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

CK1D Development Update

Published: Tuesday, August 07, 2012
Last Updated: Tuesday, August 07, 2012
Bookmark and Share
Proteome Sciences has achieved further milestones in the development of inhibitors of the casein kinase 1 delta (CK1d) target in its Alzheimer's disease portfolio.

A second round of structure activity relationship (SAR) modelling of the most active and selective CK1d inhibitors has produced a marked improvement in activity and selectivity against the main anti-target.

Following successful in silico modelling and screening of CK1d a panel of over 600 candidate compounds were identified. To date, around half of these have been tested in an in vitro assay with a good percentage of those tested showing strong activity. After the first round of SAR two compounds PS110 and PS278 were shown to knock down levels of Tau phosphorylation in a recently published human neuronal cell line model over-expressing Tau protein, as measured using proprietary pTau 2.0 & 3.0 assays that are only available through PS Biomarker Services.

In the latest round of SAR analysis we have significantly improved the anti-Ck1d activity of both compounds and for PS278 also substantially improved its selectivity by over seven-fold against the main anti-target. Further profiling of the developed SAR compounds including in vitro and in vivo pharmacokinetic studies will be completed during the summer and evaluation of biological activity assessed in a whole organism model with results expected in the autumn.

"The extensive CK1D in vitro testing programme has been matched with innovative modelling software and has led to new areas of synthetic interest. Molecules from this programme are being tested and early data suggests greater potency and selectivity. Confirmation of these studies will allow selection of the molecules to enter the key in vivo studies in Q3/4 2012." Professor Bill Dawson, non-executive director of Proteome Sciences said, adding  "I am delighted to see the successful interaction between the biological modelling and informatics programmes. It is key to explore the chemical space effectively and quickly so that these interesting series may be rapidly exploited."


Further Information

Join For Free

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 3,200+ scientific posters on ePosters
  • More than 4,700+ 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.

Related Content

Proteome Sciences Signs $2m Contract with Genting TauRx Diagnostic Centre
Contract to develop diagnostic panels to detect Alzheimer’s disease and monitor treatment efficacy.
Tuesday, September 30, 2014
Stroke Biomarker License to Randox
Stroke biomarker to develop and produce diagnostic tests that could increase by fivefold the number of patients treated for stroke.
Friday, April 06, 2012
Completion of Alzheimer’s Plasma Biomarker Study
The preliminary results demonstrate significant diagnostic and prognostic utilities.
Wednesday, April 04, 2012
Scientific News
New Cancer Drug Target in Dual-Function Protein
Scientists at The Scripps Research Institute (TSRI) have identified a protein that launches cancer growth and appears to contribute to higher mortality in breast cancer patients.
Penn State, TB Alliance, and GSK Partner To Discover New Treatments For TB
A new collaboration between TB Alliance, GSK, and scientists in the Eberly College of Science seeks to find new small molecules that can be used to create antibiotics in the fight against tuberculosis (TB).
Molecular Map Provides Clues To Zinc-Related Diseases
Mapping the molecular structure where medicine goes to work is a crucial step toward drug discovery against deadly diseases.
Platelets are the Pathfinders for Leukocyte Extravasation During Inflammation
Findings from the study could help in the prevention and treatment of inflammatory pathologies.
Genetic Research Can Significantly Improve Drug Development
With drug development costs topping $1.2bn (£850 million) to get a single treatment to the point it can be sold and used in the clinic, could genetic analysis save hundreds of millions of dollars?
New Method Opens Door to Development of Many New Medicines
Findings from TSRI reveal human proteins are better drug targets than previously thought.
Diagnosing Systemic Infections Quickly, Reliably
Team develop rapid and specific diagnostic assay that could help physicians decide within an hour whether a patient has a systemic infection and should be hospitalized for aggressive intervention therapy.
What Makes a Good Scientist?
It’s the journey, not just the destination that counts as a scientist when conducting research.
Blood Test That Detects Early Alzheimer’s Disease
A research team, led by Dr. Robert Nagele from Rowan University School of Osteopathic Medicine and Durin Technologies, Inc., has announced the development of a blood test that leverages the body’s immune response system to detect an early stage of Alzheimer’s disease – referred to as the mild cognitive impairment (MCI) stage – with unparalleled accuracy.
A New Approach to Chemical Synthesis
Communesins, originally found in fungus, could hold potential as cancer drugs.
SELECTBIO

SELECTBIO Market Reports
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
3,200+ scientific and medical posters
A library of 2,500+ scientific videos on LabTube
4,700+ scientific videos
Close
Premium CrownJOIN TECHNOLOGY NETWORKS PREMIUM FOR FREE!