Researchers Employ GTPase Activity Assay to Investigate Rab Proteins

Scientist Using a GTPase Activity Assay
GTPases are in the limelight in biology and drug discovery because of their role in a wide range of cellular processes and function.  They are highly conserved regulatory proteins involved in such diverse roles as signal transduction, protein biosynthesis, cell adhesion, membrane remodeling and trafficking, cytoskeletal reorganization, apoptosis, autophagy, and cell motility, to mention a
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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
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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
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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
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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
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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
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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
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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:
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