Jana Held
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View article: Complete attenuation of Plasmodium falciparum sporozoites by atovaquone–proguanil
Complete attenuation of Plasmodium falciparum sporozoites by atovaquone–proguanil Open
To develop a Plasmodium falciparum (Pf) vaccine that precludes replication inside the host for improved vaccine safety, we tested chemo-attenuation (CVac) of sporozoites (SPZ) with atovaquone–proguanil (AP). In mice, P. berghei sporozoites…
View article: Exploration of Fluorinated Peptoid‐Based Histone Deacetylase Inhibitors as Dual‐Stage Antiplasmodial Agents
Exploration of Fluorinated Peptoid‐Based Histone Deacetylase Inhibitors as Dual‐Stage Antiplasmodial Agents Open
The antiplasmodial properties of a series of fluorinated peptoid‐capped histone deacetylase inhibitors (HDACi) were investigated against asexual blood stages of the drug‐sensitive 3D7 and drug‐resistant Dd2 strains of Plasmodium falciparum…
View article: Exploration of fluorinated peptoid-based histone deacetylase inhibitors as dual-stage antiplasmodial agents
Exploration of fluorinated peptoid-based histone deacetylase inhibitors as dual-stage antiplasmodial agents Open
In this study, we investigated the antiplasmodial properties of a series of fluorinated peptoid-capped histone deacetylase inhibitors (HDACi) against asexual blood stages of the drug-sensitive 3D7 and drug-resistant Dd2 strains of Plasmodi…
View article: Genomic Deletion of PfHRP2 and PfHRP3 Antigens in <i>Plasmodium falciparum</i> Strains, Ethiopia, 2009
Genomic Deletion of PfHRP2 and PfHRP3 Antigens in <i>Plasmodium falciparum</i> Strains, Ethiopia, 2009 Open
Plasmodium falciparum strains lacking P. falciparum histidine-rich protein 2 (PfHRP2) and PfHRP3 threaten malaria rapid test reliability. We show that pfhrp2/pfhrp3-deleted parasites circulated in Ethiopia as early as 2009, before widespre…
View article: No Evidence of Piperaquine Resistance in Southeast Nigeria
No Evidence of Piperaquine Resistance in Southeast Nigeria Open
Artemisinin-based combination therapies (ACTs) are currently the first-line treatment for uncomplicated malaria. However, ACTs are being threatened by the emergence of Plasmodium falciparum strains resistant to artemisinins as well as thei…
View article: Exploration of fluorinated peptoid-based histone deacetylase inhibitors as dual-stage antiplasmodial agents
Exploration of fluorinated peptoid-based histone deacetylase inhibitors as dual-stage antiplasmodial agents Open
this study, we investigated the antiplasmodial properties of a series of fluorinated peptoid-capped histone deacetylase inhibitors (HDACi) against the drug-sensitive 3D7 and drug-resistant Dd2 strains of Plasmodium falciparum, as well as t…
View article: Wolbachia bacteria in Mansonella perstans isolates from patients infected in different geographical areas: a pilot study from the ESCMID Study Group for Clinical Parasitology
Wolbachia bacteria in Mansonella perstans isolates from patients infected in different geographical areas: a pilot study from the ESCMID Study Group for Clinical Parasitology Open
Background Mansonella perstans is a vector-borne filarial parasite widely endemic in sub-Saharan Africa, with sporadic cases in Latin America. Infection is often overlooked; treatment is not standardized, and effectiveness of common regime…
View article: Antiplasmodial Activity of a New Chemotype of Croton sylvaticus Hochst. Ex C. Krauss Essential Oil
Antiplasmodial Activity of a New Chemotype of Croton sylvaticus Hochst. Ex C. Krauss Essential Oil Open
Croton sylvaticus, a tropical African plant, is traditionally used to treat several diseases, including fever, inflammation, and malaria. Essential oils (EOs) from the plant’s leaves, roots, and trunk bark were obtained by hydrodistillatio…
View article: Automated total nucleic acid extraction with magnetic beads for the detection of Plasmodium falciparum in large study cohorts
Automated total nucleic acid extraction with magnetic beads for the detection of Plasmodium falciparum in large study cohorts Open
Background Molecular methods play an important role in clinical trials assessing anti-malarial drugs and vaccines, as well as in epidemiological studies aimed at detecting Plasmodium species, especially when dealing with large sample sizes…
View article: Towards Novel Antiplasmodial Agents—Design, Synthesis and Antimalarial Activity of Second-Generation β-Carboline/Chloroquine Hybrids
Towards Novel Antiplasmodial Agents—Design, Synthesis and Antimalarial Activity of Second-Generation β-Carboline/Chloroquine Hybrids Open
