How a Methyltransferase Activity Assay Could Help Identify Novel Breast Cancer Treatments

Pink Stethascope DOT1L Breast Cancer Target 420 X 280
As estrogen receptor (ER) positive breast cancer (BC) becomes resistant to antiestrogen therapy, novel ways to control the disease are and continue to be developed. There are different types of breast cancer, and the most effective treatment depends on knowing this difference.  For example, if the type is estrogen receptor positive (ER) meaning cells are
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Acetyl-CoA Carboxylase Inhibitors: Transcreener ADP Assay Powers Drug Detection Strategy

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
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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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Transcreener ADP Assay Aids in Discovery of RIPK2 Inhibitors for Autoinflammation

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
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A Novel Approach Discovers Hundreds of Cancer-Relevant Arginine Methylation Sites for CARM1

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
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Newly Patented Aurora A Kinase Inhibitor a Promising Contender for Cancer Treatment

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
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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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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
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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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Another Tool for the HTS Toolbox: Two Additional Plate Readers Certified for Transcreener Assays

Increased instrumentation costs and limited budgets mean that most HTS labs rely on a single type of multimode plate reader, which may limit the detection modes that can be used.  The ability of an assay technology to generate different types of readouts and perform well on a variety of plate readers is certainly an asset
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