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
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
Rho GTPases Rho GEFs Book
New Protocol from BellBrook Labs: High-Throughput Assay for Rho GEFs Based on the Transcreener GDP Assay In this new second edition of Springer Nature’s Rho GTPases: Methods and Protocols, researchers from BellBrook Labs describe an HTS compatible method for detecting GTPase exchange factor (GEF) activity. The protocol described in chapter twelve of the book uses
Discovery on Target 2018
BellBrook Labs will exhibit and present posters at the upcoming Discovery on Target conference in Boston, MA. At the event BellBrook will demonstrate applications for its suite of high throughput screening tools, including residence time determination, methyltransferase activity measurement, studying ectonucleotidase enzymes, screening for kinase inhibitors, and more! Discovery on Target 2018 Sheraton Boston Hotel
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
Autoimmune Disease News
The National Institutes of General Medical Sciences (NIGMS) recently awarded BellBrook Labs a $1 million phase II Small Business Innovative Research (SBIR) grant to develop new assays to detect cyclic GMP-AMP (cGAMP) levels in biological samples. The assays will be used to discover, develop, and monitor new treatments for autoimmune diseases and cancer by targeting
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
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
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
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