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 […]
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 […]
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 […]
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 […]
It would be difficult to underestimate the importance of polo-like kinase 1 (Plk1) for cancer, given its influence on cell division. As one of five members of the Polo-like family of serine/threonine protein kinases in eukaryotic cells, Plk1 plays a multifaceted role in the cell cycle and thus controls cancer progression fueled by unchecked cell […]
Aurora A Kinase in Cancer Drug Development Aurora A Kinase, along with -B and -C, are members of a family of serine/threonine protein kinases that play critical roles in coordinating mitosis, including establishment of the mitotic spindle, centrosome duplication, centrosome separation as well as maturation, chromosomal alignment, spindle assembly checkpoint, and cytokinesis. The enzyme’s role […]
Imagine viewing the plasma membrane of a cell from an interior perspective, with a front-row seat to the process by which substances enter the cell. Over in one corner, the plasma membrane begins to bulge inward, forming a sphere stretching toward you with a droplet-shaped neck on the opposite side that remains connected to the […]
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