Small GTPase Modulation: GDP Assays to Accelerate Discovery

Small GTPase Modulation
Cancer is complex, which makes determining the culprit as well as individual treatment extremely challenging. A variety of cancer types exist with a multitude of contributors. As the second leading cause of death in the US, cancer has been a target scientists have been battling for decades. When DNA is damaged or mutations occur, cells
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FUT7, Inflammation, and Fucosyltransferase Assays

FUT7 Fucosyltransferase Assays and Chronic Inflammation
Inflammation is a necessary step involved in the immune response, allowing our bodies to fight and eliminate disease, allergies, and injuries. The inflammatory response recruits several mediators to aid in the destruction of whatever pathogen caused the response in the first place. Cells such as leucocytes, eosinophils, and neutrophils get recruited to the site in
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Researchers Employ GTPase Assay to Investigate Rab Proteins

Scientist Using a GTPase Assay
Measuring Rab interaction with a GTPase Assay – GTPases are in the limelight in biology and drug discovery because of their role in a wide range of cellular processes and functions.  They are highly conserved regulatory proteins involved in such diverse roles as signal transduction, protein biosynthesis, cell adhesion, membrane remodeling and trafficking, cytoskeletal reorganization,
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Researchers from BellBrook Labs Pen Chapter in Springer’s Rho GTPases: Methods and Protocols

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
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Using the Transcreener® GDP Assay to Discern the Truth about Dynamin Inhibitors

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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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
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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
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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
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BellBrook Labs Awarded NIH Grant to Validate New Target for Liver Fibrosis Using Transcreener GTPase Assay Platform

BellBrook Labs was awarded a Phase I Small Business Innovative Research (SBIR) grant of $353,000 from the National Institute on Alcohol Abuse and Alcoholism for pharmacological validation of GIV, a nonreceptor guanine nucleotide exchange factor (GEF), as a therapeutic target for liver fibrosis.  BellBrook will use proprietary high throughput GTPase assay methods to identify small
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Unraveling RhoGDIα Regulation

Rho proteins are small, monomeric GTPases in the Ras superfamily that control cell shape and motility by regulating cytoskeletal dynamics. They cycle between a GDP-bound inactive state and a GTP-bound active state. When in the active state, Rho proteins bind to effectors at the plasma membrane, which regulate cellular processes such as cell architecture, intracellular
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