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
No Comments
TYK2 Inhibition Finally Comes of Age
Tuesday, 01 February 2022
Tyrosine kinase 2 (TYK2) was the first of the Janus family of non-receptor tyrosine kinases to be discovered. For three decades, the other members of this family, JAK1, JAK2, and JAK3, have dominated the research for inhibitors of autoimmune disease, largely because the effect upon them was more pronounced. They are called “Janus kinases” because
- Published in Emerging Targets, Innate Immunity
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 Awarded NIH Grant to Develop a High Throughput cGAS Assay for Cancer and Autoimmune Disease Drug Discovery
Wednesday, 14 June 2017
BellBrook Labs was recently awarded a $288,000 SBIR Phase I grant from the National Institutes of General Medical Sciences (NIGMS) to develop an HTS assay for cyclic GAMP synthase, an enzyme that triggers immune responses to viruses and tumors. The new assay will be used in an effort to screen for cGAS enzyme modulators as
- Published in Emerging Targets, HTS Assays, News
- 1
- 2