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View article: A drug repurposing approach reveals targetable epigenetic pathways in Plasmodium vivax hypnozoites
A drug repurposing approach reveals targetable epigenetic pathways in Plasmodium vivax hypnozoites Open
Radical cure of Plasmodium vivax malaria must include elimination of quiescent ‘hypnozoite’ forms in the liver; however, the only FDA-approved treatments are contraindicated in many vulnerable populations. To identify new drugs and drug ta…
View article: Author response: A drug repurposing approach reveals targetable epigenetic pathways in Plasmodium vivax hypnozoites
Author response: A drug repurposing approach reveals targetable epigenetic pathways in Plasmodium vivax hypnozoites Open
View article: Differential <i>ex vivo</i> susceptibility of <i>Plasmodium malariae</i> and <i>Plasmodium falciparum</i> clinical isolates from Ghana and Mali to current and lead discovery candidate antimalarial drugs
Differential <i>ex vivo</i> susceptibility of <i>Plasmodium malariae</i> and <i>Plasmodium falciparum</i> clinical isolates from Ghana and Mali to current and lead discovery candidate antimalarial drugs Open
Non-falciparum species causing malaria in humans are considered neglected in the fight toward malaria elimination. Recent data highlight the increasing contribution of Plasmodium malariae to malaria morbidity and mortality. In this study, …
View article: Revisiting the Plasmodium falciparum druggable genome using predicted structures and data mining
Revisiting the Plasmodium falciparum druggable genome using predicted structures and data mining Open
Identification of novel drug targets is a key component of modern drug discovery. While antimalarial targets are often identified through the mechanism of action studies on phenotypically derived inhibitors, this method tends to be time- a…
View article: Correction: Chemoprevention of malaria with long-acting oral and injectable drugs: an updated target product profile
Correction: Chemoprevention of malaria with long-acting oral and injectable drugs: an updated target product profile Open
View article: Revisiting the Plasmodium falciparum druggable genome using predicted structures and data mining
Revisiting the Plasmodium falciparum druggable genome using predicted structures and data mining Open
The identification of novel drug targets for the purpose of designing small molecule inhibitors is key component to modern drug discovery. In malaria parasites, discoveries of antimalarial targets have primarily occurred retroactively by i…
View article: Chemoprevention of malaria with long-acting oral and injectable drugs: an updated target product profile
Chemoprevention of malaria with long-acting oral and injectable drugs: an updated target product profile Open
Malaria is preventable, but the burden of disease remains high with over 249 million cases and 608,000 deaths reported in 2022. Historically, the most important protective interventions have been vector control and chemopreventive medicine…
View article: Author response: A Drug Repurposing Approach Reveals Targetable Epigenetic Pathways in Plasmodium vivax Hypnozoites
Author response: A Drug Repurposing Approach Reveals Targetable Epigenetic Pathways in Plasmodium vivax Hypnozoites Open
View article: A drug repurposing approach reveals targetable epigenetic pathways in Plasmodium vivax hypnozoites
A drug repurposing approach reveals targetable epigenetic pathways in Plasmodium vivax hypnozoites Open
Radical cure of Plasmodium vivax malaria must include elimination of quiescent ‘hypnozoite’ forms in the liver; however, the only FDA-approved treatments are contraindicated in many vulnerable populations. To identify new drugs and drug ta…
View article: A Drug Repurposing Approach Reveals Targetable Epigenetic Pathways in Plasmodium vivax Hypnozoites
A Drug Repurposing Approach Reveals Targetable Epigenetic Pathways in Plasmodium vivax Hypnozoites Open
Radical cure of Plasmodium vivax malaria must include elimination of quiescent ‘hypnozoite’ forms in the liver; however, the only FDA-approved treatments are contraindicated in many vulnerable populations. To identify new drugs and drug ta…
