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Antagonist of A3 Adenosine Receptor Fluorescent Probes for the Study of Diseases Such as Cancer, Autoimmune Conditions, Dry Eye

Posted May 14 2012 8:00pm

Description of Invention:
Small molecule drugs, A3AR-selective agonists, are currently in advanced clinical trials for the treatment of hepatocellular carcinoma, autoimmune inflammatory diseases, such as rheumatoid arthritis, psoriasis, and dry eye disease, and other conditions. This molecular probe may serve as a companion tool to identify and stratify patient populations based on the prevalence of the target A3 adenosine receptors.

Applications:
Useful tools to study prevalence of this receptor on neutrophils which is predictive of response to the agonist drugs.

Advantages:
Drug screening at this receptor is often done currently using radiolabeled agonists or antagonists of the human A3AR of nanomolar affinity. This method would avoid the use of radioisotopes in this part of the research and development process.

Development Status:
  • Early-stage
  • In vitro data available


Inventors:
Kenneth A Jacobson (NIDDK)


Patent Status:
HHS, Reference No. E-073-2012/0
US, Application No. 61/590,596 filed 25 Jan 2012

(Note: a separate license may be required for the fluorescent portion of the molecule.)

Relevant Publication:
  1. Novel Fluorescent Antagonist as a Molecular Probe in A3 Adenosine Receptor Binding Assays Using Flow Cytometry, manuscript submitted for publication.



For Licensing Information Please Contact:
Betty Tong Ph.D.
NIH Office of Technology Transfer
6011 Executive Blvd. Suite 325,
Rockville, MD 20852
United States
Email: tongb@mail.nih.gov
Phone: 301-594-6565
Fax: 301-402-0220


Ref No: 2437

Updated: 05/2012

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