Sialyltransferases: Sugar Makes the Medicine Go Down?

Glycan structures decorate a wide variety of cell types—dotting the surface of blood cells, linked to lipid moieties on neurons, and studding the membrane of tumor cells. These carbohydrate structures create a cellular language that is translated by binding partners, eliciting specific downstream effects. And for some cancers, the effects can be devastating.   Consider
Read more
No Comments

BellBrook Labs Awarded NIH Grant to Develop a High Throughput cGAS Assay for Cancer and Autoimmune Disease Drug Discovery

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
Read more
No Comments

Ectonucleotidases: An Outside Chance for Drug Development

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:
Read more
No Comments

New Publication: HTS Method for Measuring Drug Residence Time

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
Read more
No Comments

Detecting Rho-GEF Activity Using the Transcreener® GDP Assay

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
Read more
No Comments

BellBrook Labs Expands Drug Discovery Services Portfolio to Include Lead Discovery Services

Madison, WI, February 2017 – In response to an increasing demand for characterization and prioritization of compounds downstream of HTS or virtual screening, BellBrook Labs is expanding its Drug Discovery Services to include Lead Discovery in addition to Assay Development.  BellBrook will use its proprietary Transcreener® HTS assay platform to accelerate clients’ hit-to-lead and SAR
Read more
No Comments

Creating a Methyltransferase HTS Assay Using an SAH Riboswitch Part II

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
Read more
No Comments

Creating a Methyltransferase HTS Assay Using an SAH Riboswitch Part I

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
Read more
No Comments