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The Open Access Malaria Box: A Drug Discovery Catalyst for Neglected Diseases
TLDR
A collection of 400 chemotypes, selected based on their drug-like properties and the others as molecular probes, are assembled, termed the Malaria Box, and can now be requested as a pharmacological test set by malaria biologists, but importantly by groups working on related parasites. Expand
Open Source Drug Discovery with the Malaria Box Compound Collection for Neglected Diseases and Beyond
TLDR
The results reveal the immense potential for translating the dispersed expertise in biological assays involving human pathogens into drug discovery starting points, by providing open access to new families of molecules, and emphasize how a small additional investment made to help acquire and distribute compounds, and sharing the data, can catalyze drug discovery for dozens of different indications. Expand
Antimalarial drug discovery – the path towards eradication
TLDR
The current mainstay treatments alongside a selection of emerging new clinical molecules from the portfolio of Medicines for Malaria Venture (MMV) and their partners are highlighted. Expand
Identification of Cryptosporidium parvum Active Chemical Series by Repurposing the Open Access Malaria Box
TLDR
The utility of the Open Access Malaria Box as a source of both potential leads for drug development and chemical probes to elucidate basic biological processes in C. parvum and other apicomplexan parasites is illustrated. Expand
Reactive Oxygen Species-Induced Activation of p90 Ribosomal S6 Kinase Prolongs Cardiac Repolarization Through Inhibiting Outward K+ Channel Activity
TLDR
The findings indicate that p90RSK activation is critical for reactive oxygen species-mediated inhibition of voltage-gated K+ channel activity and leads to prolongation of cardiac repolarization. Expand
Repurposing the Open Access Malaria Box To Discover Potent Inhibitors of Toxoplasma gondii and Entamoeba histolytica
TLDR
Seven anti-Toxoplasma compounds identified in this study belong to scaffold types different from those of currently used drugs, underscoring their novelty and potential as starting points for the development of new antitoxoplasmosis drugs with novel modes of action. Expand
Malaria in South America: a drug discovery perspective
TLDR
The contribution of groups in the South American continent to the research and development of new medicines over the last decade is reviewed, including endemicity, geographical distribution, treatment, drug-resistance and diagnosis. Expand
Repurposing of the Open Access Malaria Box for Kinetoplastid Diseases Identifies Novel Active Scaffolds against Trypanosomatids
TLDR
The screening of the Malaria Box and triaging of the identified hits against kinetoplastids responsible for human African trypanosomiasis, Chagas disease, and visceral leishmaniasis are described and a collaborative model used as a way to accelerate the discovery process discussed. Expand
Orally Active Antischistosomal Early Leads Identified from the Open Access Malaria Box
TLDR
The two candidates identified by investigating the MMV malaria box are characterized by good pharmacokinetic profiles, low cytotoxic potential and easy chemistry and therefore offer an excellent starting point for antischistosomal drug discovery and development. Expand
Activities of N,N′-Diarylurea MMV665852 Analogs against Schistosoma mansoni
TLDR
Several analogs of the N,N′-diarylurea MMV665852 had high efficacy against S. mansoni in vitro and favorable physicochemical properties for permeation through the intestinal wall, and further investigations should focus on identifying compounds with improved solubility and pharmacokinetic properties. Expand
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