When it comes to the significant process that is compiling components for the correct kinase assay for your work, it can be extremely time-consuming and expensive. Having a simple mix-and-read method can take a lot of the stress out of this process. The good news is that you can find a kinase assay kit which […]
In Part I of II in this blog series, discussion included the challenges of screening methyltransferases, steps in developing an SAH assay, the experimental assay procedure, assay sensitivity, and reagent stability. Please view the previous post here: Creating a Methyltransferase HTS Assay Using an SAH Riboswitch Part I. Compatibility with Diverse MT Accepter Substrates As […]
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 […]
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 […]
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 […]
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, […]
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 […]
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 […]
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. […]
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 […]
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