Modulation of adenosine receptor affinity and intrinsic efficacy in adenine nucleosides substituted at the 2-position

We have studied the structural determinants of binding affinity and efficacy of adenosine receptor (AR) agonists. Substituents at the 2-position of adenosine have been combined with N 6-substitutions known to enhance human A 3AR affinity. The environment surrounding the 2-position within the putativ...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2004-06, Vol.12 (11), p.2995-3007
Hauptverfasser:	Ohno, Michihiro, Gao, Zhan-Guo, Van Rompaey, Philippe, Tchilibon, Susanna, Kim, Soo-Kyung, Harris, Brian A, Gross, Ariel S, Duong, Heng T, Van Calenbergh, Serge, Jacobson, Kenneth A
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenosine - agonists Adenosine - analogs & derivatives Adenosine - chemistry Agonists Antagonists Binding Binding Sites Biological and medical sciences Cyclic AMP Deoxyadenosines - chemical synthesis Deoxyadenosines - chemistry Deoxyadenosines - metabolism GPCR Humans Medical sciences Models, Molecular Molecular modeling Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Purinergic P1 Receptor Agonists Purines Receptors, Purinergic P1 - genetics Receptors, Purinergic P1 - metabolism Recombinant Proteins - metabolism Structure-Activity Relationship
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