Using a Universal GMP Assay for PDE Research

GMP Assay for PDE Inhibitor Discovery
A universal GMP assay to aid in PDE research and potential COVID-19 disruption. – Phosphodiesterase enzymes (PDEs) modulate pathways throughout the body. Since unregulated PDEs contribute to disease in many cases, it makes sense therapies that inhibit these enzymes have the potential to treat several different ailments. These include cardiovascular and respiratory issues, diabetes, fibrotic
Read more
No Comments

Fluorescence Polarization Assays for Drug Discovery

FP Assays
Fluorescence polarization assays (FP assays) are used in a variety of ways.  From uncovering molecules in solution, to monitoring drug levels in clinical settings, and are enabling in drug discovery. These binding assays have been used to gain knowledge of molecular interactions, enzymatic activity, and nucleic acid hybridization. Moreover, scientists use FP to study small
Read more
No Comments

TR-FRET Assays In Drug Discovery

TR-FRET Assays
Förster resonance energy transfer (FRET) technology and TR-FRET assays are used in laboratories globally for a variety of applications ranging from disease detection, to drug discovery, to monitoring genetic differences between individuals and populations. The brilliance of this technology is due to the sensitivity provided by the spectral overlap and the proximity of the acceptor
Read more
No Comments

Posters Presented at SLAS 2018

Thanks to all who stopped by the booth at SLAS 2018! We appreciate the great conversation and look forward to continued discussion. Its great to hear the success stories of current Transcreener users, and to meet a new group of individuals who are searching for an HTS assay for their challenging target. For those of
Read more
No Comments

A Novel Approach Discovers Hundreds of Cancer-Relevant Arginine Methylation Sites for CARM1

Protein arginine methylation is an important post-translational modification, but its impact remains rather mysterious. Approximately 7% of all arginine residues in the human proteome are modified by mono- or di-methylation (which is a similar order of magnitude to the 9% of serine residues that are phosphorylated and the 7% of lysine residues that are ubiquitinated).¹
Read more
No Comments

Doubling the Odds: Two-Pronged Strategy to Halt Cancer Cell Proliferation

It would be difficult to underestimate the importance of polo-like kinase 1 (Plk1) for cancer, given its influence on cell division. As one of five members of the Polo-like family of serine/threonine protein kinases in eukaryotic cells, Plk1 plays a multifaceted role in the cell cycle and thus controls cancer progression fueled by unchecked cell
Read more
No Comments

Taking Up Residence: Using the Transcreener ADP Assay to Measure the Kinetics of Kinase Inhibitor Interactions

Classically speaking, assays for interactions between drug molecules and their targets have measured binding affinity under equilibrium conditions. In drug discovery projects, it had long been assumed that carefully measuring IC50 (half-maximal inhibitory concentration), EC50 (effector concentration for half-maximal response), Kd  (equilibrium dissociation constant), and/or Ki (inhibition constant) would allow drug candidates to be prioritized
Read more
No Comments

BellBrook Labs Launches Ultra-Sensitive Methyltransferase Assay to Accelerate Epigenetic Drug Discovery

Methyltransferases have become a major focus of drug discovery for cancer and other diseases driven by epigenetic factors.  BellBrook Labs’ new, ultra-sensitive AptaFluor™ SAH Methyltransferase Assay eliminates cost and sensitivity barriers that are slowing the discovery of methyltransferase inhibitors. New AptaFluor SAH Methyltransferase Assay Schematic BellBrook Labs announces the launch of their latest drug discovery
Read more
No Comments

On Demand Webinar: Development of Ectonucleotidase Assay Methods Using the Transcreener® HTS Assay Platform

View the Webinar On Demand at Anytime Ectonucleotidases are plasma membrane-bound enzymes with externally oriented active sites that metabolize nucleotides to nucleosides. One example is ectonucleoside triphosphate diphosphohydrolase-1, also known as CD39, ENTPD1, or NTPDase1. CD39 hydrolyzes ATP and ADP to AMP. Other ectonucleotidases such as CD73 process the AMP further into adenosine, which is
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