ArticleJournal of biomolecular screening2009
Buffer optimization of thermal melt assays of Plasmodium proteins for detection of small-molecule ligands.
Article in Journal of biomolecular screening, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed.
- Bumped kinase inhibitor 1369 is effective against Cystoisospora suis in vivo and in vitro.International journal for parasitology. Drugs and drug resistance · 2019Article
- Isothermal Analysis of ThermoFluor Data can readily provide Quantitative Binding Affinities.Scientific reports · 2019Article
- Toxoplasma Calcium-Dependent Protein Kinase 1 Inhibitors: Probing Activity and Resistance Using Cellular Thermal Shift Assays.Antimicrobial agents and chemotherapy · 2018Article
- Selective inhibition of Sarcocystis neurona calcium-dependent protein kinase 1 for equine protozoal myeloencephalitis therapy.International journal for parasitology · 2016Article
- Mycobacterium Cytidylate Kinase Appears to Be an Undruggable Target.Journal of biomolecular screening · 2016Article
- An effective thiol-reactive probe for differential scanning fluorimetry with a standard real-time polymerase chain reaction device.Analytical biochemistry · 2016Article
- Brucella melitensis Methionyl-tRNA-Synthetase (MetRS), a Potential Drug Target for Brucellosis.PloS one · 2016Article
- Next-generation antimicrobials: from chemical biology to first-in-class drugs.Archives of pharmacal research · 2015Review
- Inhibition by stabilization: targeting the Plasmodium falciparum aldolase-TRAP complex.Malaria journal · 2015Article
- Recent developments in the use of differential scanning fluorometry in protein and small molecule discovery and characterization.Expert opinion on drug discovery · 2013Review
- Optimization of protein buffer cocktails using Thermofluor.Acta crystallographica. Section F, Structural biology and crystallization communications · 2013Article
- P6981, an arylstibonic acid, is a novel low nanomolar inhibitor of cAMP response element-binding protein binding to DNA.Molecular pharmacology · 2012Article
- Urea-based inhibitors of Trypanosoma brucei methionyl-tRNA synthetase: selectivity and in vivo characterization.Journal of medicinal chemistry · 2012Article
- Screening a fragment cocktail library using ultrafiltration.Analytical and bioanalytical chemistry · 2011Article
- Selective inhibitors of methionyl-tRNA synthetase have potent activity against Trypanosoma brucei Infection in Mice.Antimicrobial agents and chemotherapy · 2011Article
- Identification of inhibitors for putative malaria drug targets among novel antimalarial compounds.Molecular and biochemical parasitology · 2011Article
- Chemical genetics of Plasmodium falciparum.Nature · 2010Article
- Production of recombinant proteins from protozoan parasites.Trends in parasitology · 2010Review
- Use of thermal melt curves to assess the quality of enzyme preparations.Analytical biochemistry · 2010Article
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Authors and funding
16 authors.
Funding
Abstract
In the past decade, thermal melt/thermal shift assays have become a common tool for identifying ligands and other factors that stabilize specific proteins. Increased stability is indicated by an increase in the protein's melting temperature (Tm). In optimizing the assays for subsequent screening of compound libraries, it is important to minimize the variability of Tm measurements so as to maximize the assay's ability to detect potential ligands. The authors present an investigation of Tm variability in recombinant proteins from Plasmodium parasites. Ligands of Plasmodium proteins are particularly interesting as potential starting points for drugs for malaria, and new drugs are urgently needed. A single standard buffer (100 mM HEPES [pH 7.5], 150 mM NaCl) permitted estimation of Tm for 58 of 61 Plasmodium proteins tested. However, with several proteins, Tm could not be measured with a consistency suitable for high-throughput screening unless alternative protein-specific buffers were employed. The authors conclude that buffer optimization to minimize variability in Tm measurements increases the success of thermal melt screens involving proteins for which a standard buffer is suboptimal.
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