ArticleCurrent chemical genomics2012
A homogenous luminescence assay reveals novel inhibitors for giardia lamblia carbamate kinase.
Article in Current chemical genomics, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 16 citations in OpenAlex.
- Review
- Disulfiram: Mechanisms, Applications, and Challenges.Antibiotics (Basel, Switzerland) · 2023Review
- TheJournal of microbiology and biotechnology · 2022Article
- Recent Advances in Cancer Drug Discovery Through the Use of Phenotypic Reporter Systems, Connectivity Mapping, and Pooled CRISPR Screening.Frontiers in pharmacology · 2022Review
- Discovery and Preclinical Development of Antigiardiasis Fumagillol Derivatives.Antimicrobial agents and chemotherapy · 2020Article
- Disulfiram can inhibit MERS and SARS coronavirus papain-like proteases via different modes.Antiviral research · 2018Article
- Susceptibility Testing of Medically Important Parasites.Clinical microbiology reviews · 2017Review
- Cell and small animal models for phenotypic drug discovery.Drug design, development and therapy · 2017Review
- Drug Development Against the Major Diarrhea-Causing Parasites of the Small Intestine, Cryptosporidium and Giardia.Frontiers in microbiology · 2015Review
- Discovery of novel antigiardiasis drug candidates.Antimicrobial agents and chemotherapy · 2014Article
- Structural basis for inactivation of Giardia lamblia carbamate kinase by disulfiram.The Journal of biological chemistry · 2014Article
- Treatment of giardiasis: current status and future directions.Current infectious disease reports · 2014Article
- Phenotypic screens as a renewed approach for drug discovery.Drug discovery today · 2013Review
- Crystal structures of carbamate kinase from Giardia lamblia bound with citric acid and AMP-PNP.PloS one · 2013Article
Corrections and comments
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Authors and funding
10 authors at 4 institutions in 1 country.
Funding
Abstract
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 giardisis, resistance to these drugs has been reported and is likely to increase. The Giardia carbamate kinase (glCK) plays an essential role in Giardia metabolism and has no homologs in humans, making it an attractive candidate for anti-Giardia drug development. We have developed a luminescent enzyme coupled assay to measure the activity of glCK by quantitating the amount of ATP produced by the enzyme. This assay is homogeneous and has been miniaturized into a 1536-well plate format. A pilot screen against 4,096 known compounds using this assay yielded a signal-to-basal ratio of 11.5 fold and Z' factor of 0.8 with a hit rate of 0.9 % of inhibitors of glCK. Therefore, this Giardia lamblia carbamate kinase assay is useful for high throughput screening of large compound collection for identification of the inhibitors for drug development.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.