A3 Adenosine Receptor (AR) as Anti-inflammatory, Anti-cancer and Anti-ischemic Agents
Posted Dec 29 2011 7:00pm
Description of Invention: Researchers have been pursuing compounds that activate or inhibit adenosine A3 receptors because these cell membrane proteins have a wide range of physiological and disease-related effects and are thus considered to be promising drug targets. The adenosine A3 receptors are G-protein-coupled receptors and are found mostly in brain, lung, liver, heart, kidney, and testis. When this receptor is activated moderately, a cytoprotective effect is observed, such as reducing damage to heart cells from lack of oxygen. However, at high levels of stimulation they can cause cell death. Both agonists and antagonists are being tested for therapeutic potential, for example, treatment of cancer, heart conditions, neurological conditions, pain, asthma, inflammation and other immune implications.
Adenosine receptors have provided fertile leads for pharmaceutical development, and there are currently a variety of adenosinergic compounds advancing toward clinical trials. Therapeutics which target the adenosine A3 receptors is now an emerging focus that the major pharmaceutical companies are developing. Smaller companies are also developing drugs that stem from proprietary technology targeting adenosine A3 receptors. These companies have products in clinical trials for colorectal cancer and rheumatoid arthritis.
This invention pertains to highly potent A3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides.
Tchilibon S, et al. (N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists. J Med Chem. 2005 Mar 24;48(6):1745-1758. [ PMID 15771421 ]
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
Description of Invention:
Researchers have been pursuing compounds that activate or inhibit adenosine A3 receptors because these cell membrane proteins have a wide range of physiological and disease-related effects and are thus considered to be promising drug targets. The adenosine A3 receptors are G-protein-coupled receptors and are found mostly in brain, lung, liver, heart, kidney, and testis. When this receptor is activated moderately, a cytoprotective effect is observed, such as reducing damage to heart cells from lack of oxygen. However, at high levels of stimulation they can cause cell death. Both agonists and antagonists are being tested for therapeutic potential, for example, treatment of cancer, heart conditions, neurological conditions, pain, asthma, inflammation and other immune implications.
Adenosine receptors have provided fertile leads for pharmaceutical development, and there are currently a variety of adenosinergic compounds advancing toward clinical trials. Therapeutics which target the adenosine A3 receptors is now an emerging focus that the major pharmaceutical companies are developing. Smaller companies are also developing drugs that stem from proprietary technology targeting adenosine A3 receptors. These companies have products in clinical trials for colorectal cancer and rheumatoid arthritis.
This invention pertains to highly potent A3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides.
Inventors:
Kenneth A Jacobson (NIDDK)
Patent Status:
HHS, Reference No. E-248-2004/0
US, , Patent No. 7,825,126, Issued 02 Nov 2010
Relevant 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: 1027
Updated: 12/2011