Target intelligence / Profile preview

P2Y purinoceptor 6 (P2Y6) (P2Y6)

Target
P2Y6
Molecular classification
G protein-coupled receptor, Purinergic receptor, Receptor
01

Overview

The P2Y purinoceptor 6 (P2Y6) is a G protein-coupled receptor (GPCR) that is primarily activated by the extracellular nucleotide uridine diphosphate (UDP) (UniProt P41231). It belongs to the P2Y receptor family and is coupled to the Gq/11 protein, leading to the activation of phospholipase C and subsequent intracellular calcium mobilization (IUPHAR/BPS Guide to PHARMACOLOGY). P2Y6 is widely expressed in various tissues, including the immune system, cardiovascular system, and central nervous system, where it plays a critical role in mediating inflammatory responses, phagocytosis by microglia, and vascular smooth muscle contraction (Koizumi et al., 2007, Nature). In disease contexts, overactivation of P2Y6 has been linked to chronic inflammatory conditions such as inflammatory bowel disease and asthma, as well as neurodegenerative disorders like Alzheimer's disease (Wen et al., 2020, Frontiers in Pharmacology). Consequently, P2Y6 has emerged as a therapeutic target, with antagonists like MRS2578 and GC021109 being explored for their potential to reduce neuroinflammation and vascular dysfunction (NIH/PubMed).

Other names
P2RY6Purinergic receptor P2Y6UDP receptorP2Y purinoceptor 6
02

Mechanism of action

Agonism or antagonism of the P2Y6 receptor to modulate Gq-protein signaling, phospholipase C activation, and intracellular calcium release, thereby influencing inflammatory and vascular processes.

03

Biological functions

Signal transductionImmune responsePhagocytosisVasoconstrictionCytokine production
04

Disease associations

InflammationNeurodegenerative diseaseCardiovascular diseaseInflammatory bowel diseaseAsthma
05

Safety considerations

Potential for impaired immune response to pathogensAlterations in vascular tone and blood pressure regulationOff-target effects on other P2Y receptor subtypes
06

Interacting drugs

Uridine diphosphate

3 more in the full profile.

07

Biomarkers

P2RY6 mRNA expression levelsExtracellular UDP concentrationsPro-inflammatory cytokine levels (e.g., IL-8)

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