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A simultaneous assessment of CYP3A4 metabolism and induction in the DPX-2 cell line
TLDR
Comparative data obtained with a combination of the above assays suggests that the application of several independent in vitro technologies used in DPX-2 cells is the best possible strategy for the assessment of the complex phenomena of CYP3A4 induction and inhibition. Expand
Two Gα i1 Rate-Modifying Mutations Act in Concert to Allow Receptor-Independent, Steady-State Measurements of RGS Protein Activity
TLDR
To enable nonradioactive, homogeneous detection of RGS protein effects on Gαi1(R178M/A326S), the authors developed a Transcreener ® fluorescence polarization immunoassay based on a monoclonal antibody that recognizes GDP with greater than 100-fold selectivity over GTP. Expand
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
Evaluating Modulators of “Regulator of G‐protein Signaling” (RGS) Proteins
TLDR
High‐throughput screening procedures for identifying modulators of RGS protein‐mediated GTPase acceleration (GAP activity), for assessment of R GS domain/Gα interactions, and for validation of candidate GAP‐modulatory molecules with the single‐turnover GTP hydrolysis assay are described. Expand
A Homogeneous Fluorescent Live-Cell Assay for Measuring 7-Transmembrane Receptor Activity and Agonist Functional Selectivity Through Beta-Arrestin Recruitment
TLDR
The Tango™ 7TM receptor assay technology is reported on, a high-throughput homogeneous assay method for monitoring beta-arrestin recruitment that uses a live-cell fluorescent readout and is broadly applicable to 7TM receptors, independent of G-protein coupling and, as such, has been used to produce assays for over 70 7 TM receptor targets. Expand
Development of a coactivator displacement assay for the orphan receptor estrogen-related receptor-gamma using time-resolved fluorescence resonance energy transfer.
TLDR
In vitro interaction methodology suggests that binding of 4-OHT, tamoxifen, or DES to ERRgamma results in differential affinity of coregulators for ERRGamma due to unique ligand-induced conformations. Expand
Development and Validation of a Universal High-Throughput UDP-Glycosyltransferase Assay with a Time-Resolved FRET Signal.
TLDR
The TR-FRET-based UDP detection assay provides a broadly applicable approach for screening glycosyltransferases that use a UDP-sugar donor and was validated by orthogonal pooled screening with 8,000 compounds using polypeptide N-acetylgalactosaminyltransferase T3 as the target. Expand
RGS21, a regulator of taste and mucociliary clearance?
TLDR
This study investigated whether regulator of G protein signaling‐21 (RGS21) has the potential to modulate signaling pathways connected to airway mucociliary clearance, given that RGS proteins modulate GPCR signaling by acting as GTPase‐accelerating proteins (GAPs) for the Gα subunits of heterotrimeric G proteins. 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
Isolation and characterization of strains defective in vacuolar ornithine permease in Neurospora crassa.
TLDR
Results suggest that both strains are defective in the gene which encodes the vacuolar ornithine permease, which is shown to be inhibited competitively by L-arginine and histidine while Ornithine uptake was inhibited by a variety of amino acids. Expand
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