P2RY2 Membrane Protein Introduction

Introduction of P2RY2

P2RY2 is encoded by the P2RY2 gene. It belongs to the G-protein-coupled receptor (GPCR) family which is an important drug target and approximately 34% of all FDA approved drugs targeting this family. It is one of the eight subtypes of P2Y receptors (P2RY1, P2RY2, P2RY4, P2RY6, P2RY11, P2RY12, P2RY13 and P2RY14). P2RY2 possesses seven transmembrane alpha helices and is activated by extracellular nucleotides. Meanwhile, P2RY2 is also known as ATP receptor, P2U purinoceptor 1, P2U receptor 1 and purinergic receptor.

Function of P2RY2 Membrane Protein

The activity of P2RY2 is activated by ATP and UTP, which are the natural agonists for P2RY2. After the activation of P2RY2, like other typical G protein receptor, the intracellular C-terminal of P2RY2 coupled with the G-protein resulting in the phosphorylation of the intracellular C-terminal of P2RY2 and a variety of physiological responses. P2RY2 plays an important role in initiating early inflammatory responses and mediating later regenerative responses required for wound healing, cell migration, and liver regeneration. Since P2RY2 is widely expressed in multiple tissues of our whole body and plays pathophysiological roles in various functionalities, such as lung diseases, cancer progression, and immune diseases. It is a potential therapeutic target of dry eye disease. Diquafosol tetrasodium, which is a pharmaceutical drug for the treatment of dry eye disease, is the first P2RY2 agonists. Currently, numerous agonists targeting P2RY2 are undergoing development to treat different diseases.

Fig.1 Proposed mechanisms of P2RY2. (Khalafalla, 2017)

Application of P2RY2 Membrane Protein in Literature

1. Xu P., et al. Current knowledge on the nucleotide agonists for the P2Y2 receptor. Bioorganic & Medicinal Chemistry. 2018, 26(2):366-375. PubMed ID: 29254895
   
   

   This article reports the proposed structure and functions of the P2Y2 receptor and summarizes the structure-activity relationship of some more efficient agonists, which are in undergoing development stage, targeting P2Y2 receptor.

2. Lau O.C., et al. P2Y(2) receptor agonists for the treatment of dry eye disease: a review. Clinical Ophthalmology. 2014, 8:327-334. PubMed ID: 24511227
   
   

   This article reviews the recent advances in the understanding of the dry eye disease and reveals the importance of P2Y2 receptor in the treatment of dry eye disease.

3. Woods L.T, et al. P2Y2R deletion ameliorates sialadenitis in IL-14α-transgenic mice. Oral Diseases.2018, 24(5):761-771. PubMed ID: 29297959
   
   

   Authors in this group apply interleukin-14α-transgenic mice to investigate the role of P2RY2 in autoimmune endocrinopathy. The results of this study suggest that P2Y2 receptor regulates numerous inflammatory responses because it is unregulated during salivary gland inflammation.

4. Conroy S., et al. Synthesis and Evaluation of the First Fluorescent Antagonists of the Human P2Y2 Receptor Based on AR-C118925. J. Med. Chem.2018, 61(7):3089-3113. PubMed ID: 29558126
   
   

   This article focuses on the synthesis and development of the new non-nucleotide human P2Y2 receptor antagonists. The authors apply the NanoBRET-based fluorescent assay to evaluate the affinities of the new series of antagonists with astrocytoma cells expressing untagged hP2Y2R.

5. Adamson S.E., et al. Myeloid P2Y2 receptor promotes acute inflammation but is dispensable for chronic high-fat diet-induced metabolic dysfunction. Purinergic Signalling. 2018, 14(1):19-26. PubMed ID: 29086245
   
   

   This article investigates the role of P2Y2 receptor in acute inflammation mice models. The authors of this article show that P2Y2 receptor is important in mediating acute inflammation because P2Y2 receptor deficiency results in the decreased inflammation.

P2RY2 Preparation Options

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Reference

1. Khalafalla FG., et al. (2017) P2Y2 Nucleotide Receptor Prompts Human Cardiac Progenitor Cell Activation by Modulating Hippo Signaling. Circul. Res. 121(11):1224.

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