International Journal for Parasitology: Drugs and Drug Resistance This is an RSS file. You can use it to subscribe to this data in your favourite RSS reader or to display this data on your own website or blog.

High-throughput screen of drug repurposing library identifies inhibitors of Sarcocystis neurona growth
Publication date: Available online 16 February 2018 Source:International Journal for Parasitology: Drugs and Drug Resistance Author(s): Gregory D. Bowden, Kirkwood M. Land, Roberta M. O'Connor, Heather M. Fritz The apicomplexan parasite Sarcocystis neurona is the primary etiologic agent of equine protozoal myeloencephalitis (EPM), a serious neurologic disease of horses. Many horses in the U.S. are at risk of developing EPM; approximately 50% of all horses in the U.S. have been exposed to S. neurona and treatments for EPM are 60–70% effective. Advancement of treatment requires new technology to identify new drugs fo...
Source: International Journal for Parasitology: Drugs and Drug Resistance - February 17, 2018 Category: Parasitology Source Type: research

Structural model, functional modulation by ivermectin and tissue localization of Haemonchus contortus P-glycoprotein-13
Publication date: Available online 15 February 2018 Source:International Journal for Parasitology: Drugs and Drug Resistance Author(s): Marion David, Chantal Lebrun, Thomas Duguet, Franck Talmont, Robin Beech, Stéphane Orlowski, François André, Roger K. Prichard, Anne Lespine Haemonchus contortus, one of the most economically important parasites of small ruminants, has become resistant to the anthelmintic ivermectin. Deciphering the role of P-glycoproteins in ivermectin resistance is desirable for understanding and overcoming this resistance. In the model nematode, Caenorhabditis elegans, P-glycoprotein-13 is...
Source: International Journal for Parasitology: Drugs and Drug Resistance - February 15, 2018 Category: Parasitology Source Type: research

Profiling G protein-coupled receptors of Fasciola hepatica identifies orphan rhodopsins unique to phylum Platyhelminthes
This study facilitates GPCR research in the liver fluke, Fasciola hepatica, by generating the first profile of GPCRs from the F. hepatica genome. Our dataset describes 147 high confidence GPCRs, representing the largest cohort of GPCRs, and the most complete set of in silico ligand-receptor predictions, yet reported in any parasitic helminth. All GPCRs fall within the established GRAFS nomenclature; comprising three glutamate, 135 rhodopsin, two adhesion, five frizzled, one smoothened, and one secretin GPCR. Stringent annotation pipelines identified 18 highly diverged rhodopsins in F. hepatica that maintained core rhodopsi...
Source: International Journal for Parasitology: Drugs and Drug Resistance - February 6, 2018 Category: Parasitology Source Type: research

In vitro and in vivo pharmacodynamics of three novel antileishmanial lead series
Conclusions The new lead series were shown to have cidal pharmacodynamic activity. The absence of cross-resistance with any of the current antileishmanial drugs opens possibilities for combination treatment to reduce the likelihood of treatment failures and drug resistance. Graphical abstract (Source: International Journal for Parasitology: Drugs and Drug Resistance)
Source: International Journal for Parasitology: Drugs and Drug Resistance - February 1, 2018 Category: Parasitology Source Type: research

Synthesis of aminophenylhydroxamate and aminobenzylhydroxamate derivatives and in vitro screening for antiparasitic and histone deacetylase inhibitory activity
Publication date: Available online 31 January 2018 Source:International Journal for Parasitology: Drugs and Drug Resistance Author(s): C. Loeuillet, B. Touquet, B. Oury, N. Eddaikra, J.L. Pons, J.F. Guichou, G. Labesse, D. Sereno A series of aminophenylhydroxamates and aminobenzylhydroxamates were synthesized and screened for their antiparasitic activity against Leishmania, Trypanosoma, and Toxoplasma. Their anti-histone deacetylase (HDAC) potency was determined. Moderate to no antileishmanial or antitrypanosomal activity was found (IC50 > 10 μM) that contrast with the highly efficient anti-Toxoplas...
Source: International Journal for Parasitology: Drugs and Drug Resistance - February 1, 2018 Category: Parasitology Source Type: research

