Results 11 to 20 of about 665 (203)
POT1 stability and binding measured by fluorescence thermal shift assays. [PDF]
PLoS ONE, 2021 The protein POT1 (Protection of Telomeres 1) is an integral part of the shelterin complex that protects the ends of human chromosomes from degradation or end fusions. It is the only component of shelterin that binds single-stranded DNA.
Lynn W DeLeeuw +7 more
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Streamlining cellular thermal shift assay for ultra-high throughput screening
SLAS DiscoveryThe Cellular Thermal Shift Assay (CETSA) has emerged as a powerful tool for evaluating drug-target interactions in live cells, yet its application in ultra-high throughput screening (uHTS) has been limited by technical constraints.
Pascal Lambertz +9 more
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Thermal shift engagement assay for Class IIA histone deacetylase inhibitor screening
Results in ChemistryHistone deacetylase (HDAC) proteins are the targets of several anti-cancer clinical drugs, which motivates future inhibitor development. Class IIA HDAC proteins, HDAC4, HDAC5, HDAC7, and HDAC9, are pseudodeacetylases that lack a key catalytic amino acid ...
Lauren N. Kotsull, Mary Kay H. Pflum
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, 2023 Thermal shift assay or differential scanning fluorimetry analyzes the effect of small molecules on the thermostability of a protein by gradual heat denaturation and monitoring absorption of the fluorescent dye SYPR Orange at 488 nm.
Verena Dederer +3 more
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, 2023 Thermal shift assay or differential scanning fluorimetry analyzes the effect of small molecules on the thermostability of a protein by gradual heat denaturation and monitoring absorption of the fluorescent dye SYPR Orange at 488 nm.
Verena Dederer +3 more
openaire +1 more source
Interrogating Fragments Using a Protein Thermal Shift Assay [PDF]
Australian Journal of Chemistry, 2013 Protein thermal shift is a relatively rapid and inexpensive technique for the identification of low molecular weight compound interactions with protein targets. An increase in the melting temperature of the target protein in the presence of a test ligand is indicative of a promising ligand–protein interaction.
McMahon, Roisin M +2 more
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HiBiT Cellular Thermal Shift Assay (HiBiT CETSA)
, 2023 Cellular thermal shift assay (CETSA) is based on the thermal stabilization of the protein target by a compound binding. Thus, CETSA can be used to measure a compound's cellular target engagement and permeability. HiBiT CETSA method is quantitative and has higher throughput compared to the traditional Western-based CETSA.
Ramachandran, Sarath +5 more
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A fluorescence-based thermal shift assay identifies inhibitors of mitogen activated protein kinase kinase 4. [PDF]
PLoS ONE, 2013 Prostate cancer (PCa) is the second highest cause of cancer death in United States males. If the metastatic movement of PCa cells could be inhibited, then mortality from PCa could be greatly reduced. Mitogen-activated protein kinase kinase 4 (MAP2K4) has
Sankar N Krishna +6 more
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A cellular thermal shift assay for detecting amino acid sites involved in drug target engagement
STAR Protocols, 2022 Summary: Evaluating how drugs bind to specific targets at the cellular level is essential to their development and efficacy. Here, we present a protocol to detect the amino acid sites involved in drug-target engagement using a cellular thermal shift ...
Liyuan Peng +4 more
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Analysis of Protein Stability and Ligand Interactions by Thermal Shift Assay [PDF]
Current Protocols in Protein Science, 2015 AbstractPurification of recombinant proteins for biochemical assays and structural studies is time‐consuming and presents inherent difficulties that depend on the optimization of protein stability. The use of dyes to monitor thermal denaturation of proteins with sensitive fluorescence detection enables rapid and inexpensive determination of protein ...
Huynh, Kathy, Partch, Carrie L
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