Transcreener Assay Used to Evaluate PI3K Inhibitors

PI3K Inhibitors for Cancer Research
PI3K Inhibitors and Cancer – Although cancer is widespread, determining the culprit, as well as individual treatment, is challenging. A variety of cancer types exist with a multitude of contributors. Being the most common human genetic disease, a whole host of genes are involved. Some contribute to curbing cancer (tumor suppressor genes), while oncogenes promote
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Transcreener ADP Assay Used to Discover RIPK1 Inhibitors

RIPK1 Inhibitors Inflammatory disease treatment
Genentech discovers novel RIPK1 inhibitors – Like other serine/threonine protein kinases, receptor-interacting serine/threonine-protein kinase 1 (RIPK1) plays a role in several signaling pathways that keep us living healthy, functioning lives. RIPK1 is one of those enzymes’ that wears a variety of hats depending on what function needs attention. It contributes to cell death as well
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Finding Inhibitors for a Cancer Target: CDK12 Activity Assays Accelerate the Search

CDK12 Activity Assays Find Inhibitors Cancer Treatment
All systems within our bodies function by means of proteins. When these proteins aren’t made correctly, our body malfunctions.  The short explanation: DNA is at the fabric of forming a functional protein; genes (made of DNA) get transcribed and then translated to become proteins. During this complex process, genes are not always correctly transcribed and
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Using TBK1 Inhibitors to Stop Cancer in Its Tracks

Scientist Working on TBK1 Inhibitors for Cancer Research
TBK1 Inhibitors, Autoimmune Disorders, and Cancer – Inflammation is a crucial step within the immune response, helping our bodies eliminate disease. However, it can also be a burden where misregulation creates a variety of maladies including cancer. As inflammation persists, becoming chronic, the beneficial elements can be lost and disease occurs. It’s not just autoimmune
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How a Tyrosine Kinase Inhibitor Is Giving Hope to Lung Cancer Patients

tyrosine kinase inhibitor lung cancer
According to the American Cancer Society, lung cancer is the leading cause of cancer death each year and accounts for approximately 13% of all new cases. The most common type being non-small cell lung cancer (NSCLC). Although smoking is the biggest contributor, other factors such as genetics and environmental pollutants contribute to lung cancer of
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How Does a Biochemical Kinase Assay Work?

What is a kinase assay
A kinase assay works by simply measuring the activity of the kinase. A kinase is an enzyme that aids in the transfer of a phosphate from ATP to another specific molecule. They regulate many activities in the human body. The measurement is used to test potential drugs to see how they affect kinase activity. An
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Transcreener ADP Assay Enables Evaluation of NIK Inhibitors in Lupus Drug Discovery

Lupus NIK Inhibitors
  Systemic lupus erythematosus (SLE), or lupus, takes a devastating toll. An autoimmune disease that triggers a dysfunctional immune system to attack its own tissues, SLE strikes young women most often — about 4 to 12 times more frequently than men — with women aged 15 to 45 being at highest risk. Both genetic and
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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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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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