Search Results - "EGAN, TIMOTHY"

Heme Detoxification in the Malaria Parasite: A Target for Antimalarial Drug Development by de Villiers, Katherine A, Egan, Timothy J

“…Conspectus Over the last century, malaria deaths have decreased by more than 85%. Nonetheless, there were 405 000 deaths in 2018, mostly resulting from…”
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Recent advances in understanding the mechanism of hemozoin (malaria pigment) formation by Egan, Timothy J.

“…The recent literature on hemozoin/β-hematin formation is reviewed, with an emphasis on the mechanism of its formation. Recent findings from unrelated organisms…”
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Haemozoin formation by Egan, Timothy J.

“…Formation of malaria pigment or haemozoin is the major route of haem detoxification in the malaria parasite Plasmodium falciparum as well as several other…”
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Molecular Mechanism Exploration of Potent Fluorinated PI3K Inhibitors with a Triazine Scaffold: Unveiling the Unusual Synergistic Effect of Pyridine-to-Pyrimidine Ring Interconversion and CF3 Defluorination by Farrokhzadeh, Abdolkarim, Akher, Farideh Badichi, Egan, Timothy J

“…The phosphatidylinostitol-3-kinase (PI3K)/AKT/mammalian target of rapamycin signaling pathway is a vital regulator of cell proliferation, growth, and survival,…”
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Quinoline Containing Side-chain Antimalarial Analogs: Recent Advances and Therapeutic Application by Joshi, Mukesh C, Egan, Timothy J

“…The side-chains of quinoline antimalarial agents are the major concern of focus to build novel and efficaciaous bioactive and clinical antimalarials. Bioative…”
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Targeting the cannabinoid receptor CB2 in a mouse model of l-dopa induced dyskinesia by Rentsch, Peggy, Stayte, Sandy, Egan, Timothy, Clark, Ian, Vissel, Bryce

“…L-dopa induced dyskinesia (LID) is a debilitating side-effect of the primary treatment used in Parkinson's disease (PD), l-dopa. Here we investigate the effect…”
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Identifying inhibitors of β-haematin formation with activity against chloroquine-resistant Plasmodium falciparum malaria parasites via virtual screening approaches by Amod, Leah, Mohunlal, Roxanne, Teixeira, Nicole, Egan, Timothy J., Wicht, Kathryn J.

“…The biomineral haemozoin, or its synthetic analogue β-haematin (βH), has been the focus of several target-based screens for activity against Plasmodium…”
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Rhenium(I) derivatives of aminoquinoline and imidazolopiperidine-based ligands: Synthesis, in vitro and in silico biological evaluation against Plasmodium falciparum by Sovari, Sara Nasiri, Golding, Taryn M, Mbaba, Mziyanda, Mohunlal, Roxanne, Egan, Timothy J, Smith, Gregory S, Zobi, Fabio

“…A small library of aminoquinoline and imidazolopiperidine (IMP)-based ligands, containing the 1,2,3-triazole moiety, and their corresponding tricarbonyl…”
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Virtual screening as a tool to discover new β-haematin inhibitors with activity against malaria parasites by de Sousa, Ana Carolina C., Combrinck, Jill M., Maepa, Keletso, Egan, Timothy J.

“…Malaria remains a major public health problem. With the loss of antimalarials to resistance, the malaria burden will likely continue for decades. New…”
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Exploring the modulatory influence on the antimalarial activity of amodiaquine using scaffold hybridisation with ferrocene integration by Mbaba, Mziyanda, Golding, Taryn M., Omondi, Reinner O., Mohunlal, Roxanne, Egan, Timothy J., Reader, Janette, Birkholtz, Lyn-Marie, Smith, Gregory S.

