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

New Posters from DOT 2017

Poster Presentations A Homogenous, High Throughput Assay to Measure Guanine Nucleotide Exchange Factor Activity Using Transcreener® GDP Assay Guanine nucleotide exchange factors (GEFs) positively regulate Rho GTPases by accelerating GDP dissociation to allow formation of the active, GTP-bound complex. Development of inhibitors that specifically disrupt GEF action on a target Rho GTPase may be a

Discovery on Target 2017

  Here is what you may have missed… Exhibition Learn about our new AptaFluor SAH Methyltransferase Assay Discuss which HTS assays might be a fit for your research Discover how BellBrook Labs’ services can help accelerate your drug discovery program Presentations/Talks Targeting the cGAS-STING Pathway Using a Homogenous, HTS Compatible Transcreener® cGAS Assay Thursday, September
Classically speaking, assays for interactions between drug molecules and their targets have measured binding affinity under equilibrium conditions. In drug discovery projects, it had long been assumed that carefully measuring IC50 (half-maximal inhibitory concentration), EC50 (effector concentration for half-maximal response), Kd  (equilibrium dissociation constant), and/or Ki (inhibition constant) would allow drug candidates to be prioritized
Methyltransferases have become a major focus of drug discovery for cancer and other diseases driven by epigenetic factors.  BellBrook Labs’ new, ultra-sensitive AptaFluor™ SAH Methyltransferase Assay eliminates cost and sensitivity barriers that are slowing the discovery of methyltransferase inhibitors. New AptaFluor SAH Methyltransferase Assay Schematic BellBrook Labs announces the launch of their latest drug discovery
Epigenetic regulation has been shown to be a contributing factor in a variety of diseases, and discovery of methyltransferase inhibitors is an area of intense activity. Methyltransferase enzymes methylate a variety of substrates using S-adenosylmethionine (SAM) as the methyl donor leaving S-adenosylhomocysteine (SAH) as a common product. Since the difference between SAH and SAM is
When people experience neuropathic pain, they often describe “pins and needles” sensations or burning, shooting, or stabbing pain that can be agonizing and difficult to bear. In some cases, neuropathic pain is so intense that the pressure of clothing or the weight of a bed sheet can cause misery. Chronic neuropathic pain can be caused
Glycan structures decorate a wide variety of cell types—dotting the surface of blood cells, linked to lipid moieties on neurons, and studding the membrane of tumor cells. These carbohydrate structures create a cellular language that is translated by binding partners, eliciting specific downstream effects. And for some cancers, the effects can be devastating.   Consider
BellBrook Labs was recently awarded a $288,000 SBIR Phase I grant from the National Institutes of General Medical Sciences (NIGMS) to develop an HTS assay for cyclic GAMP synthase, an enzyme that triggers immune responses to viruses and tumors. The new assay will be used in an effort to screen for cGAS enzyme modulators as
TOP