P-glycoprotein-9 and macrocyclic lactone resistance status in selected strains of the ovine gastrointestinal nematode, Teladorsagia circumcincta
Publication date: Available online 31 January 2018 Source:International Journal for Parasitology: Drugs and Drug Resistance Author(s): Frank Turnbull, Nicholas N. Jonsson, Fiona Kenyon, Philip J. Skuce, Stewart A. Bisset The Teladorsagia circumcincta P-glycoprotein-9 (Tci-pgp-9) gene has previously been implicated in multiple-anthelmintic resistance in this parasite. Here we further characterise genetic diversity in Tci-pgp-9 and its possible role in ivermectin (IVM) and multi-drug resistance using two UK field isolates of T. circumcincta, one susceptible to anthelmintics (MTci2) and the other resistant to most avai...
Source: International Journal for Parasitology: Drugs and Drug Resistance - February 1, 2018 Category: Parasitology Source Type: research

Metabolism of albendazole, ricobendazole and flubendazole in Haemonchus contortus adults: Sex differences, resistance-related differences and the identification of new metabolites
Publication date: Available online 31 January 2018 Source:International Journal for Parasitology: Drugs and Drug Resistance Author(s): Lucie Raisová Stuchlíková, Petra Matoušková, Ivan Vokřál, Jiří Lamka, Barbora Szotáková, Anna Sečkařová, Diana Dimunová, Linh Thuy Nguyen, Marián Várady, Lenka Skálová Haemonchus contortus (family Trichostrongylidae, Nematoda), a hematophagous gastrointestinal parasite found in small ruminants, has a great ability to develop resistance to anthelmintic drugs. We studied the biotransformation of the three benzimidazole anthelmintics: albendazole (ABZ), ricobenda...
Source: International Journal for Parasitology: Drugs and Drug Resistance - February 1, 2018 Category: Parasitology Source Type: research

Discovery of ebselen as an inhibitor of Cryptosporidium parvum glucose-6-phosphate isomerase (CpGPI) by high-throughput screening of existing drugs
In this study, we characterized the primary biochemical features of the C. parvum glucose-6-phosphate isomerase (CpGPI) and determined its Michaelis constant towards fructose-6-phosphate (K m = 0.309 mM, V max = 31.72 nmol/μg/min). We also discovered that ebselen, an organoselenium drug, was a selective inhibitor of CpGPI by high-throughput screening of 1200 known drugs. Ebselen acted on CpGPI as an allosteric noncompetitive inhibitor (IC50 = 8.33 μM; K i = 36.33 μM), while complete inhibition of CpGPI activity was not achieved. Ebselen could also inhibit the growth of C. parvum in vitro (EC50 ...
Source: International Journal for Parasitology: Drugs and Drug Resistance - January 31, 2018 Category: Parasitology Source Type: research

The optimal timing of post-treatment sampling for the assessment of anthelminthic drug efficacy against Ascaris infections in humans
Publication date: Available online 13 January 2018 Source:International Journal for Parasitology: Drugs and Drug Resistance Author(s): Bruno Levecke, Alice V. Easton, Piet Cools, Marco Albonico, Shaali Ame, John Gilleard, Jennifer Keiser, Antonio Montresor, Roger Prichard, Johnny Vlaminck, Jozef Vercruysse The egg reduction rate (ERR) is the current standard mean to assess the efficacy of drugs against human soil-transmitted helminths (STHs; Ascaris lumbricoides, Trichuris trichiura and hookworm). Although the timing of post-treatment sampling is pivotal for a readily interpretation of drug efficacy, there is ...
Source: International Journal for Parasitology: Drugs and Drug Resistance - January 14, 2018 Category: Parasitology Source Type: research

Potential role of Plasmodium falciparum exported protein 1 in the chloroquine mode of action
Publication date: Available online 27 December 2017 Source:International Journal for Parasitology: Drugs and Drug Resistance Author(s): Andreas Martin Lisewski, Joel Patrick Quiros, Monica Mittal, Nagireddy Putluri, Arun Sreekumar, Jesper Z. Haeggström, Olivier Lichtarge In the human malaria parasite Plasmodium falciparum, membrane glutathione S-transferases (GST) have recently emerged as potential cellular detoxifying units and as drug target candidates with the artemisinin (ART) class of antimalarials inhibiting their activity at single-digit nanomolar potency when activated by iron sources such as cytotoxic he...
Source: International Journal for Parasitology: Drugs and Drug Resistance - December 28, 2017 Category: Parasitology Source Type: research

