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Category: Epigenetics

PRMT5 is Innately Interesting

Wednesday, 30 March 2022 by Bellbrook Labs
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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  • Published in Emerging Targets, Epigenetics, Innate Immunity
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The Contribution of DNA Methyltransferase Inhibitors in Treating Myelodysplastic Syndromes

Tuesday, 01 October 2019 by Bellbrook Labs
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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  • Published in Emerging Targets, Epigenetics
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Sensitive Methyltransferase Assay Proves Successful with PRMT4

Thursday, 11 October 2018 by Bellbrook Labs
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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  • Published in Epigenetics, HTS Assays
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A Novel Approach Discovers Hundreds of Cancer-Relevant Arginine Methylation Sites for CARM1

Thursday, 14 December 2017 by Bellbrook Labs
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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  • Published in Epigenetics, HTS Assays, Products, Uncategorized
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BellBrook Labs Launches Ultra-Sensitive Methyltransferase Assay to Accelerate Epigenetic Drug Discovery

Thursday, 10 August 2017 by Bellbrook Labs
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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  • Published in Epigenetics, News, Uncategorized
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Previously Recorded Webinar – The New AptaFluor™ SAH Methyltransferase Assay: A Homogenous, Universal Assay Based on a Microbial Riboswitch

Monday, 31 July 2017 by Bellbrook Labs
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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  • Published in Epigenetics, HTS Assays, Products
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EZH2 Methyltransferase Inhibitors Hold Promise for Combating Neuropathic Pain

Friday, 21 July 2017 by Bellbrook Labs
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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  • Published in Emerging Targets, Epigenetics, HTS Assays
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BellBrook Labs Awarded NIH Funding for Collaboration with University of Utah to Develop Biosensors for Epigenetic Drug Discovery

Monday, 12 December 2016 by Bellbrook Labs
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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  • Published in Epigenetics, HTS Assays
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Creating a Methyltransferase HTS Assay Using an SAH Riboswitch Part II

Wednesday, 19 October 2016 by Bellbrook Labs
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

Friday, 23 September 2016 by Bellbrook Labs
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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