Corporate Banner
Satellite Banner
Biomolecular Screening
Scientific Community
Become a Member | Sign in
Home>News>This Article

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: 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 2,600+ scientific posters on ePosters
  • More than 3,800+ 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 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
Potential Target for Treatment of Autism
Grant of $2.4 million will support further research.
Sniffing Out Cancer
Scientists have been exploring new ways to “smell” signs of cancer by analyzing what’s in patients’ breath.
Inroads Against Leukemia
Potential for halting disease in molecule isolated from sea sponges.
Molecular ‘Kiss Of Death’ Flags Pathogens For Destruction
Researchers have discovered that our bodies mark pathogen-containing vacuoles for destruction by using a molecule called ubiquitin, commonly known as the "kiss of death."
A New Single-Molecule Tool to Observe Enzymes at Work
A team of scientists at the University of Washington and the biotechnology company Illumina have created an innovative tool to directly detect the delicate, single-molecule interactions between DNA and enzymatic proteins.
Milestone Single-Biomolecule Imaging Technique May Advance Drug Design
The first nanometer resolved image of individual tobacco mosaic virions shows the potential of low-energy electron holography for imaging biomolecules at a single particle level; a milestone in structural biology and a potential new tool for drug design.
Multi-Gene Test Enables Some Breast Cancer Patients to Safely Avoid Chemotherapy
A major study is providing the best evidence to date that a 21-gene test done on the tumor can identify breast cancer patients who can safely avoid chemotherapy.
Antidepressants Plus Blood-Thinners Slow Down Brain Cancer
EPFL scientists have found that combining antidepressants with anticoagulants slows down brain tumors (gliomas) in mice.
Diagnostics Breakthrough Brings Viral Sequencing to Doctors’ Toolkit
New screening tool produces up to 10,000-fold improvement in viral matches compared with traditional high-throughput methods.
New Virus Identified In Blood Supply
Scientists have discovered a new virus that can be transmitted through the blood supply.

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
2,600+ scientific and medical posters
A library of 2,500+ scientific videos on LabTube
3,800+ scientific videos