop antimalarial drugs that furthermore prevent disease transmission, has become an increasingly important consideration. Calcium dependent protein kinases (CDPKs) regulate a variety of biological processes in the malaria parasite Plasmodium falciparum, CDPK4 being of prime importance in Plasmodium biology. In this study the structure of PfCDPK4 was used as a template in the discovery of malaria drug leads. The model structure of PfCDPK4 was generated by homology modelling, and model validation confirmed that the model of PfCDPK4 is of stereochemical quality. The molecular modelling approach of in silico screening against the target molecule PfCDPK4 utilized a large library of chemical compounds, some natural chemical compounds, and clinically approved kinase inhibitors. In silico screening of the Biofocus library against PfCDPK4 resulted in twenty-six compounds being identified; in vitro screening confirmed that three of these compounds exhibit moderate antimalarial activity against the NF54 strain of Plasmodium falciparum, with the percentage inhibition ranging between 42% and 47%. en_US
dc.language.iso en en_US
dc.publisher AOSIS en_US
dc.relation.ispartofseries Worklist;22994
dc.subject Plasmodium falciparum en_US
dc.title Characterization, modelling and docking studies of Plasmodium falciparum kinase PfCDPK4 en_US
dc.type Article en_US

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