Quick Answer: Methyltransferases (MTs) are high‑value drug targets across epigenetics, virology, oncology, and RNA biology. The most reliable, scalable way to measure MT activity for high‑throughput screening (HTS) is to detect S‑adenosyl‑L‑homocysteine (SAH), the universal product of MT reactions. Among SAH‑detection methods, AptaFluor® SAH Methyltransferase Assays provide a direct, mix‑and‑read TR‑FRET readout with ultra‑low‑nanomolar sensitivity […]
New Publication By BellBrook Scientists – Development and Validation of a Generic Methyltransferase Enzymatic Assay Based on an SAH Riboswitch A group of BellBrook scientists was recently published in SLAS Discovery for their research, “Development and Validation of a Generic Methyltransferase Enzymatic Assay Based on an SAH Riboswitch.” In this article, scientists demonstrate the development […]
KMT2B (Lysine [K] Methyltransferase 2B) or Mixed Lineage Leukemia 2 protein (MLL2) is a mammalian histone H3 lysine 4 (H3K4) methyltransferase. It readily forms complexes with WRAD, host cell factors 1 and 2, and Menin. These complexes confer H3K4 trimethylation to specific gene promoters and some enhancers to regulate bivalent developmental genes and stem cell/germ […]
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) […]
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 […]
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 […]
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 […]
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 […]
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 […]
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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