Known and unknown GPCRs now constitute major targets for drug action and development and the P2Y13 receptor may have potential as a viable target for drug development.
The US patent (6,946,244) relates in particular to screening methods to single out compounds that modulate, either up or down, the biological activity of the human P2Y13 receptor.
Research into the P2Y13 receptor, which was cloned and characterised by Didier Communi at the Université Libre de Bruxelles, revealed that ADP is the natural ligand of P2Y13 and that the P2Y13 receptor is mainly expressed in the immune system and the brain.
Studies of knockout mice show that it is involved in the inhibition of dendritic cells by ADP. Other studies indicate that it is involved in the control of ATP release from erythrocytes during hypoxia and in the internalisation of HDL by the liver, the final step in reverse cholesterol transport.
"This new US patent represents an addition to our portfolio of patented purinergic receptors," said Pierre Nokin, President and CEO of Euroscreen.
"It will enable Euroscreen to generate licensing revenues from companies wishing to use the human P2Y13 receptor in their search for innovative drugs."
The issuance of equivalent patent applications in Europe, Japan and Canada will occur in the near future.
More than 300 G protein coupled receptors (GPCRs) have been cloned thus far and it is generally assumed that well over 1000 such receptors exist.
Mechanistically, approximately 30-50 per cent of all clinically relevant drugs act by modulating the functions of various GPCRs.
In fact, approximately 30 per cent of all currently marketed drugs act on one or more GPCRs, and kinases playing an active role in cancer and inflammatory diseases.
This is achieved by either activating the receptors (agonists), or blocking the effects of receptor activation (antagonists).