As the resistance of Plasmodium to the existing antimalarials increases, there is a crucial need to expand the antimalarial drug pipeline. We recently identified potent antimalarial compounds, namely harmiquins, hybrids derived from the β-…
View article: Multicomponent syntheses enable the discovery of novel quisinostat-derived chemotypes as histone deacetylase inhibitors
Multicomponent syntheses enable the discovery of novel quisinostat-derived chemotypes as histone deacetylase inhibitors Open
In this study, we synthesized and evaluated novel histone deacetylase (HDAC) inhibitors derived from the clinical candidate quisinostat. A library of 16 compounds categorized in three novel chemotypes was rapidly generated using multicompo…
View article: Multicomponent Syntheses Enable the Discovery of Novel Quisinostat-Derived Chemotypes as Histone Deacetylase Inhibitors
Multicomponent Syntheses Enable the Discovery of Novel Quisinostat-Derived Chemotypes as Histone Deacetylase Inhibitors Open
Epigenetic drug targets have become an important focus in drug discovery. One of the key mechanisms in epigenetics is the acetylation and deacetylation of histone proteins. In this study, we synthesized and evaluated novel histone deacetyl…
View article: Targeting the <i>Plasmodium falciparum</i> IspE Enzyme
Targeting the <i>Plasmodium falciparum</i> IspE Enzyme Open
The enzyme IspE in Plasmodium falciparum is considered an attractive drug target, as it is essential for parasite survival and is absent in the human proteome. Yet it still has not been addressed by a small-molecule inhibitor. In this stud…
View article: Evolution of Pfdhps and Pfdhfr mutations before and after adopting seasonal malaria chemoprevention in Nanoro, Burkina Faso
Evolution of Pfdhps and Pfdhfr mutations before and after adopting seasonal malaria chemoprevention in Nanoro, Burkina Faso Open
Seasonal Malaria Chemoprevention consisting of monthly administration of amodiaquine/sulfadoxine-pyrimethamine to children aged 3–59 months during the transmission season could promote SP-resistance. Mutations in dihydrofolate reductase ( …
View article: Multicomponent Syntheses Enable the Discovery of Novel Quisinostat-Derived Chemotypes as Histone Deacetylase Inhibitors
Multicomponent Syntheses Enable the Discovery of Novel Quisinostat-Derived Chemotypes as Histone Deacetylase Inhibitors Open
Epigenetic drug targets have become an important focus in drug discovery. One of the key mechanisms in epigenetics is the acetylation and deacetylation of histone proteins. In this study, we synthesized and evaluated novel histone deacetyl…
View article: Development of peptoid-based heteroaryl-decorated histone deacetylase (HDAC) inhibitors with dual-stage antiplasmodial activity
Development of peptoid-based heteroaryl-decorated histone deacetylase (HDAC) inhibitors with dual-stage antiplasmodial activity Open
Dynamics of epigenetic modifications such as acetylation and deacetylation of histone proteins have been shown to be crucial for the life cycle development and survival of Plasmodium falciparum, the deadliest malaria parasite. In this stud…
View article: Development of Peptoid-Based Heteroaryl-Decorated Histone Deacetylase (HDAC) Inhibitors with Dual-Stage Antiplasmodial Activity
Development of Peptoid-Based Heteroaryl-Decorated Histone Deacetylase (HDAC) Inhibitors with Dual-Stage Antiplasmodial Activity Open
Dynamics of epigenetic modifications such as acetylation and deacetylation of histone proteins have been shown to be crucial for the life cycle development and survival of Plasmodium falciparum, the deadliest malaria parasite. In this stud…
View article: Genetic diversity of Plasmodium malariae in sub-Saharan Africa: a two-marker genotyping approach for molecular epidemiological studies
Genetic diversity of Plasmodium malariae in sub-Saharan Africa: a two-marker genotyping approach for molecular epidemiological studies Open
Introduction Plasmodium malariae is the most common non-falciparum species in sub-Saharan Africa. Despite this, data on its genetic diversity is scarce. Therefore, we aimed to establish a P. malariae genotyping approach based on size polym…
View article: Design, Synthesis, Antitumor, and Antiplasmodial Evaluation of New 7-Chloroquinoline–Benzimidazole Hybrids
Design, Synthesis, Antitumor, and Antiplasmodial Evaluation of New 7-Chloroquinoline–Benzimidazole Hybrids Open
Newly synthesized 7-chloro-4-aminoquinoline–benzimidazole hybrids were characterized by NMR and elemental analysis. Compounds were tested for their effects on the growth of the non-tumor cell line MRC-5 (human fetal lung fibroblasts) and c…
