EZH2 Methyltransferase Inhibitors Hold Promise for Combating Neuropathic Pain
Friday, 21 July 2017
When people experience neuropathic pain, they often describe “pins and needles” sensations or burning, shooting, or stabbing pain that can be agonizing and difficult to bear. In some cases, neuropathic pain is so intense that the pressure of clothing or the weight of a bed sheet can cause misery. Chronic neuropathic pain can be caused
- Published in Emerging Targets, Epigenetics, HTS Assays
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BellBrook Labs Awarded NIH Grant to Develop a High Throughput cGAS Assay for Cancer and Autoimmune Disease Drug Discovery
Wednesday, 14 June 2017
BellBrook Labs was recently awarded a $288,000 SBIR Phase I grant from the National Institutes of General Medical Sciences (NIGMS) to develop an HTS assay for cyclic GAMP synthase, an enzyme that triggers immune responses to viruses and tumors. The new assay will be used in an effort to screen for cGAS enzyme modulators as
- Published in Emerging Targets, HTS Assays, News
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
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
