From UTP to AR-C118925, the discovery of a potent non nucleotide antagonist of the P2Y2 receptor
| Autor: | Michael J. Stocks, Iain Walters, Steve Thom, Kenneth McKechnie, John Dixon, Nicholas Kindon, Premji Meghani, Iain G. Dougall, Timothy Johnson, Andrew M. Davis |
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| Rok vydání: | 2017 |
| Předmět: |
0301 basic medicine
Agonist P2Y receptor Chemistry medicine.drug_class Organic Chemistry Clinical Biochemistry Pharmaceutical Science Pharmacology Biochemistry HYDIA 03 medical and health sciences 030104 developmental biology Competitive antagonist Drug Discovery Enzyme-linked receptor medicine Molecular Medicine Selective receptor modulator Kidney disorder Receptor Molecular Biology |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 27:4849-4853 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2017.09.043 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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