“…Amodiaquine (AQ) is a potent antimalarial drug used in combination with artesunate as part of artemisinin-based combination therapies (ACTs) for malarial…”
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Intrinsic fluorescence properties of antimalarial pyrido[1,2- a ]benzimidazoles facilitate subcellular accumulation and mechanistic studies in the human malaria parasite Plasmodium falciparum by Korkor, Constance M, Garnie, Larnelle F, Amod, Leah, Egan, Timothy J, Chibale, Kelly

“…The intrinsic fluorescence properties of two related pyrido[1,2-a]benzimidazole antimalarial compounds suitable for the cellular imaging of the human malaria…”
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The Antimalarial Ferroquine: Role of the Metal and Intramolecular Hydrogen Bond in Activity and Resistance by Dubar, Faustine, Egan, Timothy J, Pradines, Bruno, Kuter, David, Ncokazi, Kanyile K, Forge, Delphine, Paul, Jean-François, Pierrot, Christine, Kalamou, Hadidjatou, Khalife, Jamal, Buisine, Eric, Rogier, Christophe, Vezin, Hervé, Forfar, Isabelle, Slomianny, Christian, Trivelli, Xavier, Kapishnikov, Sergey, Leiserowitz, Leslie, Dive, Daniel, Biot, Christophe

“…Inhibition of hemozoin biocrystallization is considered the main mechanism of action of 4-aminoquinoline antimalarials including chloroquine (CQ) but cannot…”
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Design, synthesis and in vitro antimalarial evaluation of triazole-linked chalcone and dienone hybrid compounds by Guantai, Eric M., Ncokazi, Kanyile, Egan, Timothy J., Gut, Jiri, Rosenthal, Philip J., Smith, Peter J., Chibale, Kelly

“…A targeted series of chalcone and dienone hybrid compounds containing aminoquinoline and nucleoside templates was synthesized and evaluated for in vitro…”
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Chemical Proteomics and Super-resolution Imaging Reveal That Chloroquine Interacts with Plasmodium falciparum Multidrug Resistance-Associated Protein and Lipids by Woodland, John G, Hunter, Roger, Smith, Peter J, Egan, Timothy J

“…It is well established that chloroquine, a quinoline antimalarial, inhibits hemozoin formation in the malaria parasite. Counterintuitively, this archetypal…”
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Lapatinib, Nilotinib and Lomitapide Inhibit Haemozoin Formation in Malaria Parasites by de Sousa, Ana Carolina C, Maepa, Keletso, Combrinck, Jill M, Egan, Timothy J

“…With the continued loss of antimalarials to resistance, drug repositioning may have a role in maximising efficiency and accelerating the discovery of new…”
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Fe(III) Protoporphyrin IX Encapsulated in a Zinc Metal–Organic Framework Shows Dramatically Enhanced Peroxidatic Activity by Dare, Nicola A, Brammer, Lee, Bourne, Susan A, Egan, Timothy J

“…Two MOFs, [H2N­(CH3)2]­[Zn3(TATB)2­(HCOO)]·HN­(CH3)2·DMF·6H2O (1) and Zn-HKUST-1 (2), were investigated as potential hosts to encapsulate Fe­(III) heme…”
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Interactions of quinoline antimalarials with hematin in solution by Egan, Timothy J.

“…Quinoline antimalarial drugs such as chloroquine and related compounds are believed to act by targeting ferriprotoporphyrin IX (Fe(III)PPIX) in the form of…”
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THC shows activity against cultured Plasmodium falciparum by de Sousa, Ana Carolina C., Combrinck, Jill M., Maepa, Keletso, Egan, Timothy J.

“…[Display omitted] The FDA approved drug Dronabinol was identified in a previous study applying virtual screening using the haemozoin crystal as a target…”
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A Variant PfCRT Isoform Can Contribute to Plasmodium falciparum Resistance to the First-Line Partner Drug Piperaquine by Dhingra, Satish K, Redhi, Devasha, Combrinck, Jill M, Yeo, Tomas, Okombo, John, Henrich, Philipp P, Cowell, Annie N, Gupta, Purva, Stegman, Matthew L, Hoke, Jonathan M, Cooper, Roland A, Winzeler, Elizabeth, Mok, Sachel, Egan, Timothy J, Fidock, David A

“…Current efforts to reduce the global burden of malaria are threatened by the rapid spread throughout Asia of resistance to artemisinin-based combination…”
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Insights into the Role of Heme in the Mechanism of Action of Antimalarials by Combrinck, Jill M, Mabotha, Tebogo E, Ncokazi, Kanyile K, Ambele, Melvin A, Taylor, Dale, Smith, Peter J, Hoppe, Heinrich C, Egan, Timothy J

“…By using cell fractionation and measurement of Fe­(III)­heme-pyridine, the antimalarial chloroquine (CQ) has been shown to cause a dose-dependent decrease in…”
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