Transcreener® ADP2 Assay Delivers Precise Measurement of Functional MAPK14 Residence Time

Calculating MAPK14 Residence Time
Researchers at the University of Tubingen use Transcreener to uncover how residence time works on a molecular level with p38α MAPK Inhibitors – Many factors affect the effectiveness of ligand-substrate or drug-target interactions. Conformational docking and stearic considerations help inform optimal “fits.” Ligand moiety solubility, both in free and bound forms, is also a consideration
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The Challenging Search for BTK Inhibitors

BTK's Involved in Systemic lupus erythematosus
Bruton’s Tyrosine Kinase (BTK) is a 76kDa non-receptor Tec kinase that plays numerous diverse roles in B-cell development, immunity, autoimmunity, infection, and cancer. From stem to stern, it consists of an N-terminal plekstrin homology (PH) domain, a TEC homology (TH) domain, two SRC homology (SH2 and SH3) domains, and a C-terminal kinase domain. Unlike SRC,
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Can WRN Helicase Inhibitors Treat MSI-H Cancers?

Patient With WRN Helicase Syndrome
Over 100 years ago, Otto Werner first characterized a recessive autosomal disorder that caused premature, but largely typical, aging in adults, starting by the 3rd decade and resulting in death by the 6th decade via myocardial infarction or cancer. This disease, now known as Werner syndrome, is caused by specific alterations in the 162 KDa
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Webinar: Targeting Kinases Involved in the Innate Immune Response

Abstract: Clinical trials continue to determine whether therapeutic modulation of kinases can be used to suppress the immune system in autoimmune diseases or stimulate for antiviral and cancer immunotherapy. The discovery and characterization of small molecule modulators have aided these efforts. The Transcreener ADP² Kinase Assay meets this need as it relies on direct ADP
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IKK Complex, NF-kB, and Inflammation – An Intricate Relationship

IKK Complex & Inflammation
Components of the IKK Complex The IκB kinase (IKK) complex consists of two catalytic subunits IKKα (IKK1) and IKKβ (IKK2), as well as a non-catalytic accessory protein IKKγ. IKKγ is also known as NF-κB essential modulator (NEMO). IKKα and IKKβ have high sequence homology and hence, are structurally similar. Both of those subunits possess phosphorylating
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Using a PKR Inhibitor Assay in the Fight Against Viruses

PKR Inhibitor Blog
Can a novel PKR inhibitor help lead to new treatments for viral infections? –  While the human immune response is astounding and works hard to keep us alive in the face of the many germs we encounter daily, it is exceedingly complex. Unlike the adaptive immune response, the innate response acts quickly. It is considered
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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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