Annotated PGx Gene Information for P2RY1
Submitted by: Katrin Sangkuhl (PharmGKB)
Reviewed by: under review
Submitted date: Mar 21, 2008
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| Gene HGNC Name: | P2RY1 |
|---|---|
| Gene Common Name: | P2 purinoceptor subtype Y1; P2Y purinoceptor 1; platelet ADP receptor |
| Introductory Information: | The product of this gene belongs to the G-protein coupled receptor family. Eight different mammalian P2Y (P2Y1, 2, 4, 6, 11-14) receptor subtypes have been cloned and characterized so far [15955565]. ADP is a full agonist of the P2RY1 receptor, whereas ATP seems to function as a partial agonist [15852224]. P2RY1 is known to be expressed in platelets, but it is also expressed in many other tissue types, such as heart, blood vessels, and neural tissue. The coactivation of both P2RY1 and P2RY12 is necessary for ADP-induced platelet aggregation. The P2RY1 has an important role in the early steps of platelet activation. After ADP binding, P2RY1 couples to G alpha q and triggers calcium mobilization from internal stores resulting in platelet shape change, centralization of platelet granules, and a weak aggregation [15955565]. P2RY1 receptor participates in the aggregation induced by collagen as shown by a reduced amplitude of aggregation and the delay in onset of aggregation in studies using P2RY1 receptor-null mice platelets [10606627]. The human P2RY1 receptor is encoded by an intronless gene, localized at chromosome 3q25 [9039850]. The gene encodes a 372-amino acid polypeptide [8666290]. So far, only the P2RY12 receptor has been validated as a clinically relevant target. Different in vitro and in vivo studies clearly demonstrated that the P2RY1 receptor plays also an essential role in thrombotic states. Therefore, P2RY1 represents a potential target for antiplatelet drugs [16466948]. Several selective antagonists of the P2RY1 receptor have been described in the literature. The naturally occurring adenosine bisphosphate derivates like A3P5PS and A3P5P are either partial agonists or antagonists in various species [15852224]. Based on this structure, potent nucleotide-derived antagonists of the P2RY1 were developed with various adenine base- or ribose-substitutions [9457242]. One of these compounds is MRS2179, characterized as a high affinity competitive antagonist, selective for the P2RY1 receptor [9630335]. Also non-nucleotide P2RY1 antagonists were developed [15852224]. |
| Key PubMed IDs: | 15852224, 15955565, 8666290, 10606627, 9039850 |
| Key Pathways: | Platelet Aggregation Pathway |
| Drugs/Substrates: | N/A |
| Phenotypes/Diseases: | N/A |
| Important Variants: | P2RY1:893C>T, P2RY1:1622A>G |