Corporate Banner
Satellite Banner
Informatics
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
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
Computer Model Could Explain how Simple Molecules Took First Step Toward Life
Two Brookhaven researchers developed theoretical model to explain the origins of self-replicating molecules.
The Mystery of the Instant Noodle Chromosomes
Researchers from the Lomonosov Moscow State University evaluated the benefits of placing the DNA on the principle of spaghetti.
Web App Helps Researchers Explore Cancer Genetics
Brown University computer scientists have developed a new interactive tool to help researchers and clinicians explore the genetic underpinnings of cancer.
An Innovative Algorithm to Decipher How Drugs Work Inside the Body
Researchers at Columbia University Medical Center (CUMC) have developed a computer algorithm that is helping scientists see how drugs produce pharmacological effects inside the body.
How do Networks Shape the Spread of Disease and Gossip?
A team of mathematicians from Oxford University, University of North Carolina at Chapel Hill, and Rutgers University used a set of mathematical rules to encode how a contagion spreads, and then studied the outcomes of these rules.
AncestryDNA and Calico to Research the Genetics of Human Lifespan
Collaboration will analyze family history and genetics to facilitate development of cutting-edge therapeutics.
Informatics Tool Helps Scientists Prioritize Protein Modification Research
Researchers have developed a new informatics technology that analyzes existing data repositories of protein modifications and 3D protein structures to help scientists identify and target research on "hotspots" most likely to be important for biological function.
Software Differences can Skew Medical Scan Results
Differences in software can significantly skew results of medical scans commonly used in clinical care and research.
AMRI, PerkinElmer to Collaborate on Drug Discovery
Albany Molecular Research (AMRI) and PerkinElmer are collaborating to provide drug discovery infrastructure and services in AMRI's newly launched drug discovery center.
Exploring Living cells
JPK reports the exploration of living cells using nanoscale and single molecule techniques through the application of scanning probe microscopy.
Scroll Up
Scroll Down
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!