Satellite Banner
Genomics
Scientific Community
 
Become a Member | Sign in
Home>News>This Article
  News
Return

Dimerix HIT Assay to Understand Receptor Interactions Applied to Kinase Targets

Published: Friday, May 31, 2013
Last Updated: Thursday, May 30, 2013
Bookmark and Share
Better understanding of receptor signalling, including effects arising from their functional interaction in heteromeric complexes, will progress drug development. Dimerix’s HIT assay is used to understand kinase heteromer signalling pathways.

Patents have now been granted for Dimerix’s Heteromer Investigation Technology (HIT) assay in the US, Europe, China and Australia, with applications pending in other jurisdictions.  Dimerix’s HIT assay enables a ligand responsive interrogation of a wide range of signalling pathways that can be triggered by a complex of at least two receptors (or proteins).  The assay can be utilised in high-throughput screening to obtain novel hits against the heteromer target and its components, or employed to better profile existing leads for signalling elicited through heteromer formation.  The broad application of Dimerix’s technology enables it to be licensed for a range of proximity-based reporter systems enabling optimal information and outcomes.

Most recently, an application of Dimerix’s assay to kinase heteromers has been reported.  A/Prof Kevin Pfleger, co-inventor of Dimerix’s assay technology, is senior author of a paper entitled ‘Profiling Epidermal Growth Factor Receptor and Heregulin Receptor Heteromerization Using Receptor Tyrosine Kinase Heteromer Investigation Technology’ published 20 May 2013 in PLOS ONE.

The study demonstrates the use of Dimerix’s HIT assay to investigate the heteromeric complexes formed by EGFR and HER3 receptors, and the effect on the Grb2 signalling pathway.  The data show that heteromerization of the receptors is required for HER3 to interact with Grb2, including evidence that this occurs via a transactivation mechanism.

Why is this important?  These kinase receptors are known to be involved in various human cancers.  Better understanding of receptor signalling, including effects arising from their functional interaction in heteromeric complexes, will progress drug development.  Indeed, the importance of EGFR-HER3 heteromerization has been demonstrated by other studies showing a beneficial effect of dual-action antibodies targeting both receptors. 

Dimerix’s assay not only provides a useful tool for interrogating heteromer signalling, but can also be used for high-throughput screening to identify hits against the heteromer as well as respective monomers.  In collaborative work with partners, Dimerix has enabled profiling and screening activities encompassing a range of proteins and signalling pathways.  Dimerix has strong expertise in the area of GPCRs and their various G-protein or beta-arrestin signalling pathways, including GPCR deorphanisation.

Dimerix’s internal research has used its assay in a core research program to develop an improved therapy for reduction of proteinuria in chronic kidney disease. Proteinuria is an indicator of ongoing kidney damage.

More information is available on Dimerix’s website: www.dimerix.com. To see a schematic of Dimerix’s assay for different reporter systems, please go to the Dimerix Platform section of our website.


Further Information
Access to this exclusive content is for Technology Networks Premium members only.

Join Technology Networks Premium for free access to:

  • Exclusive articles
  • Presentations from international conferences
  • Over 2,400+ scientific posters on ePosters
  • More than 3,700+ scientific videos on LabTube
  • 35 community eNewsletters


Sign In



Forgotten your details? Click Here
If you are not a member you can join here

*Please note: By logging into TechnologyNetworks.com you agree to accept the use of cookies. To find out more about the cookies we use and how to delete them, see our privacy policy.


Scientific News
Liquid Biopsies: Utilization of Circulating Biomarkers for Minimally Invasive Diagnostics Development
Market Trends in Biofluid-based Liquid Biopsies: Deploying Circulating Biomarkers in the Clinic. Enal Razvi, Ph.D., Managing Director, Select Biosciences, Inc.
10X Genomics Releases Linked-Read Data from NIST Genome Samples
Genome in a Bottle Consortium data submission for webinar presentation and public availability.
Environmental Epigenetics Affects Disease, Evolution
Researchers say environmental factors are having an underappreciated effect on the course of disease and evolution by prompting genetic mutations through epigenetics, a process by which genes are turned on and off independent of an organism’s DNA sequence.
Critical New Insights on DNA Repair
The enzyme fumarase is key to reversing genetic damage leading to cancer and therapy resistance.
Nanoparticles Used to Breach Mucus Barrier in Lungs
Proof-of-concept study conducted in mice is a key step toward better treatments for lung diseases.
Watching a Tumour Grow in Real-Time
Researchers from the University of Freiburg have gained new insight into the phases of breast cancer growth.
Childhood Cancer Cells Drain Immune System’s Batteries
Cancer cells in neuroblastoma contain a molecule that breaks down a key energy source for the body’s immune cells, leaving them too physically drained to fight the disease.
Urine Proteins Point to Early-Stage Pancreatic Cancer
A combination of three proteins found at high levels in urine can accurately detect early-stage pancreatic cancer, researchers at the BCI have shown.
Researcher Discovers Trigger of Deadly Melanoma
New research sheds light on the precise trigger that causes melanoma cancer cells to transform from non-invasive cells to invasive killer agents, pinpointing the precise place in the process where "traveling" cancer turns lethal.
Genetic Tug of War
Researchers have reported on a version of genetic parental control in mice that is more targeted, and subtle than canonical imprinting.
Skyscraper Banner

Skyscraper Banner
Go to LabTube
Go to eposters
 
Access to the latest scientific news
Exclusive articles
Upload and share your posters on ePosters
Latest presentations and webinars
View a library of 1,800+ scientific and medical posters
2,400+ scientific and medical posters
A library of 2,500+ scientific videos on LabTube
3,700+ scientific videos
Close
Premium CrownJOIN TECHNOLOGY NETWORKS PREMIUM FREE!