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Articles by Guy Caljon
Deconvoluting the mode of action of antileishmanial aminopyrazoles through chemical mutagenesis
Abstract Aminopyrazoles have emerged as a promising series of antileishmanial compounds. Molecular target deconvolution has been a major challenge because successive drug exposure failed to select for resistance. Chemical mutagenesis combined with aminopyrazole selective pressure and whole genome sequencing was used as an alternative approach.
Effects of larval density and Wolbachia strains on life-history traits of Aedes aegypti mosquitoes
Abstract Understanding how environmental conditions and symbiotic infections shape mosquito biology is essential for predicting vectorial capacity and optimizing control strategies. Here, we investigated the effects of larval density and Wolbachia infection (wMel and wAlbB) on wing morphometry and key life-history traits of Aedes aegypti.
A breath of fresh air: impact of insect-borne protozoan parasites on the respiratory system
Highlights Diseases caused by insect-borne protozoan parasites, namely malaria, leishmaniasis, and trypanosomiasis, range from subclinical infections to severe illnesses in various hosts, including immunocompetent humans, with a profound impact on public health and economies worldwide. In addition to their usual hemolymphatic invasion and dissemination within the mammalian host, insect-borne protozoan parasites can colonize noncanonical tissues.
A breath of fresh air: impact of insect-borne protozoan parasites on the respiratory system
ReviewVolume 40, Issue 8p717-730 Laboratory of Microbiology, Parasitology and Hygiene (LMPH), Infla-Med Centre of Excellence, University of Antwerp, Wilrijk, Belgium Publication History: Published online July 15, 2024 DOI: 10.1016/j.pt.2024.06.010Also available on ScienceDirect Copyright: © 2024 Elsevier Ltd. All rights are reserved, including those for text and data mining, AI training, and similar technologies.
Hydrazinated geraniol derivatives as potential broad‐spectrum antiprotozoal agents
1 INTRODUCTION Human African trypanosomiasis (HAT), commonly known as sleeping sickness, is mainly caused by the protozoa Trypanosoma brucei gambiense in West and Central Africa.[1-3] This parasite accounts for 92% of all chronic HAT infections due to its prevalence in 24 West and Central African countries.[1] However, in 13 East and Southern African countries, the disease is primarily caused by Trypanosoma brucei rhodesiense, which mainly affects cattle and wildlife but accounts for 8% of...
Practical and Divergent Synthesis of Carbocyclic Pyrazolo[3,4‐d]pyrimidine Nucleoside Analogues
Supporting Information As a service to our authors and readers, this journal provides supporting information supplied by the authors. Such materials are peer reviewed and may be re-organized for online delivery, but are not copy-edited or typeset. Technical support issues arising from supporting information (other than missing files) should be addressed to the authors.
Q586B2 is a crucial virulence factor during the early stages of Trypanosoma brucei infection that is conserved amongst trypanosomatids - Nature Communications
Abstract Human African trypanosomiasis or sleeping sickness, caused by the protozoan parasite Trypanosoma brucei, is characterized by the manipulation of the host’s immune response to ensure parasite invasion and persistence. Uncovering key molecules that support parasite establishment is a prerequisite to interfere with this process. We identified Q586B2 as a T. brucei protein that induces IL-10 in myeloid cells, which promotes parasite infection invasiveness. Q586B2 is expressed during all T.
Late‐Stage Diversification of Pyrazoles as Antileishmanial Agents
Supporting Information As a service to our authors and readers, this journal provides supporting information supplied by the authors. Such materials are peer reviewed and may be re-organized for online delivery, but are not copy-edited or typeset. Technical support issues arising from supporting information (other than missing files) should be addressed to the authors.
Late‐Stage Diversification of Pyrazoles as Antileishmanial Agents
Supporting Information As a service to our authors and readers, this journal provides supporting information supplied by the authors. Such materials are peer reviewed and may be re-organized for online delivery, but are not copy-edited or typeset. Technical support issues arising from supporting information (other than missing files) should be addressed to the authors.
Design and synthesis of imidazo[1,2‐a]pyridine‐chalcone conjugates as antikinetoplastid agents
1 INTRODUCTION Kinetoplastids represent a class of flagellated eukaryotic parasites and the uniflagellate trypanosomatids including the Leishmania and Trypanosoma species (Deschamps et al., 2011; Molyneux et al., 2017; Povelones, 2014; Stuart et al., 2008). The distinguished feature associated with this group is the presence of a kinetoplast (mitochondrial structure containing circular DNA) (Davis et al., 2003).
Structural Optimization of BIPPO Analogs as Potent Antimalarials
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Tetrahydrophthalazinone Inhibitor of Phosphodiesterase with In Vitro Activity against Intracellular Trypanosomatids
Experimental Therapeutics Julianna Siciliano de Araújo, Raiza Brandão Peres, Patrícia Bernardino da Silva, Marcos Meuser Batista, Geert Jan Sterk, Louis Maes, Guy Caljon, Rob Leurs, Harry P. de Koning, Titilola D. Kalejaiye, Maria de Nazaré Correia Soeiro DOI: 10.1128/AAC.00960-20 ABSTRACT The phosphodiesterase inhibitor tetrahydrophthalazinone NPD-008 was explored by phenotypic in vitro screening, target validation, and ultrastructural approaches against Trypanosoma cruzi.
Combining tubercidin and cordycepin scaffolds results in highly active candidates to treat late-stage sleeping sickness
Abstract African trypanosomiasis is a disease caused by Trypanosoma brucei parasites with limited treatment options. Trypanosoma is unable to synthesize purines de novo and relies solely on their uptake and interconversion from the host, constituting purine nucleoside analogues a potential source of antitrypanosomal agents.
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