The Contribution of DNA Methyltransferase Inhibitors in Treating Myelodysplastic Syndromes

DNA Methyltransferase Inhibitors for MDS
Myelodysplastic syndromes (MDS) are a broad, complex group of cancers characterized by the inability to form mature, healthy blood cells. There are different types with varying degrees of risk associated, making it difficult to diagnose and treat. Additionally, many patients are symptom-free and at an older age where they are likely to have other life-threatening
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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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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
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Creating a Methyltransferase HTS Assay Using an SAH Riboswitch Part II

In Part I of II in this blog series, discussion included the challenges of screening methyltransferases, steps in developing an SAH assay, the experimental assay procedure, assay sensitivity, and reagent stability. Please view the previous post here: Creating a Methyltransferase HTS Assay Using an SAH Riboswitch Part I. Compatibility with Diverse MT Accepter Substrates As
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Creating a Methyltransferase HTS Assay Using an SAH Riboswitch Part I

Riboswitches were discovered in 2002 by Ron Breaker at Yale as RNA-based intracellular sensors of vitamin derivatives. During the last decade, riboswitches have been identified that bind a range of small biomolecules including nucleotides, amino acids, and ions. Riboswitches exert regulatory control of transcription, translation, splicing, and RNA stability. BellBrook scientists used a riboswitch that
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BellBrook Labs Receives NIH Funding to Commercialize Methyltransferase Assays for Epigenetic Drug Discovery

BellBrook Labs has been awarded an $860,000 Phase II SBIR grant from the National Institutes of General Medical Sciences to develop an innovative methyltransferase assay for epigenetic drug discovery.  The company’s scientists engineered a fluorescent light switch into a bacterial metabolite sensor to leap-frog the limitations of conventional reagents. Madison, WI – August 31, 2016
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