HTS Assays Archives - Page 16 of 18

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 […]

September 29, 2017

HTS Assays, Uncategorized

Taking Up Residence: Using the Transcreener ADP Assay to Measure the Kinetics of Kinase Inhibitor Interactions

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 […]

August 30, 2017

Epigenetics, HTS Assays, Products

Previously Recorded Webinar – The New AptaFluor™ SAH Methyltransferase Assay: A Homogenous, Universal Assay Based on a Microbial Riboswitch

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 […]

July 31, 2017

Emerging Targets, Epigenetics, HTS Assays

EZH2 Methyltransferase Inhibitors Hold Promise for Combating Neuropathic Pain

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 […]

July 21, 2017

Emerging Targets, HTS Assays, News

BellBrook Labs Awarded NIH Grant to Develop a High Throughput cGAS Assay for Cancer and Autoimmune Disease Drug Discovery

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 […]

June 14, 2017

Emerging Targets, HTS Assays, Uncategorized

Ectonucleotidases: An Outside Chance for Drug Development

Sometimes, the most intriguing cellular processes happen outside of the cell. Case in point: purinergic signaling pathways, in which extracellular receptors sense levels of purines in the extracellular milieu. The result? A wide array of effects on neuronal signaling, vascular tone, thrombosis, and immune function. But what controls the level of extracellular purines? Enter ectonucleotidases: […]

April 28, 2017

Company, HTS Assays, News

New Publication: HTS Method for Measuring Drug Residence Time

View our latest publication, “A High-Throughput Method for Measuring Drug Residence Time Using the Transcreener® ADP2 Assay” in SLAS Discovery. Inhibitor residence times are increasingly being used to prioritize molecules early in lead discovery programs. Current methods for determining residence time are low-throughput or require the synthesis of labeled ligands. Our goal was to create […]

April 25, 2017

Company, HTS Assays, Products

Detecting Rho-GEF Activity Using the Transcreener® GDP Assay

Rho GTPases act as molecular switches to regulate the cytoskeletal dynamics underlying cell motility. Rho GEFs (guanine nucleotide exchange factors) positively regulate Rho GTPases by accelerating GDP dissociation and allowing formation of the active GTPase-GTP complex. Active Rho GTPases typically stimulate cell growth and migration, sometimes triggering tumorigenesis or invasion. Selectively disrupting GEF action using […]

March 24, 2017

Epigenetics, HTS Assays

BellBrook Labs Awarded NIH Funding for Collaboration with University of Utah to Develop Biosensors for Epigenetic Drug Discovery

BellBrook Labs was awarded a Phase I grant of $225,000 to develop biosensors for detection of chromatin modifying enzymes, such as acetyltransferases and methyltransferases, in collaboration with University of Utah chemist Jennifer Heemstra. The collaboration leverages nucleic aptamer technology being developed by Dr. Heemstra to streamline development of assays for epigenetic enzymes being targeted for […]

December 12, 2016

HTS Assays

Kinase Assays and Applications in Cancer Therapeutic Discovery

The ABL1 gene is a special type of gene that encodes a protein tyrosine kinase. It is involved in various cellular processes, including but not limited to cell adhesion, cell division, and cell differentiation. This protein’s activity is adversely regulated by its SH3 domain, which involves the deletion of the region that encodes the domain […]

November 30, 2016