Creating a Methyltransferase HTS Assay Using an SAH Riboswitch Part I
Friday, 23 September 2016
Riboswitches were discovered in 2002 by Ron Breaker at Yale as RNA-based intracellular sensors of vitamin derivatives. During the last decade, riboswitches have been identified that bind a range of small biomolecules including nucleotides, amino acids, and ions. Riboswitches exert regulatory control of transcription, translation, splicing, and RNA stability. BellBrook scientists used a riboswitch that
- Published in Epigenetics, HTS Assays, Products
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Measuring Dissociation Rates and Residence Times for Kinase Inhibitors using a Jump Dilution Protocol
Tuesday, 06 October 2015
Application Note Analysis of inhibitor residence times is increasingly being incorporated into lead development efforts because longer engagement with the target can result in improved efficacy, increased therapeutic window and reduced side effects. In this application note, BellBrook Labs scientist Meera Kumar, used a jump-dilution protocol with the Transcreener® ADP2 FP Kinase Assay to determine
- Published in HTS Assays
New Publication: HTS Assay for Rho GEFs
Tuesday, 28 July 2015
See our latest publication, “A High-Throughput Assay for Rho Guanine Nucleotide Exchange Factors Based on the Transcreener GDP Assay” in the Journal of Biomolecular Screening BellBrook Labs scientists Tom Zielinski and Meera Kumar collaborated with investigators in Mel Reichman’s laboratory at the Lankenau Institute for Medical Research to develop a robust, HTS-compatible assay for Rho
- Published in HTS Assays
View Our Kinase Inhibitor Residence Time Webinar Anytime!
Monday, 11 May 2015
Analysis of inhibitor residence times is increasingly being incorporated into lead development efforts because longer engagement with the target can result in improved efficacy, increased therapeutic window and reduced side effects. Though residence time can be determined using immobilized ligand methods such surface plasmon resonance, conjugation of drugs can affect their binding. In this webinar,
- Published in HTS Assays, News
A Specific Inhibitor for a Promiscuous Glycosyltransferase
Thursday, 23 April 2015
O-GlcNAc transferase (OGT) is a promiscuous covalent regulatory enzyme that affects diverse cellular processes by attaching O-linked N-acetylglucosamine (O-GlcNAc) residues to intracellular proteins including kinases, phosphatases, transcription factors, and histones. Though recent evidence suggests that OGT may be an anti-cancer target, developing a specific inhibitor that does not interfere with cell surface glycans is a
- Published in HTS Assays
Killing Two Kinases with One Drug
Thursday, 26 March 2015
Cancer cells are characterized by a complex network of interrelated and compensatory signaling driving multiple kinases that reduce their sensitivity to targeted therapy. Strategies that inhibit two or more kinases are needed to block the growth of refractory tumor cells. Researchers at McGill University (Canada), led by Dr. Suman Rao at the Cancer Drug Research
- Published in HTS Assays
Learn How the Transcreener® ADP2 Assay Can Determine Drug-Kinase Residence Time
Thursday, 30 October 2014
Our newest application note provides a protocol and experimental example for the use of the Transcreener ADP2 FP Assay to determine the residence time of a drug (or drug candidate) during its interaction with a kinase. The duration of residence time can be highly relevant for assessing the durable pharmacologic effects of a drug candidate.
- Published in HTS Assays
New Application Note: High Throughput GEF Assay using the Transcreener GDP Assay
Thursday, 16 October 2014
This Application note serves as a guide for using the Transcreener® GDP Assay to detect the activity of guanine nucleotide exchange factors (GEFs) based on their stimulation of steady state GTPase activity. As an example, an assay was developed using Dbs, a Rho-specific guanine nucleotide exchange factor (RhoGEF) in combination with two monomeric GTPases, CDC42
- Published in HTS Assays
Ensuring Assay Success: The Right Plate Makes All The Difference
Thursday, 19 June 2014
Transcreener® HTS Assays rely on direct immunodetection of nucleotides with a far-red readout in a simple mix-and-read format. The assays are available in three different detection modes, fluorescence polarization (FP), fluorescence intensity (FI), and time-resolved Forster resonance energy transfer (TR-FRET). A good microplate reader and the right choice of plates to differentiate specific signal versus
- Published in HTS Assays
Webinar Slides Available: Integrated Instrument-Reagent Platform for Screening Kinases and Methyltransferases
Monday, 13 May 2013
Slides from the May 15, 2013 BellBrook Labs/BMG LABTECH webinar are available here: Integrated Instrument-Reagent Platform for Screening Kinases and Methyltransferases Summary: Biochemical HTS assays are a critical component of drug discovery programs focused on enzyme targets like kinases and methyltransferases. Assembling high-quality assay reagents and validating them on a detection platform that can deliver speed, accuracy,
- Published in HTS Assays
