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Open Source Drug Discovery with the Malaria Box Compound Collection for Neglected Diseases and Beyond
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.
Orally Active Antischistosomal Early Leads Identified from the Open Access Malaria Box
- Katrin Ingram-Sieber, Noemi Cowan, J. Keiser
- Medicine, BiologyPLoS neglected tropical diseases
- 1 January 2014
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.
Activities of N,N′-Diarylurea MMV665852 Analogs against Schistosoma mansoni
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.
Repurposing of anticancer drugs: in vitro and in vivo activities against Schistosoma mansoni
This study has confirmed that oncology drugs possess antischistosomal activity, and there is space for further investigation, including elucidation of the mechanisms of action of schistosome-active cancer drugs, application of different treatment courses, and structure-activity relationship studies for improving drug potency.
Activity of Praziquantel Enantiomers and Main Metabolites against Schistosoma mansoni
- Isabel Meister, Katrin Ingram-Sieber, J. Keiser
- BiologyAntimicrobial Agents and Chemotherapy
- 30 June 2014
Investigation of the in vitro activities of PZQ and its main metabolites confirmed that R-PZQ is the main effector molecule, while S-PzQ and the metabolites do not play a significant role in the antischistosomal properties of PzQ.
Elucidation of the in vitro and in vivo activities of bridged 1,2,4-trioxolanes, bridged 1,2,4,5-tetraoxanes, tricyclic monoperoxides, silyl peroxides, and hydroxylamine derivatives against…
Evaluation of an FDA approved library against laboratory models of human intestinal nematode infections
- J. Keiser, G. Panic, R. Adelfio, Noemi Cowan, M. Vargas, Ivan Scandale
- Biology, MedicineParasites & Vectors
- 1 July 2016
Drug screening on the larval stages of intestinal parasitic nematodes is feasible using small libraries and important given the empty drug discovery and development pipeline for STH infections.
Treatment of human and livestock helminth infections in a mobile pastoralist setting at Lake Chad: Attitudes to health and analysis of active pharmaceutical ingredients of locally available…
Approved oncology drugs lack in vivo activity against Trichuris muris despite in vitro activity
A set of FDA-approved oncology drugs for activity against Trichuris muris is studied since targets relevant to cancer therapy might have a function in helminth biology and drug discovery against STH should be strengthened.
Exposure of Heligmosomoides polygyrus and Trichuris muris to albendazole, albendazole sulfoxide, mebendazole and oxantel pamoate in vitro and in vivo to elucidate the pathway of drug entry into these…