
pmid: 15301960
The fluorescence-based thermal shift assay is a general method for identification of inhibitors of target proteins from compound libraries. Using an environmentally sensitive fluorescent dye to monitor protein thermal unfolding, the ligand-binding affinity can be assessed from the shift of the unfolding temperature (Delta Tm) obtained in the presence of ligands relative to that obtained in the absence of ligands. In this article, we report that the thermal shift assay can be conducted in an inexpensive, commercially available device for temperature control and fluorescence detection. The binding affinities obtained from thermal shift assays are compared with the binding affinities measured by isothermal titration calorimetry and with the IC(50) values from enzymatic assays. The potential pitfalls in the data analysis of thermal shift assays are also discussed.
Protein Denaturation, Time Factors, Drug Evaluation, Preclinical, Temperature, Proteins, Ligands, Kinetics, Data Interpretation, Statistical, Endopeptidases, Aspartic Acid Endopeptidases, Amyloid Precursor Protein Secretases, Fluorescent Dyes
Protein Denaturation, Time Factors, Drug Evaluation, Preclinical, Temperature, Proteins, Ligands, Kinetics, Data Interpretation, Statistical, Endopeptidases, Aspartic Acid Endopeptidases, Amyloid Precursor Protein Secretases, Fluorescent Dyes
| selected citations These citations are derived from selected sources. This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically). | 616 | |
| popularity This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network. | Top 0.1% | |
| influence This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically). | Top 1% | |
| impulse This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network. | Top 10% |
