From UTP to AR-C118925, the discovery of a potent non nucleotide antagonist of the P2Y2 receptor
The G protein-coupled P2Y2 receptor, activated by ATP and UTP has been reported as a potential drug target for a wide range of important clinical conditions, such as tumor metastasis, kidney disorders, and in the treatment of inflammatory conditions. However, pharmacological studies on this receptor...
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| Format: | Article |
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Elsevier
2017
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| Online Access: | https://eprints.nottingham.ac.uk/46762/ |
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| author | Kindon, Nicholas Davis, Andrew Dougall, Iain Dixon, John Johnson, Timothy Walters, Iain Thom, Steve McKechnie, Kenneth Meghani, Premji Stocks, Michael |
| author_facet | Kindon, Nicholas Davis, Andrew Dougall, Iain Dixon, John Johnson, Timothy Walters, Iain Thom, Steve McKechnie, Kenneth Meghani, Premji Stocks, Michael |
| author_sort | Kindon, Nicholas |
| building | Nottingham Research Data Repository |
| collection | Online Access |
| description | The G protein-coupled P2Y2 receptor, activated by ATP and UTP has been reported as a potential drug target for a wide range of important clinical conditions, such as tumor metastasis, kidney disorders, and in the treatment of inflammatory conditions. However, pharmacological studies on this receptor have been impeded by the limited reported availability of stable, potent and selective P2Y2R antagonists. This article describes the design and synthesis of AR-C118925, a potent and selective non-nucleotide antagonist of the P2Y2 receptor discovered using the endogenous P2Y2R agonist UTP as the chemical starting point. |
| first_indexed | 2025-11-14T20:03:11Z |
| format | Article |
| id | nottingham-46762 |
| institution | University of Nottingham Malaysia Campus |
| institution_category | Local University |
| last_indexed | 2025-11-14T20:03:11Z |
| publishDate | 2017 |
| publisher | Elsevier |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | nottingham-467622020-05-04T19:07:45Z https://eprints.nottingham.ac.uk/46762/ From UTP to AR-C118925, the discovery of a potent non nucleotide antagonist of the P2Y2 receptor Kindon, Nicholas Davis, Andrew Dougall, Iain Dixon, John Johnson, Timothy Walters, Iain Thom, Steve McKechnie, Kenneth Meghani, Premji Stocks, Michael The G protein-coupled P2Y2 receptor, activated by ATP and UTP has been reported as a potential drug target for a wide range of important clinical conditions, such as tumor metastasis, kidney disorders, and in the treatment of inflammatory conditions. However, pharmacological studies on this receptor have been impeded by the limited reported availability of stable, potent and selective P2Y2R antagonists. This article describes the design and synthesis of AR-C118925, a potent and selective non-nucleotide antagonist of the P2Y2 receptor discovered using the endogenous P2Y2R agonist UTP as the chemical starting point. Elsevier 2017-09-21 Article PeerReviewed Kindon, Nicholas, Davis, Andrew, Dougall, Iain, Dixon, John, Johnson, Timothy, Walters, Iain, Thom, Steve, McKechnie, Kenneth, Meghani, Premji and Stocks, Michael (2017) From UTP to AR-C118925, the discovery of a potent non nucleotide antagonist of the P2Y2 receptor. Bioorganic & Medicinal Chemistry Letters . ISSN 1464-3405 (In Press) P2Y2; Purinergic; AR-C118925; P2; Antagonist https://doi.org/10.1016/j.bmcl.2017.09.043 doi:10.1016/j.bmcl.2017.09.043 doi:10.1016/j.bmcl.2017.09.043 |
| spellingShingle | P2Y2; Purinergic; AR-C118925; P2; Antagonist Kindon, Nicholas Davis, Andrew Dougall, Iain Dixon, John Johnson, Timothy Walters, Iain Thom, Steve McKechnie, Kenneth Meghani, Premji Stocks, Michael From UTP to AR-C118925, the discovery of a potent non nucleotide antagonist of the P2Y2 receptor |
| title | From UTP to AR-C118925, the discovery of a potent non nucleotide antagonist of the P2Y2 receptor |
| title_full | From UTP to AR-C118925, the discovery of a potent non nucleotide antagonist of the P2Y2 receptor |
| title_fullStr | From UTP to AR-C118925, the discovery of a potent non nucleotide antagonist of the P2Y2 receptor |
| title_full_unstemmed | From UTP to AR-C118925, the discovery of a potent non nucleotide antagonist of the P2Y2 receptor |
| title_short | From UTP to AR-C118925, the discovery of a potent non nucleotide antagonist of the P2Y2 receptor |
| title_sort | from utp to ar-c118925, the discovery of a potent non nucleotide antagonist of the p2y2 receptor |
| topic | P2Y2; Purinergic; AR-C118925; P2; Antagonist |
| url | https://eprints.nottingham.ac.uk/46762/ https://eprints.nottingham.ac.uk/46762/ https://eprints.nottingham.ac.uk/46762/ |