Abstract
Pyrimidine nucleotides, including UTP, UDP and UDP-glucose, are important signaling molecules which activate G protein-coupled membrane receptors of the P2Y family. Four distinct pyrimidine nucleotide-sensitive P2Y receptor subtypes have been cloned, P2Y2, P2Y4, P2Y6 and P2Y14. Pharmacological experiments indicate that further subtypes may exist. P2Y2 and P2Y4 receptors are activated by UTP (the P2Y2 and the rat, but not the human P2Y4 receptor are also activated by ATP), the P2Y6 receptor is activated by UDP, and the P2Y14 receptor by UDPglucose. Derivatives and analogs of the physiological nucleotides UTP, UDP and ATP have been synthesized and evaluated in order to obtain enzymatically stable, subtype-selective agonists. P2Y2 agonists are currently in clinical development for cystic fibrosis and dry eye syndrome. Selective antagonists for pyrimidinergic P2Y receptors are still lacking.
Keywords: nucleoside receptors, adenosine receptors, pyrimidinergic receptor, pyrimidine ligand, p2y
Current Pharmaceutical Design
Title: P2-Pyrimidinergic Receptors and Their Ligands
Volume: 8 Issue: 26
Author(s): Christa E. Muller
Affiliation:
Keywords: nucleoside receptors, adenosine receptors, pyrimidinergic receptor, pyrimidine ligand, p2y
Abstract: Pyrimidine nucleotides, including UTP, UDP and UDP-glucose, are important signaling molecules which activate G protein-coupled membrane receptors of the P2Y family. Four distinct pyrimidine nucleotide-sensitive P2Y receptor subtypes have been cloned, P2Y2, P2Y4, P2Y6 and P2Y14. Pharmacological experiments indicate that further subtypes may exist. P2Y2 and P2Y4 receptors are activated by UTP (the P2Y2 and the rat, but not the human P2Y4 receptor are also activated by ATP), the P2Y6 receptor is activated by UDP, and the P2Y14 receptor by UDPglucose. Derivatives and analogs of the physiological nucleotides UTP, UDP and ATP have been synthesized and evaluated in order to obtain enzymatically stable, subtype-selective agonists. P2Y2 agonists are currently in clinical development for cystic fibrosis and dry eye syndrome. Selective antagonists for pyrimidinergic P2Y receptors are still lacking.
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Cite this article as:
Muller E. Christa, P2-Pyrimidinergic Receptors and Their Ligands, Current Pharmaceutical Design 2002; 8 (26) . https://dx.doi.org/10.2174/1381612023392937
DOI https://dx.doi.org/10.2174/1381612023392937 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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