The Challenging Search for BTK Inhibitors
Tuesday, 27 December 2022
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,
- Published in Emerging Targets, HTS Assays, Innate Immunity
Can WRN Helicase Inhibitors Treat MSI-H Cancers?
Tuesday, 04 October 2022
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
- Published in Emerging Targets, HTS Assays, Innate Immunity
Webinar: Targeting Kinases Involved in the Innate Immune Response
Wednesday, 13 October 2021
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
- Published in Emerging Targets, HTS Assays, Innate Immunity
IKK Complex, NF-kB, and Inflammation – An Intricate Relationship
Tuesday, 07 September 2021
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
- Published in Emerging Targets, Innate Immunity
Using a PKR Inhibitor Assay in the Fight Against Viruses
Tuesday, 01 June 2021
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
- Published in Emerging Targets, HTS Assays, Innate Immunity
Finding Inhibitors for a Cancer Target: CDK12 Activity Assays Accelerate the Search
Tuesday, 03 December 2019
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
- Published in Emerging Targets, HTS Assays
Using TBK1 Inhibitors to Stop Cancer in Its Tracks
Tuesday, 29 October 2019
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
- Published in Emerging Targets