Salk Institute

Technologies Available for Licensing

Screening Platform for Cell Permeable Protein-Protein Interactions (PPI) Antagonists and Agonists

Assay captures all three PPI antagonist classes: Interface Binder, Conformation Trapper, Allosteric Inducer.  

INVENTION: Drs. Leo Li and Geoffery Wahl at the Salk Institute have developed a novel screening platform for the characterization of PPIs, and the discovery of compounds, which can modulate these interactions. This novel-screening platform combines an inducible protein expression system with the bi-molecular luciferase complementation (BiLC) assay, allowing for the interrogation of transient and dynamic PPIs, identification of novel intracellular protein interaction partners, and screening and characterization of PPI antagonists and agonists. 

APPLICATIONS:

  • Characterization of transient and dynamic PPIs
  • Identification of novel PPIs
  • High throughput screening (HTS) of compound libraries for modulation of PPIs
  • Characterization of PPI antagonists and agonists

ADVANTAGES

  • Highly sensitive
  • Can be used with whole cells or cell lysates
  • Can interrogate low affinity PPIs
  • Can access bioavailability and efficacy simultaneously
  • Not limited to only capturing interface binder antagonist classes
  • Screen for compounds that hit intracellular targets
  • Identify compound binding sites and mechanism of action

STAGE OF DEVELOPMENT:   Validated using at least three (3) drug candidates and one (1) FDA approved cancer therapeutic

BACKGROUND: The exploration PPIs as a strategy for the identification of new drug targets holds great potential, but has long been neglected due to various technical difficulties not associated with enzyme or receptor targets. Current methods for evaluating PPIs are not able to monitor low affinity interactions, and conventional screens for compounds that modify these interactions are not able to sufficiently assess bioavailability or functionality of PPI agonists and antagonists. This new screening platform overcomes many of the current limitations associated with drug discovery and PPIs, and has the potential to expand the field of drug discovery to include a whole new class of druggable targets.
.

INVENTORS: Yao-Cheng (Leo)  Li and Geoffrey M. Wahl
PATENT STATUS: US Provisional Application Filed
CONTACT: Michelle A. Booden, Ph.D., 858.453.4100 x1612, mbooden@salk.edu
REFERENCE #: S13010
Patent Information:
Category(s):
Drug Discovery
For Information, Contact:
Michelle Booden
Director, Licensing and Intellectual Property
Salk Institute
mbooden@salk.edu
Inventors:
Keywords:
Drug Discovery
Drug Efficacy
High Throughput Screens
Mdm2
Mdm4
p53
Protein-Protein Interactions
Proteins
Ras
Wahl
© 2017. All Rights Reserved. Powered by Inteum      

Get Involved
Join our online community
Facebook    Facebook
Twitter    Twitter
YouTube    YouTube
RSS    RSS
Contact
Salk Institute for Biological Studies
Street: 10010 North Torrey Pines Rd
City: La Jolla, CA 92037
Email: webrequest@salk.edu
Phone: 858.453.4100
Charity Navigator Rating
© Copyright 2012 Salk Institute for Biological Studies About Scientists & Research News & Media Events Support