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Updated: Jun 3, 2025

Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors
Published on: September 13, 2013
PURINE FUNCTIONALIZED CONGENERS AS MOLECULAR PROBES FOR ADENOSINE RECEPTORS
Kenneth A Jacobson1, John W Daly1
1Laboratory of Bioorganic Chemistry, National Inst. of Diabetes, Digestive, and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892.
Abstract:
The effects of distal structural changes on biological activity may be studied, using a "functionalized congener" strategy, in which suitably placed chemically reactive chains lead to biologically active conjugates. Probes for photoaffinity labeling, chemical affinity labeling, spectroscopic characterization and affinity chromatography of adenosine receptors have been derived from purine amine congeners (XAC, ADAC for A1-receptors and APEC for A2-receptors). Also, drug conjugates, including prodrugs and lipids, have been designed as potential pharmacological agents.
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