The human pathogen Giardia lamblia is an anaerobic protozoan parasite that causes giardiasis, one of the most common diarrheal diseases worldwide. Although several drugs are available for the treatment of giardiasis, drug resistance has been reported and is likely to increase, and recurrent infections are common. The search for new drugs that can overcome the drug-resistant strains of Giardia is an unmet medical need. New drug screen methods can facilitate the drug discovery process and aid with the identification of new drug targets. Using a bioluminescent ATP content assay, we have developed a phenotypic drug screen method to identify compounds that act against the actively growing trophozoite stage of the parasite. This assay is homogeneous, robust, and suitable for high-throughput screening of large compound collections. A screen of 4,096 pharmacologically active small molecules and approved drugs revealed 43 compounds with selective anti-Giardia properties, including 32 previously reported and 11 novel anti-Giardia agents. The most potent novel compound was fumagillin, which showed 50% inhibitory concentrations of 10 nM against the WB isolate and 2 nM against the GS isolate.
In-vitro susceptibility of Giardia lamblia to albendazole, mebendazole and other chemotherapeutic agents
Susceptibility of Giardia lamblia to aminoglycoside protein synthesis inhibitors: correlation with rRNA structure
A comparison of the in-vitro activity of some 5-nitroimidazoles and other compounds against Giardia intestinalis
Studies on hemoglobin Tochigi diseases ( 56-59 deleted) with particular reference to its osmotic fragility test by heating
In vitro drug susceptibility of 29 isolates of Giardia duodenalis from humans as assessed by an adhesion assay
The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones
A Simple Statistical Parameter for Use in Evaluation and Validation of High Throughput Screening Assays
Comparison between two common methods for measuring Giardia lamblia susceptibility to antiparasitic drugs in vitro
Genetic heterogeneity at the beta-giardin locus among human and animal isolates of Giardiaduodenalis and identification of potentially zoonotic subgenotypes
In vitro effects of thiazolides on Giardia lamblia WB clone C6 cultured axenically and in coculture with Caco2 cells
Quantitative high-throughput screening: a titration-based approach that efficiently identifies biological activities in large chemical libraries
Synthesis and in vitro trichomonicidal, giardicidal and amebicidal activity of N-acetamide(sulfonamide)-2-methyl-4-nitro-1H-imidazoles
Fumagillin and fumarranol interact with P. falciparum methionine aminopeptidase 2 and inhibit malaria parasite growth in vitro and in vivo
Synthesis and electrochemistry of 2-ethenyl and 2-ethanyl derivatives of 5-nitroimidazole and antimicrobial activity against Giardia lamblia
Draft genome sequencing of giardia intestinalis assemblage B isolate GS: is human giardiasis caused by two different species?
Identification of known drugs that act as inhibitors of NF-kappaB signaling and their mechanism of action
A new-generation 5-nitroimidazole can induce highly metronidazole-resistant Giardia lamblia in vitro
Identification of 23-(s)-2-amino-3-phenylpropanoyl-silybin as an antiviral agent for influenza A virus infection in vitro and in vivo
Plasmid vectors for proteomic analyses in Giardia: purification of virulence factors and analysis of the proteasome
Rapid identification of antifungal compounds against Exserohilum rostratum using high throughput drug repurposing screens
O(2)-dependent efficacy of novel piperidine- and piperazine-based chalcones against the human parasite Giardia intestinalis
A high-throughput screening assay for assessing the viability of Cryptococcus neoformans under nutrient starvation conditions
Drug Development Against the Major Diarrhea-Causing Parasites of the Small Intestine, Cryptosporidium and Giardia
3,5-Dicaffeoylquinic acid isolated from Artemisia argyi and its ester derivatives exert anti-leucyl-tRNA synthetase of Giardia lamblia (GlLeuRS) and potential anti-giardial effects
Quantitative assessment of the proliferation of the protozoan parasite Perkinsus marinus using a bioluminescence assay for ATP content
Identification of MMV Malaria Box inhibitors of Perkinsus marinus using an ATP-based bioluminescence assay
Identification of small-molecule inhibitors of Zika virus infection and induced neural cell death via a drug repurposing screen
The proteasome of the differently-diverged eukaryote Giardia lamblia and its role in remodeling of the microtubule-based cytoskeleton
Screening of the Pathogen Box for inhibitors with dual efficacy against Giardia lamblia and Cryptosporidium parvum
Identification of anisomycin, prodigiosin and obatoclax as compounds with broad-spectrum anti-parasitic activity
Identification of small-molecule agonists of human relaxin family receptor 1 (RXFP1) by using a homogenous cell-based cAMP assay
Antifungal Resistance, Metabolic Routes as Drug Targets, and New Antifungal Agents: An Overview about Endemic Dimorphic Fungi
Methionyl-tRNA synthetase inhibitor has potent in vivo activity in a novel Giardia lamblia luciferase murine infection model.
Host-targeted niclosamide inhibits C. difficile virulence and prevents disease in mice without disrupting the gut microbiota
The giardicidal activity of lobendazole, fabomotizole, tenatoprazole and ipriflavone: A ligand-based virtual screening and in vitro study
TriTOX: A novel Trichomonas vaginalis assay platform for high-throughput screening of compound libraries.
CRISPR Screens in Drug Resistance
CRISPR-Cas system enables the editing of genes to create or correct mutations. This feed focuses on the application of CRISPR-Cas system in high-throughput genome-wide screens to identify genes that may confer drug resistance.
This feed focuses mechanisms underlying addiction and addictive behaviour including heroin and opium dependence, alcohol intoxication, gambling, and tobacco addiction.