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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Sensitive Methyltransferase Assay Proves Successful with PRMT4

Histone Methylation PRMT4
Histone methyltransferases (HMTs) play a critical role in many diseases. Dysregulation of histone methylation and the subsequent alterations in epigenetic states can cause gene expression patterns that drive a variety of cancers,[1] endometriosis,[2] osteoporosis,[3] osteoarthritis and rheumatoid arthritis,[4] cardiovascular disease,[5] and autism,[6] to name only a few. In this light, a global assay for HMT
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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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BellBrook Labs Launches Ultra-Sensitive Methyltransferase Assay to Accelerate Epigenetic Drug Discovery

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
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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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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
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Posters and Presentations from DOT 2016

Did you miss the DOT 2016 meeting in Boston or would like a recap? View the posters and presentations from BellBrook’s scientists below. Posters: Aptamer Based Homogenous Single-Reagent HTS Assay Platform for Human Growth Factors Aniket, Elizabeth Vu, Meera Kumar, Tom Zielinski, Justin Brink, and Robert G. Lowery Determination of Drug Residence Time in a
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Discovery on Target Conference 2016

Discovery on Target 2016 September 19-22 Westin Boston Waterfront Boston, MA Exhibition Visit Booth #24 to: Discuss BellBrook’s current HTS assays. Share your thoughts on the future of drug discovery. Learn about upcoming AptaFluor™ HTS assays! Presentations/Talks AptaFluor™ Methyltransferase Assay: A Homogenous, Universal HMT Assay Based on a Microbial Riboswitch Tuesday, September 20th – 3:15PM Poster
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Inhibition of Methyltransferase SMYD3 Targets Ras-driven Cancers

The methyltransferase SMYD3 is overexpressed in several tumor types, and its overexpression correlates with aggressiveness in breast carcinoma.    Its epigenetic role has been investigated extensively: SMYD3 methylates histone H4 at K5, stimulating expression of critical oncogenic proteins that drive cell proliferation, invasion and metastasis.  However, it has recently been discovered that SMYD3 also methylates non-histone
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Digging into Dopamine Signaling: Arginine Methylation Regulates GPCRs

The neurotransmitter dopamine is one of the most fascinating substances regulating behavior, with both delightful and dark qualities. Affecting a mere 20,000 dopamine-responsive neurons out of 100 billion neurons in the human brain, dopamine nonetheless governs critical aspects of our existence including voluntary movement, psychosis, and addiction. Disrupted dopamine signaling is involved in maladies ranging
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