Webinar: Streamline HTS and Lead Discovery with the Transcreener ADP Kinase Assay

Identifying bona fide hits efficiently and effectively is a challenge in any small molecule drug discovery program. Using the appropriate assays for screening and hit-to-lead is an important determinant of success, but choosing from among the myriad types of assays can be a daunting process. ADP detection simplifies discovery, providing a universal approach to targeting
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Minding the Membrane: Powerful Approach to Interrogate Molecular Events in Ras-PI3K Interactions

It has been 30 years since the lipid signaling molecule phosphatidylinositol 3,4,5-trisphosphate (PIP3) was first identified¹, and its role as a key regulator of cell growth and survival was recognized in the earliest investigations into this molecule.² Class IA phosphoinositide 3-kinases (PI3Ks) generate PIP3. The inappropriate activation of this pathway has grave consequences in many
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Transcreener Assay Helps Find New Approach to C. difficile

Clostridium difficile – One of the Deadliest Enemies in Hospitals There are half a million reasons to consider Clostridium difficile as “Enemy Number 1” for public health. That’s because the annual cases of C. difficile, or C diff, infection now top 500,000 per year in the U.S.—resulting in more than 29,000 deaths per year. Worse
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Transcreener ADP Assay Aids in Discovery of RIPK2 Inhibitors for Autoinflammation

When the body responds to a bacterial pathogen, fragments of bacterial peptidoglycan alert a human host to the presence of a microbial invader. A receptor named NOD2 recognizes the peptidoglycans and sounds the alarm, initiating immune responses by causing the production of pro-inflammatory cytokines via NF-κB and MAP kinase pathways 1. In this manner, NOD2
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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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Newly Patented Aurora A Kinase Inhibitor a Promising Contender for Cancer Treatment

Aurora A Kinase in Cancer Drug Development Aurora A Kinase, along with -B and -C, are members of a family of serine/threonine protein kinases that play critical roles in coordinating mitosis, including establishment of the mitotic spindle, centrosome duplication, centrosome separation as well as maturation, chromosomal alignment, spindle assembly checkpoint, and cytokinesis. The enzyme’s role
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Using the Transcreener® GDP Assay to Discern the Truth about Dynamin Inhibitors

Imagine viewing the plasma membrane of a cell from an interior perspective, with a front-row seat to the process by which substances enter the cell. Over in one corner, the plasma membrane begins to bulge inward, forming a sphere stretching toward you with a droplet-shaped neck on the opposite side that remains connected to the
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New Posters from DOT 2017

Poster Presentations A Homogenous, High Throughput Assay to Measure Guanine Nucleotide Exchange Factor Activity Using Transcreener® GDP Assay Guanine nucleotide exchange factors (GEFs) positively regulate Rho GTPases by accelerating GDP dissociation to allow formation of the active, GTP-bound complex. Development of inhibitors that specifically disrupt GEF action on a target Rho GTPase may be a
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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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