View article: Optimization of Plasmodium vivax infection of colonized Amazonian Anopheles darlingi
Optimization of Plasmodium vivax infection of colonized Amazonian Anopheles darlingi Open
View article: Advances in malaria pharmacology and the online guide to MALARIA PHARMACOLOGY: IUPHAR review 38
Advances in malaria pharmacology and the online guide to MALARIA PHARMACOLOGY: IUPHAR review 38 Open
Antimalarial drug discovery has until recently been driven by high‐throughput phenotypic cellular screening, allowing millions of compounds to be assayed and delivering clinical drug candidates. In this review, we will focus on target‐base…
View article: Comparative Susceptibility of Plasmodium ovale and Plasmodium falciparum Field Isolates to Reference and Lead Candidate Antimalarial Drugs in Ghana
Comparative Susceptibility of Plasmodium ovale and Plasmodium falciparum Field Isolates to Reference and Lead Candidate Antimalarial Drugs in Ghana Open
Current malaria control and elimination tools such as drug treatments are not specifically targeting P.ovale . P. ovale can form hypnozoite and cause relapsing malaria. P. ovale is the third most dominant species in Africa and requires rad…
View article: Assessment of the drugability of initial malaria infection through miniaturized sporozoite assays and high-throughput screening
Assessment of the drugability of initial malaria infection through miniaturized sporozoite assays and high-throughput screening Open
The sporozoite stages of malaria parasites are the primary cause of infection of the vertebrate host and are targeted by (experimental) vaccines. Yet, little is known about their susceptibility to chemical intervention. Phenotypic high-thr…
View article: A Drug Repurposing Approach Reveals Targetable Epigenetic Pathways in <i>Plasmodium vivax</i> Hypnozoites
A Drug Repurposing Approach Reveals Targetable Epigenetic Pathways in <i>Plasmodium vivax</i> Hypnozoites Open
Radical cure of Plasmodium vivax malaria must include elimination of quiescent ‘hypnozoite’ forms in the liver; however, the only FDA-approved treatments are contraindicated in many vulnerable populations. To identify new drugs and drug ta…
View article: Plasmodium exoerythrocytic parasites redirect trafficking of human proteins to the parasitophorous vacuole
Plasmodium exoerythrocytic parasites redirect trafficking of human proteins to the parasitophorous vacuole Open
A bstract Changes in host cell morphology and transcription after apicomplexan parasite infection have long been noted, but there have been few studies of the functional consequences of host cell remodeling. Here we show, using time-depend…
View article: Plasmodium vivax latent liver infection is characterized by persistent hypnozoites, hypnozoite-derived schizonts, and time-dependent efficacy of primaquine
Plasmodium vivax latent liver infection is characterized by persistent hypnozoites, hypnozoite-derived schizonts, and time-dependent efficacy of primaquine Open
Plasmodium vivax is a malaria-causing pathogen that establishes a dormant form in the liver (the hypnozoite), which can activate weeks, months, or years after the primary infection to cause a relapse, characterized by secondary bloo…
View article: Preclinical characterization and target validation of the antimalarial pantothenamide MMV693183
Preclinical characterization and target validation of the antimalarial pantothenamide MMV693183 Open
Drug resistance and a dire lack of transmission-blocking antimalarials hamper malaria elimination. Here, we present the pantothenamide MMV693183 as a first-in-class acetyl-CoA synthetase (AcAS) inhibitor to enter preclinical development. O…
View article: Discovery and Preclinical Pharmacology of INE963, a Potent and Fast-Acting Blood-Stage Antimalarial with a High Barrier to Resistance and Potential for Single-Dose Cures in Uncomplicated Malaria
Discovery and Preclinical Pharmacology of INE963, a Potent and Fast-Acting Blood-Stage Antimalarial with a High Barrier to Resistance and Potential for Single-Dose Cures in Uncomplicated Malaria Open
A series of 5-aryl-2-amino-imidazothiadiazole (ITD) derivatives were identified by a phenotype-based high-throughput screening using a blood stage Plasmodium falciparum (Pf) growth inhibition assay. A lead optimization progra…
