Ectonucleotidases: An Outside Chance for Drug Development
Friday, 28 April 2017
Sometimes, the most intriguing cellular processes happen outside of the cell. Case in point: purinergic signaling pathways, in which extracellular receptors sense levels of purines in the extracellular milieu. The result? A wide array of effects on neuronal signaling, vascular tone, thrombosis, and immune function. But what controls the level of extracellular purines? Enter ectonucleotidases:
- Published in Emerging Targets, HTS Assays, Uncategorized
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New Publication: HTS Method for Measuring Drug Residence Time
Tuesday, 25 April 2017
View our latest publication, “A High-Throughput Method for Measuring Drug Residence Time Using the Transcreener® ADP2 Assay” in SLAS Discovery. Inhibitor residence times are increasingly being used to prioritize molecules early in lead discovery programs. Current methods for determining residence time are low-throughput or require the synthesis of labeled ligands. Our goal was to create
- Published in Company, HTS Assays, News
Detecting Rho-GEF Activity Using the Transcreener® GDP Assay
Friday, 24 March 2017
Rho GTPases act as molecular switches to regulate the cytoskeletal dynamics underlying cell motility. Rho GEFs (guanine nucleotide exchange factors) positively regulate Rho GTPases by accelerating GDP dissociation and allowing formation of the active GTPase-GTP complex. Active Rho GTPases typically stimulate cell growth and migration, sometimes triggering tumorigenesis or invasion. Selectively disrupting GEF action using
- Published in Company, HTS Assays, Products
BellBrook Labs Awarded NIH Funding for Collaboration with University of Utah to Develop Biosensors for Epigenetic Drug Discovery
Monday, 12 December 2016
BellBrook Labs was awarded a Phase I grant of $225,000 to develop biosensors for detection of chromatin modifying enzymes, such as acetyltransferases and methyltransferases, in collaboration with University of Utah chemist Jennifer Heemstra. The collaboration leverages nucleic aptamer technology being developed by Dr. Heemstra to streamline development of assays for epigenetic enzymes being targeted for
- Published in Epigenetics, HTS Assays
Kinase Assays and Applications in Cancer Therapeutic Discovery
Wednesday, 30 November 2016
The ABL1 gene is a special type of gene that encodes a protein tyrosine kinase. It is involved in various cellular processes, including but not limited to cell adhesion, cell division, and cell differentiation. This protein’s activity is adversely regulated by its SH3 domain, which involves the deletion of the region that encodes the domain
- Published in HTS Assays
The Major Applications of Kinase Activity Assays
Sunday, 20 November 2016
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
- Published in HTS Assays
Creating a Methyltransferase HTS Assay Using an SAH Riboswitch Part II
Wednesday, 19 October 2016
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
- Published in Epigenetics, HTS Assays, Products
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
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
