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A High-Throughput Assay for Rho Guanine Nucleotide Exchange Factors Based on the Transcreener GDP Assay
TLDR
A simple, generic biochemical assay method for measuring GEF activity based on the fact that GDP dissociation is generally the rate-limiting step in the Rho GTPase catalytic cycle, and thus addition of a GEF causes an increase in steady-state GTP enzyme activity is developed. Expand
A bioluminescent-based, HTS-compatible assay to monitor G-protein-coupled receptor modulation of cellular cyclic AMP.
TLDR
A novel assay for monitoring changes in intracellular cyclic AMP (cAMP) concentration with high sensitivity and reproducibility, and of format amenable to high throughput screening (HTS) in 96, 384, and 1,536-well plates, and as a bioluminescent assay is potentially less prone to interferences originating from fluorescent compounds. Expand
Development and Validation of a Generic Fluorescent Methyltransferase Activity Assay Based on the Transcreener AMP/GMP Assay
TLDR
The authors have developed a robust HTS assay for HMTs that should be broadly applicable to other types of methyltransferases as well and is based on the well-characterized Transcreener AMP/GMP assay. Expand
A High-Throughput Method for Measuring Drug Residence Time Using the Transcreener ADP Assay
  • Meera Kumar, R. Lowery
  • Chemistry, Medicine
  • SLAS discovery : advancing life sciences R & D
  • 1 February 2017
TLDR
This work used the Transcreener ADP2 Kinase assay as a universal, homogenous method to monitor the recovery of kinase activity as the drugs dissociated from preformed inhibitor–kinase complexes and found that the rank ordering of inhibitor koff values correlated with literature values determined using ligand binding assays. Expand
Biochemical Assay Development for Histone Methyltransferases Using a Transcreener-Based Assay for S-Adenosylhomocysteine.
TLDR
The Transcreener(®) EPIGEN Methyltransferase assay is developed, a sensitive SAH detection method with a fluorescence polarization readout, to enable universal HMT detection independent of acceptor substrate. Expand
A highly-sensitive high throughput assay for dynamin's basal GTPase activity
TLDR
A highly sensitive fluorescence-based assay capable of detecting dynamin’s basal GTPase activity under conditions compatible with high throughput screening is reported, providing the basis for a more extensive search for more potent and chemically desirable dynamin inhibitors. Expand
High-Throughput Screening Assays for Cancer Immunotherapy Targets: Ectonucleotidases CD39 and CD73
TLDR
HTS-compatible assays for ectonucleotidase activity may allow identification of purinergic signaling pathway inhibitors important for tumor-specific immune responses during tumor pathogenesis. Expand
High-Throughput Assay for RhoGEFs Based on the Transcreener® GDP Assay.
TLDR
A high-throughput screening (HTS)-compatible method for detecting GTPase exchange factor (GEF) activity based on stimulation of GDP formation by Rho GTPases using a fluorescence polarization immunoassay. Expand
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