View article: <i>Ex Vivo Plasmodium malariae</i> Culture Method for Antimalarial Drugs Screen in the Field
<i>Ex Vivo Plasmodium malariae</i> Culture Method for Antimalarial Drugs Screen in the Field Open
In vitro and ex vivo cultivation of Plasmodium (P) falciparum has facilitated active research into the malaria parasite toward the quest for basic knowledge and the discovery of effective drug treatments. Such a drug d…
View article: Probing the distinct chemosensitivity of Plasmodium vivax liver stage parasites and demonstration of 8-aminoquinoline radical cure activity in vitro
Probing the distinct chemosensitivity of Plasmodium vivax liver stage parasites and demonstration of 8-aminoquinoline radical cure activity in vitro Open
View article: Prioritization of Molecular Targets for Antimalarial Drug Discovery
Prioritization of Molecular Targets for Antimalarial Drug Discovery Open
There is a shift in antimalarial drug discovery from phenotypic screening toward target-based approaches, as more potential drug targets are being validated in Plasmodium species. Given the high attrition rate and high cost of drug …
View article: Preclinical characterization and target validation of the antimalarial pantothenamide MMV693183
Preclinical characterization and target validation of the antimalarial pantothenamide MMV693183 Open
Drug resistance and a dire lack of transmission-blocking antimalarials hamper malaria elimination. Here, we present the pantothenamide MMV693183 as a first-in-class acetyl-CoA synthetase (ACS) inhibitor to enter preclinical development. Ou…
View article: MalDA, Accelerating Malaria Drug Discovery
MalDA, Accelerating Malaria Drug Discovery Open
View article: Chemoprotective Antimalarial Activity of P218 against Plasmodium falciparum: A Randomized, Placebo-Controlled Volunteer Infection Study
Chemoprotective Antimalarial Activity of P218 against Plasmodium falciparum: A Randomized, Placebo-Controlled Volunteer Infection Study Open
P218 is a highly selective dihydrofolate reductase inhibitor with potent in vitro activity against pyrimethamine-resistant Plasmodium falciparum . This single-center, randomized, double-blind, placebo-controlled phase Ib study evaluated P2…
View article: Probing the distinct chemosensitivity of Plasmodium vivax liver stage parasites and demonstration of 8-aminoquinoline radical cure activity in vitro
Probing the distinct chemosensitivity of Plasmodium vivax liver stage parasites and demonstration of 8-aminoquinoline radical cure activity in vitro Open
Improved control of malaria caused by Plasmodium vivax can be achieved with the discovery of new antimalarials with radical cure efficacy, including prevention of relapse caused by hypnozoites residing in the liver of vivax patients. We sc…
View article: Discovery of FNDR-20123, a histone deacetylase inhibitor for the treatment of Plasmodium falciparum malaria
Discovery of FNDR-20123, a histone deacetylase inhibitor for the treatment of Plasmodium falciparum malaria Open
View article: Plasmodium vivax liver stage assay platforms using Indian clinical isolates
Plasmodium vivax liver stage assay platforms using Indian clinical isolates Open
View article: An adaptable soft-mold embossing process for fabricating optically-accessible, microfeature-based culture systems and application toward liver stage antimalarial compound testing
An adaptable soft-mold embossing process for fabricating optically-accessible, microfeature-based culture systems and application toward liver stage antimalarial compound testing Open
An intrahepatic Plasmodium vivax liver stage schizont and hypnozoite develop in a microfeature-based, 384-well culture system for primary human hepatocytes.
View article: The IUPHAR/BPS Guide to PHARMACOLOGY in 2020: extending immunopharmacology content and introducing the IUPHAR/MMV Guide to MALARIA PHARMACOLOGY
The IUPHAR/BPS Guide to PHARMACOLOGY in 2020: extending immunopharmacology content and introducing the IUPHAR/MMV Guide to MALARIA PHARMACOLOGY Open
The IUPHAR/BPS Guide to PHARMACOLOGY (www.guidetopharmacology.org) is an open-access, expert-curated database of molecular interactions between ligands and their targets. We describe significant updates made over the seven releases during …