Unpuzzling DNMT3A as a Key Epigenetic Player

DNMT3A Actions in Epigenetics
DNA methyltransferase 3-alpha (DNMT3A) effects de novo cytosine methylation in embryonic and somatic cells through the transfer of a methyl group from S-Adenosyl-L-methionine (SAM) to the cytosine-C5 position of newly created CpG DNA residues. In somatic cells, 60 to 80% of these structures are methylated at any given time. Nonetheless, clusters of CpG residues (islands)
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METTL16: An RNA Methyltransferase That Wears Many Hats

RNA Methyltransferase METTL16 Performing Many Functions
Methyltransferase-like protein 16 (METTL16) is a recently characterized human RNA methyltransferase in the class I SAM-methyltransferase family. It methylates adenosine at the N6 position in a consensus sequence on U6 small nuclear RNA (U6 snRNA) and S-adenosylmethionine (SAM) synthetase (MAT2A) pre-mRNA to control the activity of these molecules. By regulating SAM homeostasis in a feedback
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PRMT5 is Innately Interesting

PRMT5 Role with Macrophages
PRMT5 is a type II arginine methyltransferase that dimethylates arginine residues symmetrically. Its various functions extend into T cell development, B cell regulation, hematopoiesis, and mitotic control. In the past, research on PRMT5 primarily focused on cancer and the adaptive immune response. These are both situations where metabolism and growth are critical. Recent reports implicate
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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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