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

Domainex Researchers Identify Small-Molecule Inhibitors of TBK1/IKKepsilon Affecting IL-17 Signaling

Published: Monday, November 05, 2012
Last Updated: Monday, November 05, 2012
Bookmark and Share
Inhibitors may have utility in autoimmune disease treatment.

Domainex Ltd. has developed a number of chemical series with potent and selective activity against two closely-related kinases TBK1 and IKKepsilon.

IL-17 mediated signaling is known to induce the expression of cytokines and other effectors that can cause a variety of immunological diseases such as psoriasis and Chronic Obstructive Pulmonary Disease (COPD).

Domainex researchers are now the first to report that small-molecule inhibitors of TBK1/IKKepsilon are able to affect IL-17 signaling.

These results suggest that the Domainex inhibitors may have utility in a wide range of clinically-important diseases that have great unmet medical needs.

Recent clinical studies reported in The New England Journal of Medicine by Lilly and Amgen have shown that neutralizing anti-IL-17 monoclonal antibodies can have a major impact on psoriasis (Leonardi et al. 2012 and Papp et al. 2012 respectively).

The demonstration by Domainex that small-molecule drugs targeting IKKepsilon can inhibit IL-17 signaling indicates that these compounds have great clinical potential in this disease and other important settings.

Domainex has developed three series of drug-like compounds, each series having inhibitors with high potency and selectivity against other kinases.

The lead compounds have good metabolic properties and the Company is now driving these compounds forwards towards a clinical candidate.

Domainex's Research Director, Trevor Perrior, said: "Domainex, in collaboration with The Institute of Cancer Research, has previously shown that its inhibitors of TBK1/IKKepsilon have activity against a variety of cancer cell-lines. Domainex has also demonstrated that its inhibitors are very potent blockers of interferon-beta production in immune cells, showing the compounds may have utility in diseases such as lupus. The latest finding that our TBK1/IKKepsilon inhibitors can also inhibit IL-17 signaling suggests that the compounds are also of potential use for treatment of other major diseases such as psoriasis and COPD. Domainex has recently obtained funding from the government-backed Biomedical Catalyst programme to explore the use of its inhibitors of IKKepsilon in COPD."

Eddy Littler, CEO of Domainex, said: "The latest results showing the activity of Domainex's TBK1/IKKepsilon inhibitors against IL-17 signaling reinforces the fact that this project is of very high interest to pharma. Indeed Domainex is already in discussion with a number of potential partners with a view to them helping us to progress the programme to the clinic, and fully exploit its enormous potential. We are also grateful for the Biomedical Catalyst award that will enable us to extend our work to COPD, and help us fully exploit our intellectual property on inhibitors of TBK1 and IKKepsilon".

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 2,800+ scientific posters on ePosters
  • More than 4,000+ 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.

Related Content

ZoBio, Domainex Partner to support FORMA Therapeutics’ Drug Discovery Programs
ZoBio and Domainex Ltd. announce a collaboration with FORMA Therapeutics to provide NMR-based structural biology services for a substantial panel of FORMA drug targets.
Monday, December 08, 2014
Domainex Awarded Technology Strategy Board Funding
£250,000 grant to support the development of a new drug for the treatment of cancers.
Friday, November 04, 2011
Domainex Ltd Wins Biotechnology Innovation Award
The award was presented by UK Trade & Investment for developing new technologies for streamlining and accelerating the drug discovery process.
Wednesday, August 22, 2007
Scientific News
New Tech Vastly Improves CRISPR/Cas9 Accuracy
A new CRISPR/Cas9 technology developed by scientists at UMass Medical School is precise enough to surgically edit DNA at nearly any genomic location, while avoiding potentially harmful off-target changes typically seen in standard CRISPR gene editing techniques.
New Class of RNA Tumor Suppressors Identified
Two short, “housekeeping” RNA molecules block cancer growth by binding to an important cancer-associated protein called KRAS. More than a quarter of all human cancers are missing these RNAs.
Biologists Induce Flatworms to Grow Heads and Brains of Other Species
Findings shed light on role of a new kind of epigenetic signaling in evolution, could yield clues for understanding birth defects and regeneration.
Turning up the Tap on Microbes Leads to Better Protein Patenting
Mining millions of proteins could become faster and easier with a new technique that may also transform the enzyme-catalyst industry, according to University of California, Davis, researchers.
Mathematical Model Forecasts the Path of Breast Cancer
Chances of survival depend on which organs breast cancer tumors colonize first.
Exploring the Causes of Cancer
Queen's research to understand the regulation of a cell surface protein involved in cancer.
Ancient Viral Molecules Essential for Human Development
Genetic material from ancient viral infections is critical to human development, according to researchers at the Stanford University School of Medicine.
Tardigrade's Are DNA Master Thieves
Tardigrades, nearly microscopic animals that can survive the harshest of environments, including outer space, hold the record for the animal that has the most foreign DNA.
The Secret Behind the Power of Bacterial Sex
Migration between different communities of bacteria is the key to the type of gene transfer that can lead to the spread of traits such as antibiotic resistance, according to researchers at Oxford University.
Farming’s in Their DNA
Ancient genomes reveal natural selection in action.
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
2,800+ scientific and medical posters
A library of 2,500+ scientific videos on LabTube
4,000+ scientific videos