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
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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
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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
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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
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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
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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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