ArticleJournal of biomolecular screening2008
Evaluating PI3 kinase isoforms using Transcreener ADP assays.
Article in Journal of biomolecular screening, 2008. 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, 31 citations in OpenAlex.
- Article
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- Article
- Required hydrophobicity of fluorescent reporters for phosphatidylinositol family of lipid enzymes.Analytical and bioanalytical chemistry · 2017Article
- Development and validation of a high-throughput intrinsic ATPase activity assay for the discovery of MEKK2 inhibitors.Journal of biomolecular screening · 2013Article
- High-throughput screening for RecA inhibitors using a transcreener adenosine 5'-O-diphosphate assay.Assay and drug development technologies · 2012Article
- A homogeneous and nonisotopic assay for phosphatidylinositol 4-kinases.Analytical biochemistry · 2011Article
- Regulators of G-protein signaling and their Gα substrates: promises and challenges in their use as drug discovery targets.Pharmacological reviews · 2011Review
- Structure of lipid kinase p110β/p85β elucidates an unusual SH2-domain-mediated inhibitory mechanism.Molecular cell · 2011Article
- Fluorescence polarization assays in small molecule screening.Expert opinion on drug discovery · 2011Article
- Development and validation of a transcreener assay for detection of AMP- and GMP-producing enzymes.Assay and drug development technologies · 2010Article
- Two Galpha(i1) rate-modifying mutations act in concert to allow receptor-independent, steady-state measurements of RGS protein activity.Journal of biomolecular screening · 2009Article
- A basis for reduced chemical library inhibition of firefly luciferase obtained from directed evolution.Journal of medicinal chemistry · 2009Article
- Characterization and optimization of a red-shifted fluorescence polarization ADP detection assay.Assay and drug development technologies · 2009Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
Development of drugs targeting lipid kinases has been delayed by the lack of robust screening assays. Methods are needed that can accommodate the presentation of different acceptor substrates in the optimal lipid environment. The Transcreener ADP Assay relies on homogeneous immunodetection of adenosine diphosphate (ADP), using either fluorescence polarization (FP) or time-resolved fluorescence resonance energy transfer (TR-FRET) as a signal output. Detection of ADP--the invariant product of all kinase reactions--provides complete flexibility for varying lipid substrate parameters. The authors used this assay to optimize dispersal methods for C8 and C16 phosphatidylinositol 4,5 bisphosphate substrates and to assess the effects of chain length on the activity and inhibition of phosphoinositide-3-kinase (PI3K) isoforms. The nonphysiological C8 substrate supported the highest activity. Known inhibitors were profiled using both the FP- and TR-FRET-based assays, and there was excellent concordance (r(2)=0.93) in the IC(50) values. The overall rank order of inhibitors was the same using the C8 and C16 substrates, except for minor deviations. Adenosine triphosphate (ATP) hydrolysis in the absence of substrate was detected with the PI3Kalpha isoform, and inhibitors affected PI3Kalpha intrinsic ATP hydrolysis activity similarly to lipid phosphorylation.
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Registered trials
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