The Multifaceted Roles of IRE1 Are Unfolding

IRE1 Proteins in ER
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
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TYK2 Inhibition Finally Comes of Age

TYK2 Inhibition Discovery
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
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Five Considerations When Choosing a Biochemical Assay Development Services CRO

Assay Development Services - Two Scientists Working In the Lab
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
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A Novel Approach Discovers Hundreds of Cancer-Relevant Arginine Methylation Sites for CARM1

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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Doubling the Odds: Two-Pronged Strategy to Halt Cancer Cell Proliferation

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
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Newly Patented Aurora A Kinase Inhibitor a Promising Contender for Cancer Treatment

Aurora A Kinase in Cancer Drug Development Aurora A Kinase, along with -B and -C, are members of a family of serine/threonine protein kinases that play critical roles in coordinating mitosis, including establishment of the mitotic spindle, centrosome duplication, centrosome separation as well as maturation, chromosomal alignment, spindle assembly checkpoint, and cytokinesis. The enzyme’s role
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Using the Transcreener® GDP Assay to Discern the Truth about Dynamin Inhibitors

Imagine viewing the plasma membrane of a cell from an interior perspective, with a front-row seat to the process by which substances enter the cell. Over in one corner, the plasma membrane begins to bulge inward, forming a sphere stretching toward you with a droplet-shaped neck on the opposite side that remains connected to the
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New Posters from DOT 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
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Taking Up Residence: Using the Transcreener ADP Assay to Measure the Kinetics of Kinase Inhibitor Interactions

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
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BellBrook Labs Awarded NIH Grant to Develop a High Throughput cGAS Assay for Cancer and Autoimmune Disease Drug Discovery

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
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