Search results for "Plasmodium"

showing 6 items of 86 documents

Identification, Characterization and Synthesis of Natural Parasitic Cysteine Protease Inhibitors – More Potent Falcitidin Analogs

2021

ABSTRACTProtease inhibitors represent a promising therapeutic option for the treatment of parasitic diseases such as malaria and human African trypanosomiasis. Falcitidin was the first member of a new class of inhibitors of falcipain-2, a cysteine protease of the malaria parasite Plasmodium falciparum. Using a metabolomics dataset of 25 Chitinophaga strains for molecular networking enabled identification of over 30 natural analogs of falcitidin. Based on MS/MS spectra, they vary in their amino acid chain length, sequence, acyl residue, and C-terminal functionalization; therefore, they were grouped into the four falcitidin peptide families A-D. The isolation, characterization and absolute st…

chemistry.chemical_classificationProteasesProteasebiologyIn silicomedicine.medical_treatmentPlasmodium falciparumPeptidebiology.organism_classificationCysteine proteasePentapeptide repeatAmino acidBiochemistrychemistrymedicine
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Data from: Early Plasmodium-induced inflammation does not accelerate aging in mice

2018

Aging is associated with a decline of performance leading to reduced reproductive output and survival. While the antagonistic pleiotropy theory of aging has attracted considerable attention, the molecular/physiological functions underlying the early-life benefits/late-life costs paradigm remain elusive. We tested the hypothesis that while early activation of the inflammatory response confers benefits in terms of protection against infection, it also incurs costs in terms of reduced reproductive output at old age, and shortened longevity. We infected mice with the malaria parasite Plasmodium yoelii and increased the inflammatory response using an anti-IL-10 receptor antibody treatment. We qu…

medicine and health careLife SciencesMedicineAntagonistic pleiotropyPlasmodium yoelii
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Data from: Continental-scale patterns of pathogen prevalence: a case study on the corncrake

2014

Pathogen infections can represent a substantial threat to wild populations, especially those already limited in size. To determine how much variation in the pathogens observed among fragmented populations is caused by ecological factors, one needs to examine systems where host genetic diversity is consistent among the populations, thus controlling for any potentially confounding genetic effects. Here, we report geographic variation in haemosporidian infection among European populations of corncrake. This species now occurs in fragmented populations, but there is little genetic structure and equally high levels of genetic diversity among these populations. We observed a longitudinal gradient…

medicine and health carePlasmodiumhaemosporidian parasitesHaemoproteusparasite transmissionLeucocytozoonCrex CrexLife SciencesMedicineAvian malariacorncrake
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Synthesis and Molecular Modeling Studies of Derivatives of a Highly Potent Peptidomimetic Vinyl Ester as Falcipain-2 Inhibitors

2012

Herein we report the synthesis of a set of constrained peptidomimetics endowed with an electrophilic vinyl ester warhead and structurally related to a previously identified lead compound, a potent and irreversible inhibitor of falcipain-2 (FP-2). FP-2 is the main hemoglobinase of the malaria parasite P. falciparum. The new compounds were evaluated for their inhibition against FP-2, and the results were rationalized on the basis of docking experiments. These studies underscore the pivotal role of both the ester function at the P1' site and the trifluoromethyl group of the P3 side chain in determining the correct orientation of the Michael acceptor warhead in the catalytic site, and as a cons…

peptidomimeticdMolecular modelPeptidomimeticStereochemistryPlasmodium falciparumVinyl esterBiochemistrycysteine proteasesfalcipain-2 inhibitorsAntimalarialschemistry.chemical_compoundCatalytic DomainDrug DiscoverySide chainHumansEnzyme InhibitorsMalaria FalciparumGeneral Pharmacology Toxicology and PharmaceuticsPharmacologyTrifluoromethylOrganic Chemistrydocking studiescysteine proteases; peptidomimeticd; docking studies; falcipain-2 inhibitorsMolecular Docking SimulationCysteine EndopeptidaseschemistryDocking (molecular)Michael reactionMolecular MedicinePeptidomimeticsLead compoundChemMedChem
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Development of Henneguya zschokkei (Myxozoa: Myxosporea) actinospores in oligochaetes and plasmodia in whitefish Coregonous lavaretus

2013

The aim of this study was to describe the life cycle of H. zschokkei by observing the development of actinospores in oligochaete and the morphological development of H. zschokkei cysts in whitefish. Laboratory observation of seasonal occurrence of actinospores sampled from oligochaetes from RTKL Tervo Fish Farm revealed 6 types of actinospores from collective groups of Triactinomyxon, Raabeia and Aurantiactinomyxon in 2010, and 3 types of actinospores in 2011. Both years showed similar patterns with the release of actinospores peaking in both summer (June and July) and winter (January and February) times. The infection experiment was not successful in infecting Coregonus lavaretus with myxo…

plasmodium-kystivuodenaikaisuusvuodenajatactinosporespiimäsiikasiikaHenneguya zschokkeiseasonal occurenceCoregonus lavaretusrakkoloisioplasmodium cystkehittyminenaktinospoori
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Data from: Impact of host nutritional status on infection dynamics and parasite virulence in a bird-malaria system

2013

1. Host resources can drive the optimal parasite exploitation strategy by offering a good or a poor environment to pathogens. Hosts living in resource-rich habitats might offer a favourable environment to developing parasites because they provide a wealth of resources. However, hosts living in resource-rich habitats might afford a higher investment into costly immune defences providing an effective barrier against infection. Understanding how parasites can adapt to hosts living in habitats of different quality is a major challenge in the light of the current human-driven environmental changes. 2. We studied the role of nutritional resources as a source of phenotypic variation in host exploi…

virulencemedicine and health carenutritionenvironmental variationPlasmodium relictumavian malariaLife SciencesMedicinehost-parasite interaction
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