Paul R. Gilson

Improving the capacity of vaccine-induced antibodies to arrest the growth of Plasmodium falciparum

Paul R. Gilson, Alysha H. Literski, Claudia Barnes, Molly Parkyn Schneider et autres

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Unpacking boxes: identification of novel inhibitors of malaria parasite invasion

Claudia B. G. Barnes, Molly Parkyn Schneider, Olivia D. Ventura, Zahra Razook et autres

With resistance to current frontline antimalarial treatments rapidly emerging in malaria endemic regions, there is an urgent need to identify new antimalarial compounds with novel mechanisms of action. Currently, no clinically used antimalarials target erythrocyte invasion, the process by which the short-lived, …

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MMV687794 blocks Plasmodium falciparum invasion of red blood cells by targeting a Surface-associated Lipid-Interacting Rhoptry Protein, Pf SLIRP

Dawson B. Ling, Ghizal Siddiqui, Christopher A. MacRaild, Yoshiki Yamaryo‐Botté et autres

Abstract Invasion of red blood cells (RBCs) by the human malaria parasite, Plasmodium falciparum , drives disease. During invasion, the parasite pushes its way into the RBC while wrapping the RBC membrane around itself to establish the parasitophorous vacuole, a stable niche …

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Deconvolution of the On-Target Activity of Plasmepsin V Peptidomimetics in Plasmodium falciparum Parasites

W.-G. Su, William Nguyen, Ghizal Siddiqui, Jerzy M. Dziekan et autres

High Resolution Image Download MS PowerPoint Slide Plasmepsin V (PMV), an essential aspartyl protease, plays a critical role during the asexual blood stage of infection of Plasmodium by enabling the export of parasite proteins into the host red blood cell. This export …

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Deconvolution of the on-target activity of plasmepsin V peptidomimetics in P. falciparum parasites

W.-G. Su, William Nguyen, Ghizal Siddiqui, Jerzy M. Dziekan et autres

ABSTRACT Plasmepsin V (PMV), an essential aspartyl protease, plays a critical role during the asexual blood stage of infection of Plasmodium by enabling the export of parasite proteins into the host red blood cell. This export is vital for parasite survival and …

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Optimization and Characterization of the Antimalarial Activity of N -Aryl Acetamides that are Susceptible to Mutations in ROM8 and CSC1

William Nguyen, Coralie Boulet, Madeline G. Dans, Katie Loi et autres

Abstract New antimalarials are needed due to the threat of emerging resistance against existing antimalarial therapies. A phenotypic screen uncovered the N-aryl acetamide class that inhibits the development of P. falciparum asexual ring-stage parasites. The structure–activity relationship of this class was investigated, …

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Review 1: "Prodrug Activation in Malaria Parasites Mediated by An Imported Erythrocyte Esterase, Acylpeptide Hydrolase (APEH)"

Paul R. Gilson

The reviewer found the study reliable. He applauded the novelty of a prodrug relying on activation of human enzymes however had suggestions for additional experiments to explain the mechanism and update of APEH by the parasites.

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Review of "Prodrug Activation in Malaria Parasites Mediated by An Imported Erythrocyte Esterase, Acylpeptide Hydrolase (APEH)"

Paul R. Gilson

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Aryl N-acetamide compounds exert antimalarial activity by acting as agonists of rhomboid protease Pf ROM8 and cation channel Pf CSC1

Coralie Boulet, Joyanta K. Modak, Natalie A. Counihan, Molly Parkyn Schneider et autres

Abstract With resistance to current frontline antimalarials spreading globally, new drug candidates need to be discovered to populate the antimalarial drug development pipeline. We previously screened the Medicines for Malaria Venture Pathogen Box for compounds that prevent Plasmodium falciparum parasites from exiting …

ch, au (code pays fourni par la source)

Author Correction: Aryl amino acetamides prevent Plasmodium falciparum ring development via targeting the lipid-transfer protein PfSTART1

Madeline G. Dans, Coralie Boulet, G. M. Watson, William Nguyen et autres

The original version of the Supplementary Information associated with this Article contained an error in Supplementary Fig. 7c and d, in which the concentrations of W-991 were provided on the x-axes in the wrong order. The HTML has been updated to include …

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Aryl amino acetamides prevent Plasmodium falciparum ring development via targeting the lipid-transfer protein PfSTART1

Madeline G. Dans, Coralie Boulet, G. M. Watson, William Nguyen et autres

With resistance to most antimalarials increasing, it is imperative that new drugs are developed. We previously identified an aryl acetamide compound, MMV006833 (M-833), that inhibited the ring-stage development of newly invaded merozoites. Here, we select parasites resistant to M-833 and identify mutations …

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Mitochondrial FtsZ in a chromophyte alga

PL Beech, Thao Nheu, Thomas F. Schultz, Shane Herbert et autres

Mitochondrial FtsZ in a chromophyte alga

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