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All Outputs (31)

Alteration of the expression of sirtuins and var genes by heat shock in the malaria parasite Plasmodium falciparum (2022)
Journal Article

Background In Plasmodium falciparum the monoallelic expression of var virulence genes is regulated through epigenetic mechanisms. A study in the Gambia showed that an increase in var gene expression is associated with fever, high blood lactate with... Read More about Alteration of the expression of sirtuins and var genes by heat shock in the malaria parasite Plasmodium falciparum.

N,N ''-Substituted thioureas and their metal complexes: syntheses, structures and electronic properties (2022)
Journal Article

The synthesis of six N,N'-substituted thiourea ligands (L1a-L3b) was achieved in two steps. A corresponding extensive series of Cu(I), Cu(II), Ni(II) and Zn(II) complexes (1-24) with varying formulations were synthesised from these ligands by the rea... Read More about N,N ''-Substituted thioureas and their metal complexes: syntheses, structures and electronic properties.

Temperate zone plant natural products – a novel resource for activity against tropical parasitic diseases (2021)
Journal Article

The use of plant-derived natural products for the treatment of tropical parasitic diseases often has ethnopharmacological origins. As such, plants grown in temperate regions remain largely untested for novel anti-parasitic activities. We describe her... Read More about Temperate zone plant natural products – a novel resource for activity against tropical parasitic diseases.

In vivo efficacy and metabolism of the antimalarial cycleanine and improved in vitro antiplasmodial activity of novel semisynthetic analogues. (2020)
Journal Article

Bisbenzylisoquinoline (BBIQ) alkaloids are a diverse group of natural products that demonstrate a range of biological activities. In this study, the in vitro antiplasmodial activity of three BBIQ alkaloids (cycleanine (1), isochondodendrine (2) and 2... Read More about In vivo efficacy and metabolism of the antimalarial cycleanine and improved in vitro antiplasmodial activity of novel semisynthetic analogues..

The relative rate of kill of the MMV Malaria Box compounds provide links to the mode of antimalarial action and highlight scaffolds of medicinal chemistry interest (2019)
Journal Article

Objectives: Rapid rate-of-kill (RoK) is a key parameter in the target candidate profile 1 (TCP1) for the next-generation antimalarial drugs for uncomplicated malaria, termed Single Encounter Radical Cure and Prophylaxis (SERCaP). TCP1 aims to rapidly... Read More about The relative rate of kill of the MMV Malaria Box compounds provide links to the mode of antimalarial action and highlight scaffolds of medicinal chemistry interest.

Development of NanoLuc-PEST expressing Leishmania mexicana as a new drug discovery tool for axenic- and intramacrophage-based assays. (2018)
Journal Article

The protozoan parasite Leishmania causes leishmaniasis; a spectrum of diseases of which there are an estimated 1 million new cases each year. Current treatments are toxic, expensive, difficult to administer, and resistance to them is emerging. New th... Read More about Development of NanoLuc-PEST expressing Leishmania mexicana as a new drug discovery tool for axenic- and intramacrophage-based assays..

G-quadruplex DNA motifs in the malaria parasite Plasmodium falciparum and their potential as novel antimalarial drug targets (2018)
Journal Article

G-quadruplexes are DNA or RNA secondary structures that can be formed from guanine-rich nucleic acids. These four-stranded structures, composed of stacked quartets of guanine bases, can be highly stable and have been demonstrated to occur in vivo in... Read More about G-quadruplex DNA motifs in the malaria parasite Plasmodium falciparum and their potential as novel antimalarial drug targets.

Identification of heparin modifications and polysaccharide inhibitors of Plasmodium falciparum merozoite invasion that have potential for novel drug development. (2017)
Journal Article

Despite recent successful control efforts, malaria remains a leading global health burden. Alarmingly, resistance to current antimalarials is increasing, and the development of new drug families is needed to maintain malaria control. Current antimala... Read More about Identification of heparin modifications and polysaccharide inhibitors of Plasmodium falciparum merozoite invasion that have potential for novel drug development..

A validated bioluminescence-based assay for the rapid determination of the initial rate of kill for discovery antimalarials (2016)
Journal Article

Objectives: A future treatment for uncomplicated malaria will contain at least one component that exerts a rapid rate of kill. We describe here the validation and application of a simple, robust and rapid bioluminescence-based assay for the determina... Read More about A validated bioluminescence-based assay for the rapid determination of the initial rate of kill for discovery antimalarials.

Triaging informative cis -regulatory elements for the combinatorial control of temporal gene expression during Plasmodium falciparum intraerythrocytic development (2015)
Journal Article

Background Over 2700 genes are subject to stage-specific regulation during the intraerythrocytic development of the human malaria parasite Plasmodium falciparum. Bioinformatic analyses have identified a large number of over-represented motifs in the... Read More about Triaging informative cis -regulatory elements for the combinatorial control of temporal gene expression during Plasmodium falciparum intraerythrocytic development.