Motility in the L3 stage is a poor phenotype for detecting and measuring resistance to avermectin/milbemycin drugs in gastrointestinal nematodes of livestock
Publication date: Available online 18 December 2017 Source:International Journal for Parasitology: Drugs and Drug Resistance Author(s): Melissa M. George, Lorraine Lopez-Soberal, Bob E. Storey, Sue B. Howell, Ray M. Kaplan Motility is a commonly used in vitro phenotype for assessing anthelmintic activity of candidate compounds, and for detecting anthelmintic resistance in nematodes. Third-stage larvae (L3) of parasitic nematodes are commonly used in motility-based assays because L3 are simple to obtain and can remain viable in storage for extended periods. To improve the measurement of motility of microscopic stages...
Source: International Journal for Parasitology: Drugs and Drug Resistance - December 19, 2017 Category: Parasitology Source Type: research

Monepantel is a non-competitive antagonist of nicotinic acetylcholine receptors from Ascaris suum and Oesophagostomum dentatum
Publication date: Available online 16 December 2017 Source:International Journal for Parasitology: Drugs and Drug Resistance Author(s): Melanie Abongwa, Djordje S. Marjanovic, James G. Tipton, Fudan Zheng, Richard J. Martin, Sasa M. Trailovic, Alan P. Robertson Zolvix® is a recently introduced anthelmintic drench containing monepantel as the active ingredient. Monepantel is a positive allosteric modulator of DEG-3/DES-2 type nicotinic acetylcholine receptors (nAChRs) in several nematode species. The drug has been reported to produce hypercontraction of Caenorhabditis elegans and Haemonchus contortus somatic muscl...
Source: International Journal for Parasitology: Drugs and Drug Resistance - December 17, 2017 Category: Parasitology Source Type: research

An automated high-throughput system for phenotypic screening of chemical libraries on C. elegans and parasitic nematodes
Publication date: Available online 2 December 2017 Source:International Journal for Parasitology: Drugs and Drug Resistance Author(s): Frederick A. Partridge, Anwen E. Brown, Steven D. Buckingham, Nicky J. Willis, Graham M. Wynne, Ruth Forman, Kathryn J. Else, Alison A. Morrison, Jacqueline B. Matthews, Angela J. Russell, David A. Lomas, David B. Sattelle Parasitic nematodes infect hundreds of millions of people and farmed livestock. Further, plant parasitic nematodes result in major crop damage. The pipeline of therapeutic compounds is limited and parasite resistance to the existing anthelmintic compounds is...
Source: International Journal for Parasitology: Drugs and Drug Resistance - December 3, 2017 Category: Parasitology Source Type: research

Disulfiram as a novel inactivator of Giardia lamblia triosephosphate isomerase with antigiardial potential
Publication date: December 2017 Source:International Journal for Parasitology: Drugs and Drug Resistance, Volume 7, Issue 3 Author(s): Adriana Castillo-Villanueva, Yadira Rufino-González, Sara-Teresa Méndez, Angélica Torres-Arroyo, Martha Ponce-Macotela, Mario Noé Martínez-Gordillo, Horacio Reyes-Vivas, Jesús Oria-Hernández Giardiasis, the infestation of the intestinal tract by Giardia lamblia, is one of the most prevalent parasitosis worldwide. Even though effective therapies exist for it, the problems associated with its use indicate that new therapeutic options are needed. It has been shown that disulfi...
Source: International Journal for Parasitology: Drugs and Drug Resistance - December 2, 2017 Category: Parasitology Source Type: research

Polypyridylruthenium(II) complexes exert in vitro and in vivo nematocidal activity and show significant inhibition of parasite acetylcholinesterases
Publication date: Available online 29 November 2017 Source:International Journal for Parasitology: Drugs and Drug Resistance Author(s): Madhu Sundaraneedi, Ramon M. Eichenberger, Rafid Al-Hallaf, Dai Yang, Javier Sotillo, Siji Rajan, Phurpa Wangchuk, Paul R. Giacomin, F. Richard Keene, Alex Loukas, J. Grant Collins, Mark S. Pearson Over 4.5 billion people are at risk of infection with soil transmitted helminths and there are concerns about the development of resistance to the handful of frontline nematocides in endemic populations. We investigated the anti-nematode efficacy of a series of polypyridylruthenium...
Source: International Journal for Parasitology: Drugs and Drug Resistance - November 30, 2017 Category: Parasitology Source Type: research