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
Read more
No Comments

Transcreener ADP Assay Enables Evaluation of NIK Inhibitors in Lupus Drug Discovery

Lupus NIK Inhibitor
  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
Read more
No Comments

Sensitive Methyltransferase Assay Proves Successful with PRMT4

Histone Methylation PRMT4
Histone methyltransferases (HMTs) play a critical role in many diseases. Dysregulation of histone methylation and the subsequent alterations in epigenetic states can cause gene expression patterns that drive a variety of cancers,[1] endometriosis,[2] osteoporosis,[3] osteoarthritis and rheumatoid arthritis,[4] cardiovascular disease,[5] and autism,[6] to name only a few. In this light, a global assay for HMT
Read more
No Comments

Acetyl-CoA Carboxylase Inhibitors: Transcreener ADP Assay Powers Drug Detection Strategy

Acetyl CoA Carboxylase Inhibitors
The impact of Acetyl-CoA carboxylases (ACCs) on eukaryotic metabolism and metabolic-related disease states is profound. ACCs catalyze the formation of malonyl-CoA by ATP-dependent carboxylation of acetyl-CoA. In humans, the two isoforms of ACC exhibit highly regulated, tissue-specific patterns of expression, with ACC1 being present in lipogenic tissues such as liver and adipose, and ACC2 being
Read more
No Comments

A Guide to Measuring Drug-Target Residence Times with Biochemical Assays

Residence Time Guide
Learn How to Determine Drug-Target Residence Times with Biochemical Assays in this Free Guide Drug-target residence time has become a critical component in the discovery of new therapeutics. BellBrook Labs has recently published a guide to help describe the use of a proven “jump-dilution” method along with BellBrook’s Transcreener Assay platform to help streamline efforts
Read more
No Comments

ABC Transporter MsbA Inhibitors Discovered to Help Fight Against Gram-Negative Bacteria

ABC Transporter Inhibitor Klebsiella Treatment
Gram-negative bacterial pathogens pose grave dangers in clinical and environmental settings alike. They include foodborne disease pathogens such as E. coli 0157:H7, waterborne pathogens such as Vibrio cholera, vector-borne pathogens such as Yersinia pestis, and a disturbingly large number of Gram-negative pathogens that now display resistance to multiple antimicrobial agents.1 Resistant Gram-negative pathogens include some
Read more
No Comments

Enhancing Checkpoint Blockade Immunotherapy: Sensitizing Tumors with HSP90 Inhibitors

HSP90 Inhibitor Immunotherapy
Checkpoint blockade is turning heads in the oncology community. This form of immunotherapy, which uses anti-PD-1 or anti-CTLA-4 antibodies to coax the immune system into recognizing and attacking cancer cells, has been a game-changer — but only for some patients. Types of cancer for which checkpoint blockade currently cannot presently be used include gastrointestinal tumors
Read more
No Comments

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
Read more
No Comments

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
Read more
No Comments

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
Read more
No Comments