Sialyltransferases: Sugar Makes the Medicine Go Down?
Monday, 26 June 2017
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
- Published in Emerging Targets
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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 Expands Drug Discovery Services Portfolio to Include Lead Discovery Services
Wednesday, 22 February 2017
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
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
New Case Study: Discovery of GALNT3 Inhibitors Using a Universal Glycosyltransferase Assay and Orthogonal Pooled Screening
Friday, 27 November 2015
Glycosyltransferase (GT) enzymes participate in diverse metabolic and regulatory roles by catalyzing the transfer of sugars to protein, lipid and carbohydrate acceptors as well as to other molecules. Within the GT family, there are over 20 distinct polypeptide N-acetylgalactosaminyltransferases (GALNTs) that catalyze the initial step of O-glycosylation. GALNT3 overexpression and dysregulation has been directly linked
“Simplifying HTS with Orthogonal Pooled Screening” Webinar – Encore Presentation
Monday, 17 August 2015
Access to this webinar is now available anytime to suit your schedule! In this webinar, Dr. Mel Reichman, Director of Chemical Genomics Center at the Lankenau Institute for Medical Research (LIMR, Wynnewood, PA) describes the Orthogonal Pooled Screening (OPS™) Platform that he developed to provide a drastically more efficient and less expensive approach for rapidly finding
- Published in News
