Format

Send to

Choose Destination
Drug Discov Today. 2012 Apr;17(7-8):359-66. doi: 10.1016/j.drudis.2011.10.007. Epub 2011 Oct 19.

Pharmacological and therapeutic effects of A3 adenosine receptor agonists.

Author information

1
Can-Fite BioPharma Ltd, Kiryat-Matalon, 10 Bareket St, PO Box 7537, Petah-Tikva 49170, Israel.

Abstract

The A(3) adenosine receptor (A(3)AR) coupled to G(i) (inhibitory regulative guanine nucleotide-binding protein) mediates anti-inflammatory, anticancer and anti-ischemic protective effects. The receptor is overexpressed in inflammatory and cancer cells, while low expression is found in normal cells, rendering the A(3)AR as a potential therapeutic target. Highly selective A(3)AR agonists have been synthesized and molecular recognition in the binding site has been characterized. In this article, we summarize preclinical and clinical human studies that demonstrate that A(3)AR agonists induce specific anti-inflammatory and anticancer effects through a molecular mechanism that entails modulation of the Wnt and the NF-κB signal transduction pathways. At present, A(3)AR agonists are being developed for the treatment of inflammatory diseases, including rheumatoid arthritis (RA) and psoriasis; ophthalmic diseases such as dry eye syndrome and glaucoma; liver diseases such as hepatocellular carcinoma and hepatitis.

PMID:
22033198
PMCID:
PMC3289754
DOI:
10.1016/j.drudis.2011.10.007
[Indexed for MEDLINE]
Free PMC Article

Supplemental Content

Full text links

Icon for Elsevier Science Icon for PubMed Central
Loading ...
Support Center