A Novel Approach Discovers Hundreds of Cancer-Relevant Arginine Methylation Sites for CARM1
Thursday, 14 December 2017
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
- Published in Epigenetics, HTS Assays, Products, Uncategorized
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EZH2 Methyltransferase Inhibitors Hold Promise for Combating Neuropathic Pain
Friday, 21 July 2017
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
- Published in Emerging Targets, Epigenetics, HTS Assays
Inhibition of Methyltransferase SMYD3 Targets Ras-driven Cancers
Wednesday, 04 May 2016
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
- Published in Emerging Targets
Digging into Dopamine Signaling: Arginine Methylation Regulates GPCRs
Monday, 25 January 2016
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
- Published in Emerging Targets
Preparing for the Epigenevitable
Tuesday, 14 July 2015
Epigenetic drug discovery has generated a lot of excitement in the past few years, and many stakeholders are eagerly awaiting clinical results for the first two histone methyltransferase (HMT) inhibitor drugs, which target Dot1L and EZH2. The analogies with kinase drug discovery, i.e., targeting oncogenic gain-of-function driver mutations in enzymes that catalyze post-translational modifications, helped
- Published in Epigenetics
New Publication: Optimizing Histone Methyltransferase Assays
Tuesday, 09 June 2015
See our latest publication, “Biochemical Assay Development for Histone Methyltransferases Using a Transcreener-Based Assay for S-Adenosylhomocysteine” in Assay and Drug Development Technologies Screening or profiling histone methyltransferases (HMTs) can often require challenging assay development. Their complex enzyme and substrate requirements compound the difficulties imposed by their unusual (read SLOW) kinetic properties. In a recent study
- Published in News
DNA Methylation Modulates Alcohol Addiction
Wednesday, 13 May 2015
Alcoholism is a multifaceted disorder caused by both genetic and environmental influences and epigenetic modifications, including histone acetylation and DNA methylation, have been shown to control alcohol-related behaviors. In a recent study, Estelle Barbier, from Linköping University in Sweden, collaborated with scientists at NIH to begin to understand how DNA methylation contributes to the lasting
- Published in Epigenetics
Ensuring Assay Success: The Right Plate Makes All The Difference
Thursday, 19 June 2014
Transcreener® HTS Assays rely on direct immunodetection of nucleotides with a far-red readout in a simple mix-and-read format. The assays are available in three different detection modes, fluorescence polarization (FP), fluorescence intensity (FI), and time-resolved Forster resonance energy transfer (TR-FRET). A good microplate reader and the right choice of plates to differentiate specific signal versus
- Published in HTS Assays
Epigenetics: Making Bad Memories a Thing of the Past?
Thursday, 06 February 2014
Traumatic events generate some of the most enduring forms of memories. Extreme physical or psychological harm often leads to the development of PTSD or other fear and anxiety-related disorders. Not only are these memories intensely painful, they are also extremely difficult to treat with behavioral therapy. A recent study by a group of researchers based
- Published in Epigenetics
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