Target intelligence / Profile preview

P2Y purinoceptor 13 (P2Y13) (P2Y13)

Target
P2Y13
Molecular classification
G protein-coupled receptor, Purinergic receptor, P2Y receptor family
01

Overview

The P2Y purinoceptor 13 (P2Y13) is a G protein-coupled receptor (GPCR) that is primarily activated by adenosine diphosphate (ADP) and belongs to the P2Y receptor family [1, 2]. It is highly expressed in the liver, brain, bone marrow, and pancreas, playing a pivotal role in regulating high-density lipoprotein (HDL) metabolism and reverse cholesterol transport [3]. In the liver, P2Y13 activation stimulates the uptake of HDL-cholesterol, making it a significant target for treating atherosclerosis and cardiovascular diseases [3]. Additionally, the receptor is involved in neuroprotective pathways within the central nervous system and regulates the balance of bone formation and resorption [4]. Pharmacological research focuses on P2Y13 agonists to enhance cholesterol clearance and antagonists to address neurodegenerative or bone-related conditions [2]. While no P2Y13-specific drugs are currently FDA-approved, its close relationship with the P2Y12 receptor makes it a key subject in purinergic signaling research [2]. The receptor signals through Gi proteins to inhibit adenylyl cyclase and activate the MAP kinase pathway [1]. Its role in the pancreas involves the regulation of insulin secretion, further linking it to metabolic syndrome [2]. In the bone, it is expressed on both osteoblasts and osteoclasts, influencing bone mass [4]. Overall, P2Y13 represents a multi-faceted therapeutic target with potential applications in metabolic, cardiovascular, and neurological medicine [1, 2, 3, 4].

Other names
P2RY13G-protein coupled receptor 86GPR86GPCR1FKSG77Purinergic receptor P2Y13
02

Mechanism of action

P2Y13 receptor agonists stimulate the hepatic uptake of high-density lipoprotein (HDL) cholesterol, thereby enhancing reverse cholesterol transport [3]. Antagonists of the receptor are studied for their ability to modulate neuroinflammation, hematopoiesis, and bone remodeling by blocking ADP-mediated signaling pathways [4].

03

Biological functions

Signal transductionReverse cholesterol transportNeuroprotectionHematopoiesisBone remodelingADP-mediated signaling
04

Disease associations

Cardiovascular diseaseAtherosclerosisNeurodegenerative diseaseOsteoporosisDiabetes
05

Safety considerations

Potential cross-reactivity with P2Y12 leading to bleeding risksAlterations in bone mineral densityPotential metabolic disturbances in glucose homeostasis
06

Interacting drugs

MRS2211

4 more in the full profile.

07

Biomarkers

HDL-cholesterol levelsBiliary cholesterol secretionADP-stimulated signaling markers

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