The Multifaceted Roles of IRE1 Are Unfolding
Wednesday, 09 March 2022
IRE1 (Inositol-Requiring Enzyme 1) is one of three resident transmembrane endoplasmic reticulum (ER) proteins that sense and signal distress from improper protein synthesis and conformation. (While IRE1 alpha is almost universally expressed and IRE1 beta is confined to the gut, both will be conflated as IRE1 here.) Secreted and transmembrane proteins are primarily produced in
- Published in Emerging Targets, Innate Immunity
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Five Considerations When Choosing a Biochemical Assay Development Services CRO
Monday, 28 September 2020
There are many options out there for choosing assay development services, and finding what you need can be a challenging endeavor. Here we outline five items to look for when searching for the CRO that is right for your project. To narrow things down a bit, this article will focus on biochemical assay development services
- Published in Resources
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
Doubling the Odds: Two-Pronged Strategy to Halt Cancer Cell Proliferation
Wednesday, 29 November 2017
It would be difficult to underestimate the importance of polo-like kinase 1 (Plk1) for cancer, given its influence on cell division. As one of five members of the Polo-like family of serine/threonine protein kinases in eukaryotic cells, Plk1 plays a multifaceted role in the cell cycle and thus controls cancer progression fueled by unchecked cell
- Published in HTS Assays, News, Uncategorized
New Posters from DOT 2017
Friday, 29 September 2017
Poster Presentations A Homogenous, High Throughput Assay to Measure Guanine Nucleotide Exchange Factor Activity Using Transcreener® GDP Assay Guanine nucleotide exchange factors (GEFs) positively regulate Rho GTPases by accelerating GDP dissociation to allow formation of the active, GTP-bound complex. Development of inhibitors that specifically disrupt GEF action on a target Rho GTPase may be a
- Published in HTS Assays, News
Taking Up Residence: Using the Transcreener ADP Assay to Measure the Kinetics of Kinase Inhibitor Interactions
Wednesday, 30 August 2017
Classically speaking, assays for interactions between drug molecules and their targets have measured binding affinity under equilibrium conditions. In drug discovery projects, it had long been assumed that carefully measuring IC50 (half-maximal inhibitory concentration), EC50 (effector concentration for half-maximal response), Kd (equilibrium dissociation constant), and/or Ki (inhibition constant) would allow drug candidates to be prioritized
- Published in HTS Assays, Uncategorized
BellBrook Labs Launches Ultra-Sensitive Methyltransferase Assay to Accelerate Epigenetic Drug Discovery
Thursday, 10 August 2017
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
- Published in Epigenetics, News, Uncategorized
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