Description:

ALLOSTERIC PROBES FOR CB1 CANNABINOID RECEPTOR

INV-14020

INVENTORS:  Ganeshsingh Arjunsingh Thakur, Alexandros Makriyannis, Pushkar Mukund Kulkarni, Abhijit Raghunath Kulkarni, Ritesh B Tichkule

 

Description       

CB1 is a well-known therapeutic target among pharma industry and drug discovery researchers.  Currently, the majority of research and development in this domain is focusing on binding of various agents (such as agonists, antagonists, etc.) to CB1 at its orthosteric site.  However, such techniques are associated with a reduced therapeutic value with many adverse effects.  Though, allosteric modulators are also known in the prior art, their structural analysis has proved to be extremely difficult.  This invention discloses the development and use of novel allosteric probes for binding to CB1s allosteric sites for their thorough identification and characterization.

Value Proposition

The probes:

•Are synthetic derivatives

•Are associated with a prolonged duration of action

•Bind covalently and irreversibly to CB1 receptor’s allosteric site

•Are capable of being used as covalent drugs for treatment of CB1 medicated diseases

•Have an extremely high affinity (as high as 250%) for the binding site as compared to conventional techniques

•Would be commercially useful for the following applications:

oDiagnostics/analytics tools for CB1 allosterism

oMapping of CB1 allosteric sites

oLong lasting modulation of CB1

oAdd-ons to conventional cannabinoid therapy

oTreatment of obesity, pain, cancer, and other related diseases

 

Intellectual Property status

Provisional Application 61/868,794

 

License status

Available for license

 

Patent Information:
For Information, Contact:
Mark Saulich
Associate Director of Commercialization
Northeastern University
m.saulich@northeastern.edu
Inventors:
Ganeshsingh Thakur
Pushkar Kulkarni
Abhijit Kulkarni
Ritesh Tichkule
Keywords:
Chemistry
Drug Discovery & Development
Health
Pharmaceutical Composition