Selective A1-adenosine receptor antagonists identified using yeast Saccharomyces cerevisiae functional assays

Evaluation of a biased "library" of pyrrolo[2,3-d]pyrimidines using yeast-based functional assays expressing human A1- and A2a-adenosine receptors, led to the A1 selective antagonist 4b. A direct correlation between yeast functional activity and binding data was established. Practical comp...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1999-08, Vol.9 (16), p.2413-2418
Main Authors: CAMPBELL, R. M, CARTWRIGHT, C, SILVERMAN, L, TRUEHEART, J, WEBB, D. R, WILKINSON, V, WITTER, D. J, XIAOBING XIE, CASTELHANO, A. L, CHEN, W, YONG CHEN, DUZIC, E, FU, J.-M, LOVELAND, M, MANNING, R, MCKIBBEN, B, PLEIMAN, C. M
Format: Article
Language:English
Subjects:
Binding, Competitive
Biological and medical sciences
Cell Line
Humans
Hydrogen Bonding
Medical sciences
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems
Pharmacology. Drug treatments
Purinergic P1 Receptor Antagonists
Pyrimidines - chemistry
Pyrimidines - metabolism
Pyrimidines - pharmacology
Radioligand Assay
Receptors, Purinergic P1 - genetics
Receptors, Purinergic P1 - metabolism
Recombinant Proteins - antagonists & inhibitors
Recombinant Proteins - genetics
Recombinant Proteins - metabolism
Saccharomyces cerevisiae - genetics
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Summary:Evaluation of a biased "library" of pyrrolo[2,3-d]pyrimidines using yeast-based functional assays expressing human A1- and A2a-adenosine receptors, led to the A1 selective antagonist 4b. A direct correlation between yeast functional activity and binding data was established. Practical compounds with polar residues at C-4 of the pyrrolopyrimidine system required H-bond donor functionality for high potency.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(99)00398-4