View article: Development of Peptoid-Based Heteroaryl-Decorated Histone Deacetylase (HDAC) Inhibitors with Dual-Stage Antiplasmodial Activity
Development of Peptoid-Based Heteroaryl-Decorated Histone Deacetylase (HDAC) Inhibitors with Dual-Stage Antiplasmodial Activity Open
Malaria remains a significant global health challenge, causing approximately 608,000 deaths and over 249 million infections in 2022. With the rise of resistance to current chemotherapies, including artemisinin-based combination therapies (…
View article: Evaluating Malaria Rapid Diagnostic Tests and Microscopy for Detecting Plasmodium Infection and Status of Plasmodium falciparum Histidine-Rich Protein 2/3 Gene Deletions in Southeastern Nigeria
Evaluating Malaria Rapid Diagnostic Tests and Microscopy for Detecting Plasmodium Infection and Status of Plasmodium falciparum Histidine-Rich Protein 2/3 Gene Deletions in Southeastern Nigeria Open
Delays in malaria diagnosis increase treatment failures and deaths. In endemic regions, standard diagnostic methods are microscopy and malaria rapid diagnostic tests (mRDTs) detecting Plasmodium falciparum histidine-rich protein 2/3 (PFHRP…
View article: Functionalization of Chlorotonils: Dehalogenil as Promising Lead Compound for In Vivo Application
Functionalization of Chlorotonils: Dehalogenil as Promising Lead Compound for In Vivo Application Open
The natural product chlorotonil displays high potency against multidrug‐resistant Gram‐positive bacteria and Plasmodium falciparum . Yet, its scaffold is characterized by low solubility and oral bioavailability, but progress was recently m…
View article: Dynamics of Plasmodium species and genotype diversity in adults with asymptomatic infection in Gabon
Dynamics of Plasmodium species and genotype diversity in adults with asymptomatic infection in Gabon Open
Our results reveal complex intra-host dynamics of P. falciparum genotypes and Plasmodium species and underscore the importance of serial sampling in clinical trials for antimalarial drugs with asymptomatically P. falciparum-infected indivi…
View article: High Target Homology Does Not Guarantee Inhibition: Aminothiazoles Emerge as Inhibitors of <i>Plasmodium falciparum</i>
High Target Homology Does Not Guarantee Inhibition: Aminothiazoles Emerge as Inhibitors of <i>Plasmodium falciparum</i> Open
In this study, we identified three novel compound classes with potent activity against Plasmodium falciparum, the most dangerous human malarial parasite. Resistance of this pathogen to known drugs is increasing, and compounds with differen…
View article: PA-382 Trends in sulfadoxine-pyrimethamine resistance molecular markers among plasmodium falciparum isolates before and after adopting seasonal malaria chemoprevention in Nanoro, Burkina Faso
PA-382 Trends in sulfadoxine-pyrimethamine resistance molecular markers among plasmodium falciparum isolates before and after adopting seasonal malaria chemoprevention in Nanoro, Burkina Faso Open
Background Despite various efforts to control malaria among children, the disease remains a leading cause of morbidity and mortality worldwide. In the Sahel region, including Burkina Faso, seasonal malaria chemoprevention (SMC) using Sulfa…
View article: Synthesis, antiproliferative and antiplasmodial evaluation of new chloroquine and mefloquine-based harmiquins
Synthesis, antiproliferative and antiplasmodial evaluation of new chloroquine and mefloquine-based harmiquins Open
Here we present the synthesis and evaluation of the biological activity of new hybrid compounds, ureido-type (UT) harmiquins, based on chloroquine (CQ) or mefloquine (MQ) scaffolds and β-carboline alkaloid harmine against cancer cell lines…
View article: Efficacy and safety of ivermectin for the treatment of Plasmodium falciparum infections in asymptomatic male and female Gabonese adults – a pilot randomized, double-blind, placebo-controlled single-centre phase Ib/IIa clinical trial
Efficacy and safety of ivermectin for the treatment of Plasmodium falciparum infections in asymptomatic male and female Gabonese adults – a pilot randomized, double-blind, placebo-controlled single-centre phase Ib/IIa clinical trial Open
This study was funded by the Centre de Recherches Médicales de Lambaréné and the Centre for Tropical Medicine of the Bernhard Nocht Institute for Tropical Medicine.
View article: CCDC 2129280: Experimental Crystal Structure Determination
CCDC 2129280: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 2129279: Experimental Crystal Structure Determination
CCDC 2129279: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …